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Phosphorylation of specific tyrosineand threonine residues in the activation loop of this enzyme by EC 2.7.12.2, mitogen-activated protein kinase kinase (MAPKK) is necessary for enzyme activation. Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline. A distinguishing feature of all MAPKs is the conserved sequence Thr-Xaa-Tyr (TXY). Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth...pk; PMK-1; PMK-2; PMK-3; pp42; pp44mapk; p44mpk; SAPK; STK26; stress-activated protein kinase. Enzyme Commission Number: EC 2.7.11.24. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3144; mitogen-activated protein kinase; EC 2.7.11.24; c-Jun N-terminal kinase; Dp38; ERK; ERK1; ERK2; extracellular signal-regulated kinase; JNK; JNK3α1; LeMPK3; MAP kinase; MAP-2 kinase; MAPK; MBP kinase I; MBP kinase II; microtubule-associated protein 2 kinase; microtubule-associated protein kinase; myelin basic protein kinase; p38Δ; p38-2; p42 mitogen-activated protein kinase; p42mapk; PMK-1; PMK-
mitogen-activated protein kinase kinase
This enzyme is a dual-specific protein kinase and requires mitogen-activated protein kinase kinase kinase (MAPKKK) for activation. It is required for activation of EC 2.7.11.24, mitogen-activated protein kinase. Phosphorylation of MEK1 by Raf involves phosphorylation of two serine residues. Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumour necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischaemic injury. Group: Enzymes. Synonyms: MAP kinase kinase; MAP kinase kinase 4; MAP kinase kinase 7; MAP kinase or ERK . Enzyme Commission Number: EC 2.7.12.2. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3162; mitogen-activated protein kinase kinase; EC 2.7.12.2; MAP kinase kinase; MAP kinase kinase 4; MAP kinase kinase 7; MAP kinase or ERK kinase; MAP2K; MAPKK; MAPKK1; MEK; MEK1; MEK2; MKK; MKK2; MKK4; MKK6; MKK7; STK27. Cat No: EXWM-3162.
mitogen-activated protein kinase kinase kinase
This enzyme phosphorylates and activates its downstream protein kinase, EC 2.7.12.2, mitogen-activated protein kinase kinase (MAPKK) but requires MAPKKKK for activation. Some members of this family can be activated by p21-activated kinases (PAK/STE20) or Ras. While c-Raf and c-Mos activate the classical MAPK/ERK pathway, MEKK1 and MEKK2 preferentially activate the c-Jun N-terminal protein kinase(JNK)/stress-activated protein kinase (SAPK) pathway. Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e...mes. Synonyms: cMos; cRaf; MAPKKK; MAP3K; MAP kinase kinase kinase; MEKK; MEKK1; MEKK2; MEKK3; MEK kinase; Mil/Raf; MLK-like mitogen-activated protein triple kinase; MLTK; MLTKa; MLTKb; REKS; STK28. Enzyme Commission Number: EC 2.7.11.25. CAS No. 146702-84-3. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3145; mitogen-activated protein kinase kinase kinase; EC 2.7.11.25; 146702-84-3; cMos; cRaf; MAPKKK; MAP3K; MAP kinase kinase kinase; MEKK; MEKK1; MEKK2; MEKK3; MEK kinase; Mil/Raf; MLK-like mitogen-activated protein triple kinase; MLTK; MLTKa; MLTKb; REKS; STK28. Cat No: EXWM-3145.
MNK1/2 Inhibitor II, ETP-45835 (ETP45835?MNK Inhibitor II, Mitogen-Activated Protein Kinase-Interacting Kinase Inhibitor II) (4-(3-(Piperidin-4-yl)-1H-pyrazol-5-yl)pyridine, diHCl)
A cell-permeable 3,5-disubstituted pyrazolo compound that acts as a selective MNK inhibitor (IC50=646 and 575nM, respectively, against MNK1 and MNK2) with much reduced or little activity against 24 other kinases (<15% inhibition at 5uM). Reported to exhibit good aqueous solubility (>100uM at pH 7.4) and inhibit the proliferation (IC50=17uM) and cellular eIF4E Ser209 phosphorylation (IC50=4.7uM) of MV4:11 cells. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N? 2HCl. US Biological Life Sciences.
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10Z-Hymenialdisine
Insecticidal and cytotoxic. Potent NF-kappaB inhibitor. Inhibits various pro-inflammatory cytokines such as IL-1, IL-2, IL-6, IL-8, TNF-alpha and nitric oxide (NO) in a variety of cell lines. ATP-competitive kinase inhibitor. Inhibits DNA damage checkpoint at G2, cyclin-dependent kinases CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK4/cyclin D1, CDK5/p25, GSK-3beta and casein kinase 1 (CK1). Potent mitogen-activated protein kinase kinase-1 (MEK-1) inhibitor. MARK (microtubule affinity-regulating kinase) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 500ug, 1mg. Molecular Formula: C??H??BrN?O?, Method for Determining. US Biological Life Sciences.
Isolated from sponge Axinella carteri. A potent inhibitor of mitogen-activated protein kinase kinase-1 (MEK-1) (IC50=6nm). Blocks the in vivo phosphorylation of the microtubule-binding protein tau at sites that are hyperphosphorylated by glycogen synthase kinase-b (GSK-3b) and CDK5/p35 in Alzheimers disease. Inhibitor of DNA damage checkpoint at G2 phase (IC50=6uM), cyclin-dependent kinases CDK1/cyclin B (IC50=22nm), CDK2/cyclin A (IC50=70 nm), CDK2/cyclin E (IC50=40nm), CDK4/cyclin D1 (IC50 = 600nm), CDK5/p25 (IC50=28nm), GSK-3b (IC50=10nm), and casein kinase 1 (CK1) (IC50=35nm). Group: Biochemicals. Grades: Highly Purified. CAS No. 82005-12-7. Pack Sizes: 250ug, 1mg. US Biological Life Sciences.
2-(2-Chloropyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one is used to prepare pyrrolopyridine Inhibitors of Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MK-2). It is also used to synthesize heteroaryl-substituted pyrrolopyridinones and analogs as cdc7 kinase inhibitors and potential antitumor agents. Group: Biochemicals. Grades: Highly Purified. CAS No. 724726-05-0. Pack Sizes: 5mg, 10mg. Molecular Formula: C12H10ClN3O. US Biological Life Sciences.
2-Bromo-1-(2-chloropyridin-4-yl)ethanone hydrobromide is a reagent in the synthesis of pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) (M424495). Group: Biochemicals. Grades: Highly Purified. CAS No. 569667-89-6. Pack Sizes: 100mg, 250mg. Molecular Formula: C7H6Br2ClNO, Molecular Weight: 315.39. US Biological Life Sciences.
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2-Fluoro-4-iodoaniline
2-Fluoro-4-iodoaniline is widely used in the pharmaceutical, chemical and food industries as a fundamental building block to create a variety of important compounds. 2-Fluoro-4-iodoaniline is mostly known as a moiety of TAK-733, a selective inhibitor of mitogen-activated or extracellular signal-regulated protein kinase kinase 2 (MEK2). Group: Biochemicals. Grades: Highly Purified. CAS No. 29632-74-4. Pack Sizes: 25g, 50g. Molecular Formula: C6H5FIN, Molecular Weight: 237.01. US Biological Life Sciences.
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3,3-Diethoxypropionitrile
3,3-Diethoxypropionitrile is a propionitrile derivative used in the preparation of various biologically active compounds such as p38α mitogen-activated protein kinase inhibitors. Group: Biochemicals. Alternative Names: 3, 3-Diethoxypropane nitrile; Cyanoacetaldehyde Diethyl Acetal; Malonaldehydenitrile Diethyl Acetal. Grades: Highly Purified. CAS No. 2032-34-0. Pack Sizes: 1g. US Biological Life Sciences.
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Acumapimod
Acumapimod is a P38 mitogen-activated protein kinase inhibitor with IC50 value of less than 1 μM for p38&alpha. Phase II clinical trials for the treatment of Chronic obstructive pulmonary disease are on-going. Uses: Chronic obstructive pulmonary disease. Synonyms: BCT-197; BCT197; BCT 197; BCT197A2201; Acumapimod;3-(5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl)-N-cyclopropyl-4-methylbenzamide. Grades: 98%. CAS No. 836683-15-9. Molecular formula: C22H19N5O2. Mole weight: 385.42.
AICAR phosphate
AICAR phosphate, is an AMP-activated protein kinase activator, which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes. It stimulates glucose uptake and increases the activity of p38 mitogen-activated protein kinases α and β in skeletal muscle tissue, as well as suppressing apoptosis by reducing production of reactive oxygen compounds inside the cell. Synonyms: Acadesine phosphate; AICA Riboside phosphate. Grades: >98%. CAS No. 681006-28-0. Molecular formula: C9H17N4O9P. Mole weight: 356.23.
Ammocidin
It is produced by the strain of Saccharothrix sp. AJ 9571. It can reduce the phosphorylation level of mitogen-activated protein kinase (MAPK)S6K. It induces apoptosis in Ras Ba/F3-V12 cells with an IC50 of 66 ng/mL, but not in IL-3 Ba/F3-V12 cells with 100 μg/mL. Synonyms: Ammocidin A. Molecular formula: C59H96O21. Mole weight: 1141.38.
Anisomycin (Flagecidin, Antibiotic SA 3097C1, Antibiotic PA 106, Anhydroscopin A, NSC)
Anisomycin is a phenyl methyl enepyrrolidine first isolated from Streptomyces griseolus in 1954 as an antiprotozoan with antifungal activity. Anisomycin acts as an inhibitor of protein synthesis by binding to the 60S ribosomal subunit. Interestingly, anisomycin has found use for the induction of amnesia in animal models. More recently, anisomycin has been demonstrated to induce apoptosis, to be a selective signalling agonist, to activate mitogen-activated protein (MAP) kinases and to be immunomodulatory via its action on T cells. Group: Biochemicals. Alternative Names: ((2R,3S,4S)-2-(4-Methoxybenzyl)-3,4-pyrrolidinediol-3-acetate, 2-[(4-Methoxyphenyl)methyl]-3,4-pyrrolidinediol 3-acetate. Grades: Highly Purified. CAS No. 22862-76-6. Pack Sizes: 25mg, 100mg, 250mg. US Biological Life Sciences.
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anthrax lethal factor endopeptidase
From the bacterium Bacilus anthracis that causes anthrax. One of three proteins that are collectively termed anthrax toxin. Cleaves several MAP kinase kinases near their N-termini, preventing them from phosphorylating the downstream mitogen-activated protein kinases. In peptidase family M34. Group: Enzymes. Synonyms: lethal toxin. Enzyme Commission Number: EC 3.4.24.83. CAS No. 477950-41-7. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-4367; anthrax lethal factor endopeptidase; EC 3.4.24.83; 477950-41-7; lethal toxin. Cat No: EXWM-4367.
Asiaticoside
Antibacterial. Human collagen I synthesis inducer. Anti-wrinkle activity. Shows wound healing activity. Enhances normal human skin cell migration, attachment and growth. Suppresses collagen expression and TGF-beta/Smad signaling by inducing Smad7 and inhibiting TGF-betaRI and TGF-betaRII. Anti-inflammatory. Anti-gastric ulcer. Mitogen-activated protein kinases (MAPKs), nuclear factor-kappaB (NF-kappaB), cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS; NOSII) expression, production of serum tumor necrosis factor (TNF-alpha) and interleukin-6 (IL-6) inhibitor. Apoptosis inducer in cancer cells. Enhances antitumor activity of vincristine in cancer cells. Might be useful in cancer chemotherapy. Anxiolytic. Antidepressant-like activity. Hepatoprotective effects. CYP2C19 and CYP3A4 inhibitor. Neuroprotective. Antileishmanial activity. cPLA2 and sPLA2 inhibitor. Group: Biochemicals. Alternative Names: Blastostimulina, Centelase, Emdecassol, Madecassol, Marticassol, FK1080, BRN 0078195, NSC 166062. Grades: Highly Purified. CAS No. 16830-15-2. Pack Sizes: 10mg, 50mg. Molecular Formula: C48H78O19. US Biological Life Sciences.
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AZD-8330
AZD8330 is an orally active, selective MEK inhibitor with potential antineoplastic activity. AZD8330 specifically inhibits mitogen-activated protein kinase kinase 1 (MEK or MAP/ERK kinase1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. Synonyms: AZD8330; AZD-8330; AZD 8330; ARRY424704; ARRY 424704; ARRY-424704; ARRY704; ARRY-704; ARRY 704. Grades: 0.98. CAS No. 869357-68-6. Molecular formula: C16H17FIN3O4. Mole weight: 461.232.
Berberine chloride hydrate
The plant-based alkaloid berberine has potential therapeutic applications for breast cancer, although a better understanding of the genes and cellular pathways regulated by this compound is needed to define the mechanism of its action in cancer treatment. In this review, the molecular targets of berberine in various cancers, particularly breast cancer, are discussed. Berberine was shown to be effective in inhibiting cell proliferation and promoting apoptosis in various cancerous cells. Some signaling pathways affected by berberine, including the MAP (mitogen-activated protein) kinase and Wnt/β-catenin pathways, are critical for reducing cellular migration and sensitivity to various growth factors. Treatment with BBR(Berberine) in rats on the atherogenic diet reduced plasma total cholesterol and nonHDL cholesterol levels by 29%-33% and 31%-41%, respectively, with no significant differences being observed among the three doses. Berberine induced both apoptotic and autophagic death of HepG2 cells, which was associated with a significant activation of AMPK and an increased expression of the inactive form of acetyl-CoA carboxylase (ACC). Berberine did not show major effects on viability of HEK-293 embryonic kidney and HCT116 colon carcinoma cells and was not toxic in concentrations up to 20 μM. Berberine inhibited β-catenin transcriptional activity and attenuated anchorage-independent growth. As a result of berberine treatment, cellular levels of active β-catenin were reduced concomitant with an increase in the expression of E-cadherin. Synonyms: Natural Yellow 18. Grades: >98%. CAS No. 141433-60-5. Molecular formula: C20H18ClNO4. Mole weight: 371.81.
β-Lapachone
β-Lapachone is a naturally occurring quinone obtained from the bark of the lapacho tree (Tabebuia avellanedae), exhibiting anti-inflammatory properties by suppressing the NF-κB activation by blocking IκBα degradation and downregulating the ERK, p38 mitogen-activated protein kinase and Akt pathway. Synonyms: ARQ501, ARQ 501, ARQ-501, beta lapachone; BETA-LAPACHONE; 3,4-DIHYDRO-2,2-DIMETHYL-2H-NAPHTHO[1,2-B]PYRAN-5,6-DIONE; 3,4-DIHYDRO-2,2-DIMETHYL-2H-NAPHTHOL[1,2-B]PYRAN-5,6-DIONE; 2-b)pyran-5,6-dione,3,4-dihydro-2,2-dimethyl-2h-naphtho(; b-Lapachone; B-LAPACHONE,2,2-DIMETHYL-3,4-DIHYDRO-2H-BENZO[H]CHROME. Grades: > 98%. CAS No. 4707-32-8. Molecular formula: C15H14O3. Mole weight: 242.27.
BI-847325
BI-847325 is an orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK) and Aurora kinases, with potential antineoplastic activity. Upon oral administration, MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity of MEK, which both prevents the activation of MEK-dependent effector proteins and inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits the activity of the Aurora kinases A, B and C which may disrupt the assembly of the mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular division and proliferation in Aurora kinase-overexpressing tumor cells. Uses: Designed for use in research and industrial production. Additional or Alternative Names: BI-847325; BI 847325; BI847325. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1207293-36-4. Molecular formula: C29H28N4O2. Mole weight: 464.57. Purity: >98%. IUPACName: (Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide. Canonical SMILES: O=C(NCC)C#CC1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=C(CN(C)C)C=C3)/C4=CC=CC=C4. Product ID: ACM1207293364-1. Alfa Chemistry ISO 9001:2015 Certified.
BMS582949
BMS582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 value of 13nM, which plays a crucial role in regulating the biosynthesis of many inflammatory cytokines including TNFα and IL-1&beta. It is used for the treatment of rheumatoid arthritis. It was developed by Bristol-Myers Squibb and was in clinic phase 2 trials, but now it is terminated. Uses: Bms582949 is used for the treatment of rheumatoid arthritis. Synonyms: 4-[[5-[(Cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide;BMS-582949;PS-540446; BMS 582949; PS 540446; BMS582949; PS540446. Grades: 98%. CAS No. 623152-17-0. Molecular formula: C22H26N6O2. Mole weight: 406.49.
BMS-582949 hydrochloride
BMS-582949 hydrochloride is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 of 13 nM. It displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases including serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. It does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 in vitro. It exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. It is currently under Phase II clinical trials for the treatment of inflammatory diseases. Uses: Bms-582949 hydrochloride is used for the treatment of inflammatory diseases. Synonyms: BMS 582949 hydrochloride; BMS582949 hydrochloride; BMS-582949 hydrochloride; 4-((5-((Cyclopropylamino)carbonyl)-2-methylphenyl)amino)-5-methyl-n-propylpyrrolo(2,1-f)(1,2,4)triazine-6-carboxamide. Grades: >98%. CAS No. 912806-16-7. Molecular formula: C22H27ClN6O2. Mole weight: 442.94.
bpV(phen)
Potent protein phosphotyrosine phosphatase inhibitor Insulin receptor kinase (IRK) inducer. Insulin mimetic in vitro and in vivo. Apoptosis inducer. ERK inducer. Mitogen-activated protein kinase phosphatase-1 (MKP-1) inducer. Angiogenesis inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 171202-16-7. Pack Sizes: 5mg, 25mg. Molecular Formula: K[VO(O2)2C12H8N2]. 3H2O. US Biological Life Sciences.
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CMPD-1
CMPD-1, also called MK2a Inhibitor, inhibits tubulin polymerisation. It inhibit p38α-mediated MK2a phosphorylation (apparent Ki = 330 nM). Synonyms: CMPD1; CMPD-1; CMPD 1; IN1225; IN-1225; IN 1225; 4-[4-(2-fluorophenyl)phenyl]-N-(4-hydroxyphenyl)butanamide; MK2a Inhibitor; MAPKAPK2a Inhibitor; CMPD1; CHEMBL235658; 41179-33-3; IN1225; 4-(2' -Fluorobiphenyl-4-yl)-N-(4-hydroxyphenyl)-butyramide; Mitogen-activated protein kinase-activated protein kinase 2a Inhibitor; MK2a Inhibitor_x000D_; SCHEMBL169905. CAS No. 41179-33-3. Molecular formula: C22H20FNO2. Mole weight: 349.4.
CP654577
CP654577 is a selective p185(erbB2) kinase inhibitor. It could reduce the levels of the activated form of mitogen-activated protein kinase of SKBr3 human breast cancer cells. Synonyms: CP-654577; CP 654577; 3-Azabicyclo(3.1.0)hexane-6-methanol, 3-((4-(4-((3-methoxy-4-phenoxyphenyl)amino)-6-quinazolinyl)phenyl)methyl)-, (1alpha,5alpha,6alpha)-. Grades: 98%. CAS No. 639087-64-2. Molecular formula: C34H32N4O3. Mole weight: 544.65.
Doramapimod
Doramapimod is a highly potent inhibitor of p38 mitogen-activated protein kinase (MAPK). Doramapimod is a potential agent for the treatment of inflammatory diseases. Doramapimod blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation leading to enhanced cytotoxicity and caspase activation. Group: Biochemicals. Alternative Names: N-[3-(1,1-Dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]-N'-[4-[2-(4-morpholinyl)ethoxy]-1-naphthalenyl]urea; BIRB 796BS; Birb 796. Grades: Highly Purified. CAS No. 285983-48-4. Pack Sizes: 10mg. US Biological Life Sciences.
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DOTAP
DOTAP is a cationic lipid structure, used for in vitro and in vivo nucleic acid and protein delivery. DOTAP is a good immunomodulator, the antigen presenting capacity of antigen presenting cells can be obviously improved by preparing cationic liposome by packaging polypeptide or protein antigens and the DOTAP, and the DOTAP can activate the antigen presenting cells through a mitogen-activated protein kinase (MAP) pathway to induce specific immune response, unlike the traditional adjuvant which activates the antigen presenting cells through a Toll-like receptor pathway. Synonyms: 1,2-Dioleoyloxy-3-(trimethylammonium)propane; 1,2-Dotap; N,N,N-Trimethyl-2,3-bis((-1-oxo-octadecenyl)oxy)-(Z,Z)-1-propanaminium; N,N,N-Trimethyl-2,3-bis(oleoyloxy)propan-1-aminium. CAS No. 113669-21-9. Molecular formula: C42H80NO4. Mole weight: 663.09.
E6201
E6201 is a synthetic, fungal metabolite analogue inhibitor of mitogen-activated protein kinase kinase 1 (MEK-1) and mitogen-activated protein kinase kinase kinase 1 (MEKK-1) with potential antipsoriatic and antineoplastic activities. MEK-1/MEKK-1 inhibitor E6201 specifically binds to and inhibits the activities of MEK-1 and MEKK-1, which may result in the inhibition of tumor cell proliferation. MEK-1 and MEKK-1 are key components in the RAS/RAF/MEK/MAPK signaling pathway, which regulates cell proliferation and is frequently activated in human cancers. Synonyms: E6201; E 6201; E-6201; ER 806201; ER806201; ER-806201; LL-Z1640-2. CAS No. 603987-35-5. Molecular formula: C21H27NO6. Mole weight: 389.45.
FR-167653
FR-167653 is a p38 mitogen-activated protein kinase inhibitor, which suppresses the development of endometriosis in a murine model. FR-167653 meliorates murine bleomycin-induced pulmonary fibrosis. Uses: Anti-inflammatory agents, non-steroidal. Synonyms: FR-167653; FR 167653; FR167653. CAS No. 158876-66-5. Molecular formula: C24H20FN5O6S. Mole weight: 525.51.
FR-167653 Free base
FR-167653, a pyrazolo?triazin derivative, has been found to be a cytokine inhibitor as well as P38 mitogen-activated protein kinase inhibitor and was once studied as an anticoagulant. Synonyms: FR167653; FR-167653; FR 167653; 1,?2-Ethanedione, 1-[7-(4-fluorophenyl)?-3,?4-dihydro-8-(4-pyridinyl)?pyrazolo[5,?1-c]?[1,?2,?4]?triazin-2(1H)?-yl]?-2-phenyl-. Grades: 98%. CAS No. 158876-65-4. Molecular formula: C24H18FN5O2. Mole weight: 427.43.
FTI-277
FTI-277, a peptide mimetic of the COOH-terminal Cys-Val-Ile-Met of K-Ras4B that inhibited potently FTase in vitro (IC50 = 500 pM) and was highly selective for FTase over geranylgeranyltransferase I (GGTase I) (IC50 = 50 nM). FTI-277, the methyl ester derivative of FTI-276, was extremely potent (IC50 = 100 nM) at inhibiting H-Ras, but not the geranylgeranylated Rap1A processing in whole cells. Treatment of H-Ras oncogene-transformed NIH 3T3 cells with FTI-277 blocked recruitment to the plasma membrane and subsequent activation of the serine/threonine kinase c-Raf-1 in cells transformed by farnesylated Ras (H-RasF), but not geranylgeranylated, Ras (H-RasGG). FTI-277 induced accumulation of cytoplasmic non-farnesylated H-Ras that was able to bind Raf and form cytoplasmic Ras/Raf complexes in which Raf kinase was not activated. Furthermore, FTI-277 blocked constitutive activation of mitogen-activated protein kinase (MAPK) in H-RasF, but not H-RasGG, or Raf-transformed cells. FTI-277 also inhibited oncogenic K-Ras4B processing and constitutive activation of MAPK, but the concentrations required were 100-fold higher than those needed for H-Ras inhibition. The results demonstrate that FTI-277 blocks Ras oncogenic signaling by accumulating inactive Ras/Raf complexes in the cytoplasm, hence preventing constitutive activation of the MAPK cascade. Uses: Radiation-sensitizing agents. Synonyms: FTI-277; FTI 277; FTI277. CAS No. 170006-73-2. Molecular formula: C22H29N3O3S2. Mole weight: 447.612.
GDC-0623
GDC-0623 is an orally active, selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Synonyms: GDC0623; GDC-0632; GDC 0632; G868; G 868; G-868. CAS No. 1168091-68-6. Molecular formula: C16H14FIN4O3. Mole weight: 456.216.
GDC-0994
GDC-0994, also known as RG7842, is an orally available inhibitor of extracellular signal-regulated kinase (ERK), with potential antineoplastic activity. Upon oral administration, GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. This prevents ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in a variety of tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. Uses: Antineoplastic agents. Synonyms: GDC0994; GDC 0994; RG7842; RG-7842; RG 7842; Ravoxertinib. CAS No. 1453848-26-4. Molecular formula: C21H18ClFN6O2. Mole weight: 440.863.
Ginsenoside F4
Ginsenoside F4 is extracted from the root of Panax ginseng C. A. Mey. It has inhibitory effect on human lymphocytoma JK cell by inducing its apoptosis. It was found to strongly inhibit activation of p38 mitogen-activated protein kinase in signal transduction pathways. Synonyms: Ginsenoside Rg6; (20E)-Ginsenoside F4. Grades: >98%. CAS No. 181225-33-2. Molecular formula: C42H70O12. Mole weight: 767.
GNE-495
GNE-495 is a Selective MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) Inhibitor. IC50 value is 3.7 nM. GNE-495 shows excellent potency and good PK In vivo. GNE-495 was used to demonstrate in vivo efficacy in a retinal angiogenesis model recapitulating effects that are observed in the inducible Map4k4 knockout mice. Synonyms: GNE-495; GNE 495; GNE495. 8-amino-N-(1-(cyclopropanecarbonyl)azetidin-3-yl)-2-(3-fluorophenyl)-1,7-naphthyridine-5-carboxamide. Grades: 98%. CAS No. 1449277-10-4. Molecular formula: C22H20FN5O2. Mole weight: 405.43.
Gossypetin
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities [1]. Uses: Scientific research. Group: Natural products. CAS No. 489-35-0. Pack Sizes: 1 mg; 5 mg. Product ID: HY-119917.
GYY-4137 Morpholine salt
GYY-4137 Morpholine salt is a novel water-soluble and slow releasing Hydrogen sulfide(H2S) donor. It protects against myocardial ischemia and reperfusion injury by attenuating oxidative stress and apoptosis in rats. It inhibits the inflammatory response by suppressing the activation of nuclear factor-kappa B and mitogen-activated protein kinases in Coxsackie virus B3-infected rat cardiomyocytes. It exhibits potent anti-cancer activity. It exhibits vasodilator and antihypertensive activity in rats, in either the acute or chronic hypertension models. It does not influence vascular smooth muscle cell viability in culture. It also protects against endotoxic shock in rats, inhibiting tumor necrosis factor-α, interleukin (IL)-1β, and IL-6 production and reducing NF-κB activation, iNOS and cyclooxygenase-2 expression, and NO and prostaglandin E2 generation. Uses: Gyy-4137 morpholine salt inhibits the inflammatory response. it exhibits potent anti-cancer activity. it exhibits vasodilator and antihypertensive activity. Synonyms: GYY4137; GYY-4137; GYY 4137; GYY 4137 morpholine salt; ZYJ1122; ZYJ 1122; ZYJ-1122. GYY4137 Morpholine salt;(4-Methoxyphenyl)morpholino-phosphinodithioic acid compound with morpholine;ZYJ1122 morpholine salt;ZYJ-1122 morpholine salt. Grades: ≥95%. CAS No. 106740-09-4. Molecular formula: C15H25N2O3PS2. Mole weight: 376.47.
ISCK03
ISCK03 is a potent c-kit inhibitor. ISCK03 inhibits SCF/c-kit signaling in 501mel human melanoma cells and abolishes melanin production in mice and brownish guinea pigs. ISCK03 also inhibited p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. ISCK03 might be used as skin-whitening agents. Uses: Designed for use in research and industrial production. Additional or Alternative Names: ISCK03, ISCK-03, ISCK 03. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 945526-43-2. Molecular formula: C19H21N3O2S. Mole weight: 355.46. Purity: >98%. IUPACName: [4-t-butylphenyl]-N-(4-imidazol-1-yl phenyl)sulfonamide. Canonical SMILES: O=S(N(C1=CC=C(C(C)(C)C)C=C1)C2=CC=C(N3C=CN=C3)C=C2)=O. Product ID: ACM945526432-2. Alfa Chemistry ISO 9001:2015 Certified.
JNJ 17029259
JNJ 17029259 is an selective, nanomolar inhibitors of the vascular endothelial growth factor receptor-2 (VEGF-R2), blocks VEGF-stimulated mitogen-activated protein kinase signaling, proliferation/migration. Uses: Vascular endothelial growth factor receptor-2 (vegf-2) kinase inhibitor. Synonyms: JNJ-17029259; JNJ 17029259; JNJ17029259. 4-[4-(2-aminopropan-2-yl)phenyl]-2-[4-(2-morpholin-4-ylethyl)anilino]pyrimidine-5-carbonitrile. Grades: ≥98%. CAS No. 314267-57-7. Molecular formula: C26H30N6O. Mole weight: 442.56.
A potent agonist and assumed endogenous ligand of GPR55, shown to induce rapid phosphorylation of p38 mitogen-activated protein kinase (MAPK) and its downstream activating transcription factor 2 (ATF2) in both GPR55-transfected HEK293 cells, and in IM-9 lymphoblastoid cells naturally expressing GPR55 at 1uM, while having no effect on vector-transfected cells. In addition, shown to enhance serum induced cell migration in MCF-7 cells over expressing GPR55. Group: Biochemicals. Grades: Highly Purified. CAS No. 796963-91-2. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
LB42708
LB42708 is a potent, orally active and selective nonpeptidic farnesyltransferase inhibitor (FTase inhibitor). LB42708 inhibited VEGF-induced Ras activation and subsequently suppressed angiogenesis in vitro and in vivo by blocking the mitogen-activated protein kinase kinase/extracellular signal-regulated kinase/p38 mitogen-activated protein kinase (MAPK) and phosphatidylinositol 3-kinase (PI3K)/Akt/endothelial nitric-oxide synthase pathways in endothelial cells without altering FAK/Src activation. Synonyms: LB-42708; LB 42708; (1-((1-(4-Bromobenzyl)-1H-imidazol-5-yl)methyl)-4-(naphthalen-1-yl)-1H-pyrrol-3-yl)(morpholino)methanone. Grades: 98%. CAS No. 226929-39-1. Molecular formula: C30H27BrN4O2. Mole weight: 555.47.
LY3214996
LY3214996 is a highly selective and orally available inhibitor of ERK1 an dERK2 (IC50= 5 nM for both enzymes in biochemical assays)and thereby preventing the activation of mitogen-activated protein kinase (MAPK)/ERK-mediated signal transduction pathways. Synonyms: temuterkib; LY-3214996; LY 3214996. CAS No. 1951483-29-6. Molecular formula: C22H27N7O2S. Mole weight: 453.56.
MEK1 Derived Peptide Inhibitor 1
It is a peptide composed of the first 13 amino acids of the human mitogen-activated protein kinase kinase-1 (MEK1). It inhibits the in vitro activation of ERK2 by MEK1. Synonyms: H-Met-Pro-Lys-Lys-Lys-Pro-Thr-Pro-Ile-Gln-Leu-Asn-Pro-OH; L-methionyl-L-prolyl-L-lysyl-L-lysyl-L-lysyl-L-prolyl-L-threonyl-L-prolyl-L-isoleucyl-L-glutaminyl-L-leucyl-L-asparagyl-L-proline. Grades: >98%. Molecular formula: C68H118N18O17S. Mole weight: 1491.84.
Mitogen activated protein kinase from rat, Recombinant
Mitogen-activated protein kinases (MAPK) are protein kinases that are specific to the amino acids serine, threonine, and tyrosine. MAPKs belong to the CMGC (CDK/MAPK/GSK3/CLK) kinase group. MAPKs are involved in directing cellular responses to a diverse array of stimuli, such as mitogens, osmotic stress, heat shock and proinflammatory cytokines. They regulate cell functions including proliferation, gene expression, differentiation, mitosis, cell survival, and apoptosis. > 95% (sds-page), buffered aqueous glycerol solution, recombinant, expressed in e. coli (n-terminal histidine tagged). Group: Enzymes. Synonyms: ERK2; Extracellular-signal regulated kinase; MAP Kinase Activated from rat; MAPK; Mitogen activated protein kinase. Purity: > 95% (SDS-PAGE). MAP kinase. Mole weight: mol wt 42 kDa. Activity: > 500 U/mg. Stability: -70°C. Form: buffered aqueous glycerol solution. Source: E. coli. Species: Rat. ERK2; Extracellular-signal regulated kinase; MAP Kinase Activated from rat; MAPK; Mitogen activated protein kinase. Pack: vial of 100 ng. Cat No: NATE-0443.
MK2 Inhibitor III
MK2 inhibitor III is a cell-permeable and ATP-competitive inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2). It was shown to block LPS-induced synthesis of TNF-α in human monocyte-like U937 cells with IC50 value of 4.4 μM. Synonyms: 2-(2-(Quinolin-3-yl)pyridin-4-yl)-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4(5H)-one hydrate. Grades: ≥95%. CAS No. 1186648-22-5. Molecular formula: C21H16N4O·H2O. Mole weight: 358.4.
ML3403
ML 3403 is a potent and selective p38 mitogen-activated protein kinase (MAPK) inhibitor. MAPK is a key mediator in cytokine-induced signaling events and plays an integral role in disease states including oncogenesis, autoimmune diseases, and inflammatory processes. Therefore, MAPK inhibitors such as ML 3403 provides an attractive strategy for therapeutic intervention. Synonyms: ML 3403; ML-3403; p38 MAP Kinase Inhibitor III; 4-(4-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-5-yl)-N-(1-phenylethyl)pyridin-2-amine. Grades: 98%. CAS No. 549505-65-9. Molecular formula: C23H21FN4S. Mole weight: 404.51.
MLN2480
MLN2480 is an oral, selective pan-Raf kinase inhibitor. The Raf kinases (A-Raf, B-Raf and C-Raf) are key regulators of cell proliferation and survival within the mitogen-activated protein kinase (MAPK) pathway. The MAPK pathway is frequently disregulated in human cancers, often via activating mutations of Ras or Raf. Synonyms: TAK-580; TAK 580; TAK580; MLN 2480; MLN-2480; MLN2480; AMG 2112819; AMG2112819; AMG-2112819. Grades: >98%. CAS No. 1096708-71-2. Molecular formula: C17H12Cl2F3N7O2S. Mole weight: 506.29.
N-Decanoyl-L-homoserine lactone
N-decanoyl-L-homoserine lactone (C10-HSL) is a N-acyl-homoserine lactone (AHL) N-decanoyl-L-homoserine lactone can inhibit primary root growth in Arabidopsis. N-decanoyl-L-homoserine lactone triggers a transient and immediate increase in the concentrations of cytosolic free Ca 2+ and reactive oxygen species ( ROS ), increases the activity of mitogen-activated protein kinase 6 ( MPK6 ), and induces nitric oxide ( NO ) production in Arabidopsis roots [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: C10-HSL. CAS No. 177315-87-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136409.
N-Methylparoxetine
N-Methylparoxetine is a derivative of Paroxetine that induces Apoptosis NSCLC cells by activating mitogen-activated protein kinase ( MAPK ). N-Methylparoxetine has antitumor activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 110429-36-2. Pack Sizes: 250 mg; 500 mg; 1 g; 5 g; 10 g. Product ID: HY-Z3832.
non-specific serine/threonine protein kinase
This is a heterogeneous group of serine/threonine protein kinases that do not have an activating compound and are either non-specific or their specificity has not been analysed to date. Group: Enzymes. Synonyms: A-kinase; AP50 kinase; ATP-protein transphosphorylase; calcium-dependent protein kinase C; calcium/phospholipid-dependent protein kinase; cAMP-dependent protein kinase; cAMP-dependent protein kinase A; casein kinase; casein kinase (phosphorylating); casein kinase 2; casein kinase I; casein kinase II; cGMP-dependent protein kinase; CK-2; CKI; CKII; cyclic AMP-dependent protein kinase; cyclic AMP-dependent protein kinase A; cyclic monophosphate-dependent protein kinase; cyclic nucleotide-dependent protein kinase; cyclin-dependent kinase; cytidine 3',5'-cyclic monophosphate-responsive protein kinase; dsk1; glycogen synthase a kinase; glycogen synthase kinase; HIPK2; Hpr kinase; hydroxyalkyl-protein kinase; hydroxyalkyl-protein kinase; M phase-specific cdc2 kinase; mitogen-activated S6 kinase; p82 kinase; phosphorylase b kinase kinase; PKA; protein glutamyl kinase; pr. Enzyme Commission Number: EC 2.7.11.1. STK. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3128; non-specific serine/threonine protein kinase; EC 2.7.11.1; A-kinase; AP50 kinase;
NSC 663284
NSC 663284 is a potent, irreversible, cell permeable and mixed competitive Cdc25 dual specificity phosphatases inhibitor (IC50= 0.21 μM), and poorly inhibits other phosphatases, including Vaccinia virus VH1-related (IC50 = 4.0 μM), PTP1B (no inhibition), and the mitogen-activated protein kinase phosphatases (MKP) MKP-1 or -3 (no inhibition). Synonyms: 6-chloro-7-(2-morpholin-4-ylethylamino)quinoline-5,8-dione; SPS8I1; SPS-8I1; SPS 8I1; DA3003-1; DA3003 1; DA30031; NSC-663284; NSC 663284; NSC663284. CAS No. 383907-43-5. Molecular formula: C15H16ClN3O3. Mole weight: 321.76.
Org 48762-0
Org 48762-0 is a p38 mitogen-activated protein kinase inhibitor. It can be used for the treatment of autoimmune disease and neuropathic pain. Synonyms: UR-13870, UR 13870, UR13870; 4,6-Bis(4-fluorophenyl)-2-methyl-5-(4-pyridyl)-2H-pyrazolo[3,4-b]pyridine; Org 48762-0. Grades: ≥98% by HPLC. CAS No. 755753-89-0. Molecular formula: C24H16F2N4. Mole weight: 398.41.
p38 MAPK Inhibitor
p38 MAPK inhibitor is a potent inhibitor of p38 MAP kinase with IC50 value of 35 nM. Synonyms: p38 MAP Kinase Inhibitor; p38 Mitogen-activated Protein Kinase Inhibitor; 2-(4-chlorophenyl)-4-(4-fluorophenyl)-5-pyridin-4-yl-1H-pyrazol-3-one. Grades: ≥98%. CAS No. 219138-24-6. Molecular formula: C20H13ClFN3O. Mole weight: 365.8.
p38 MAPK Inhibitor IV
p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38α/β MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38??, and p38δ, respectively. Synonyms: p38 MAP Kinase Inhibitor IV; p38 Mitogen-activated Protein Kinase Inhibitor IV; 2,2'-sulfonylbis(3,4,6-trichlorophenol); 3,4,6-trichloro-2-(2,3,5-trichloro-6-hydroxyphenyl)sulfonylphenol. Grades: ≥98%. CAS No. 1638-41-1. Molecular formula: C12H4Cl6O4S. Mole weight: 456.9.
PD0325901
PD-0325901 is a potent bioavailable and selective MEK inhibitor, which targets mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors. Uses: Reprogramming, self-renewal. Synonyms: PD 0325901; PD 325901. Grades: >98%. CAS No. 391210-10-9. Molecular formula: C16H14F3IN2O4. Mole weight: 482.198.
Perifosine
Perifosine is an orally active alkyl-phosphocholine compound with potential antineoplastic activity. Targeting cellular membranes, perifosine modulates membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. Perifosine has a lower gastrointestinal toxicity profile than the related agent miltefosine. Synonyms: KRX-0401; KRX 0401; KRX0401; NKA17; NSC639966; NSC 639966; NSC-639966; D 21266; D-21266; D21266; D-21266N; N-Dimethylpiperidinium-4-yl(octadecyl)phosphate; 1, 1-Dimethyl-4-[[ (octadecyloxy) hydroxyphosphoryl]oxy]piperidinium inner salt. Grades: >98%. CAS No. 157716-52-4. Molecular formula: C25H52NO4P. Mole weight: 461.668.
PF 06260933 dihydrochloride
PF 06260933 is a highly selective, orally active and small-molecule inhibitor of MAP4K4 (Mitogen-activated protein kinase kinase kinase kinase 4) (IC50 = 140 nM). It also inhibits MINK and TNIK (IC50= 8 and 13 nM, respectively). PF-06260933 dihydrochloride has been shown to improves fasting hyperglycemia in mice. Synonyms: 5-(4-Chlorophenyl)-[3,3'-bipyridine]-6,6'-diamine dihydrochloride; PF-06260933 dihydrochloride; PF06260933 dihydrochloride; PF 06260933 dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1883548-86-4. Molecular formula: C16H13ClN4.2HCl. Mole weight: 369.68.
PF-3644022
PF-3644022 is a potent freely reversible ATP-competitive compound that inhibits MK2 activity (Ki = 3 nM) with good selectivity when profiled against 200 human kinases. PF-3644022 is a benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor α production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation. Group: Biochemicals. Alternative Names: (10R)-9, 10, 11, 12-Tetrahydro-10-methyl-3-(6-methyl-3-pyridinyl)-8H-[1, 4]diazepino[5', 6':4, 5]thieno[3, 2-f]quinolin-8-one. Grades: Highly Purified. CAS No. 1276121-88-0. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
PH-797804
PH-797804 is a diarylpyridinone inhibitor of p38 mitogen-activated protein (MAP) kinase. PH-797804 exhibited exceptionally high specificity against MAP kinases and the related kinases. No cross-reactivity was observed in large panels of kinase screens (selectivity ratio of >500-fold). In cellular assays, PH-797804 demonstrated superior potency and selectivity consistent with the biochemical measurements. PH-797804 has met safety criteria in human phase I studies and is under clinical development for several inflammatory conditions. Understanding the rationale for selectivity at the molecular level helps elucidate the biological function and design of specific p38alpha kinase inhibitors. Synonyms: PH 797804; PH797804; 3-(3-Bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1(2H)-yl)-N,4-dimethylbenzamide. CAS No. 586379-66-0. Molecular formula: C22H19BrF2N2O3. Mole weight: 477.30.
PHA 767491 Dihydrochloride Salt
A potent and selective ATP-competitive dual inhibitor cdc7/cdk9. It blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. Inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. Also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK-2). Group: Biochemicals. Alternative Names: 1,5,6,7-Tetrahydro-2-(4-pyridinyl)-4H-pyrrolo[3,2-c]pyridin-4-one Dihydrochloride;PHA 767491 Dihydrochloride Salt; PF-02334471. Grades: Highly Purified. Pack Sizes: 25mg. US Biological Life Sciences.
Worldwide
PHA-767491 hydrochloride
PHA-767491 hydrochloride is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor, which prevents initiation of DNA replication. It inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. It also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2). Synonyms: CAY-10572 hydrochloride; PHA-767491 hydrochloride; CAY 10572 hydrochloride; PHA 767491 hydrochloride; CAY10572 hydrochloride; PHA767491 hydrochloride. Grades: >98%. CAS No. 942425-68-5. Molecular formula: C12H12ClN3O. Mole weight: 249.7.
Most commonly-used phorbol ester. Binds to and activates protein kinase C (PKC) at nM concentrations. Induces cell growth arrest through a variety of pathways including the mitogen-activated protein kinases (MAPKs), p38 and c-Jun N-terminal kinase (JNK) pathways mediated by cyclin dependent kinase (CDK) inhibitors such as p21WAF1/CIP1, p27KIP1, p15 and p16. Potent mouse skin tumor promoter. Promoter of inducible NOS (iNOS; NOS II). Apoptosis inducer. Potential effective cancer therapeutic agent. Inhibitor of anti-lipolytic activity of insulin. Group: Biochemicals. Alternative Names: PMA; TPA; 12-O-Tetradecanoylphorbol 13-acetate. Grades: Highly Purified. CAS No. 16561-29-8. Pack Sizes: 1mg, 5mg, 10mg. Molecular Formula: C36H56O8, Molecular Weight: 616.83. US Biological Life Sciences.
Worldwide
PLX4032 (Vemurafenib)
Vemurafenib selective BRAFV600E kinase inhibitor; an antitumor agent. Vemurafenib functions by inhibiting the proliferation and mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase and ERK phosphorylation in a panel of tumor cell lines, including melanoma cell lines expressing BRAFV600E or other mutant BRAF proteins altered at codon 600. Group: Biochemicals. Alternative Names: N-[3-[[5-(4-Chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide; PLX4032; RG7204; RO51-85426; Zelboraf. Grades: Highly Purified. CAS No. 918504-65-1. Pack Sizes: 500mg, 1g, 2g, 5g, 10g. US Biological Life Sciences.
Worldwide
PRX 08066
PRX 08066, a selective 5-hydroxytryptamine receptor 2B(5-HT2BR) antagonist, causes selective vasodilation of pulmonary arteries. Its IC50 value is 3.4 nM. It can potentially inhibit the pathologic 5-HT-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (PAH). It reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. It shows effects on the vascular muscularization induced by 5-HT in the in vitro studies. It inhibits 5-HT-induced mitogen-activated protein kinase activation and markedly reduces thymidine incorporation in Chinese hamster ovary cells expressing the human 5-HT2BR in vitro. It decrea...ts and mice without affecting the systemic mean arterial pressure in the animals. It is also found to have anti-proliferative and anti-fibrotic effects. It was developed by Allergan company and is in clinical phase 2 with no progression. Uses: Prx 08066 can potentially inhibit the pathologic 5-ht-induced vascular muscularization and is developed to treat for pulmonary arterial hypertension (pah). it is also found to have anti-proliferative and anti-fibrotic effects. Synonyms: PRX-08066; PRX 08066; PRX08066. 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile. Grades: >98%. CAS No. 866206-54-4. Molecular formula: C19H17ClFN5S. Mole weight: 401.89.
R-130823
R-130823 is a highly selective inhibitor against mitogen-activated protein kinase p38alpha (IC50=22 nM). The release of tumor necrosis factor-alpha, interleukin-1beta, -6 and -8 was inhibited in lipopolysaccharide-stimulated human blood pretreated by R-130823, with IC50 values of 0.089, 0.066, 0.95 and 0.16 microM, respectively. Synonyms: R130823; R 130823; 2-(4-Fluorophenyl)-4-(1-phenethyl-1,2,3,6-tetrahydropyridin-4-yl)-3-(pyridin-4-yl)-1H-pyrrole. CAS No. 321344-32-5. Molecular formula: C28H26FN3. Mole weight: 423.53.
R1487 HCl
R1487 is an orally bioavailable and highly selective inhibitor of p38α mitogen-activated protein kinase, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively. Synonyms: R1487 ; R 1487 ; R-1487 ; R1487 HCl. Grades: 98%. CAS No. 449808-64-4. Molecular formula: C19H19ClF2N4O3. Mole weight: 424.83.
R-268712
R-268712 is a potent and selective inhibitor of TGF-β type I receptor/ALK5 with an IC50 of 2.5 nM, an approximately 5000-fold more selectivity for ALK5 than p38 mitogen-activated protein kinase (MAPK). It suppresses development of renal fibrosis in a unilateral ureteral obstruction model. It also reduces proteinuria, glomerulosclerosis and improves renal function in an anti-Thy1 glomerulonephritis model. Synonyms: R-268712; R 268712; R268712. Grades: >98 %. CAS No. 879487-87-3. Molecular formula: C20H18FN5O. Mole weight: 363.39.
Refametinib
Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor RDEA119 specifically inhibits mitogen-activated protein kinase kinase 1 (MAP2K1 or MAPK/ERK kinase 1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers. Synonyms: RDEA119; RDEA-119; RDEA 119; BAY 869766; BAY-69766; BAY869766; BAY 86 9766; BAY 86-9766; BAY86-9766; BAY 869766. Grades: >98%. CAS No. 923032-37-5. Molecular formula: C19H20F3IN2O5S. Mole weight: 572.338.
Rhein
Rhein is a lipophilic anthraquinone extensively found in medicinal herbs, and has many pharmacological effects, including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities.IC50 value:Target:In vitro: Rhein (0.1 and 1 mg/mL) evidently suppressed cell proliferation and mitogen-activated protein (MAP) kinase activation in human colon adenocarcinoma cells (Caco-2) but significantly lessened H2O2-induced DNA damage and the elevated MDA and ROS levels induced by H2O2/Fe2+ at the concentrations of 0.1-10 mg/mL.In vivo: Oral administration of rhein (150 mg/kg/d) evidently ameliorated renal interstitial fibrotic lesions and attenuated the expression of α-SMA and deposition of fibronectin (FN) in mice with renal interstitial fibrosis induced by unilateral ureteral obstruction. Rhein also suppressed TGF-β1 and its type I receptor expression in obstructed kidneys. The biochemical parameters results of IgAN model rats showed that rhein-prevented and rhein-treated both improved the biochemical parameters and relieved renal pathological injury. The expressions of renal tissue TLR4, TGF-β1, but not TLR9 were significantly elevated in IgAN model rats (P < 0.05). Rhein-prevented and rhein-treated both inhibited TLR4 and TGF-β1 expressions. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Chrysazin-3-carboxylicacid. Product Cat
Rineterkib free base
Rineterkib, also known as LTT-462 or ERK-IN-1, is a ERK1/2 inhibitor which has demonstrated preclinical activity in multiple MAPK activated cancer cells and xenograft models. LTT462 binds to and inhibits ERK, thereby preventing the activation of ERK-mediated signal transduction pathways. This results in the inhibition of ERK-dependent tumor cell proliferation and survival. The mitogen-activated protein kinase (MAPK)/ERK pathway is upregulated in numerous tumor cell types and plays a key role in tumor cell proliferation, differentiation and survival. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Rineterkib; ERK-IN-1; ERK IN 1; ERK IN-1; ERK-IN 1; LTT 462; LTT-462; LTT462. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 1715025-32-3. Molecular formula: C26H27BrF3N5O2. Mole weight: 578.43. Purity: >98%. IUPACName: 4-{3-amino-6-[(1S,3S,4S)-3-fluoro-4-hydroxycyclohexyl]pyrazin-2-yl}-N-[(1S)-1-(3-bromo-5-fluorophenyl)-2-(methylamino)ethyl]-2-fluorobenzamide. Canonical SMILES: O=C(N[C@@H](C1=CC(F)=CC(Br)=C1)CNC)C2=CC=C(C3=NC([C@@H]4C[C@H](F)[C@@H](O)CC4)=CN=C3N)C=C2F. Product ID: ACM1715025323. Alfa Chemistry ISO 9001:2015 Certified.
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