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ERK inhibitor, a reversible thiazolidinedione compound, is a cell-permeable inhibitor that binds ERK2 near its docking domain with a KD of 5 μM and prevents its interaction with protein substrates. Synonyms: Extracellular Regulated Kinase Inhibitor; 3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylene]-2,4-thiazolidinedione, monohydrochloride. Grades: ≥95%. CAS No. 1049738-54-6. Molecular formula: C14H16N2O3S·HCl. Mole weight: 328.8.
ERK Inhibitor - CAS 1049738-54-6
The ERK Inhibitor, also referenced under CAS 1049738-54-6, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
ERK Inhibitor II, FR180204 - CAS 865362-74-9
ERK Inhibitor II, FR 180204, CAS 865362-74-9, is a cell-permeable, potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC?? = 510 nM and 330 nM; Ki = 310 nM and 140 nM, respectively). Group: Fluorescence/luminescence spectroscopy.
ERK Inhibitor III - CAS 331656-92-9
The ERK Inhibitor III, also referenced under CAS 331656-92-9, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
ERK Inhibitor II, Negative Control, FR180209 - CAS 1177970-73-8
The ERK Inhibitor II, Negative Control, also referenced under CAS 1177970-73-8, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
ERK Inhibitor VIII ((S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide)
A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2nM against Erk2; [ATP] = 65uM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4uM; IC50 ≥1uM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100nM WZ4002 with or without 1uM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo. Group: Biochemicals. Grades: Highly Purified. CAS No. 896720-20-0. Pack Sizes: 10mg. Molecular Formula: C??H??Cl?FN?O?. US Biological Life Sciences.
Worldwide
ERK Activation Inhibitor Peptide I, Cell-Permeable
The ERK Activation Inhibitor Peptide I, Cell-Permeable controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
ERK Activation Inhibitor Peptide II, Cell-Permeable
The ERK Activation Inhibitor Peptide II, Cell-Permeable controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
InSolution ERK Inhibitor II, FR180204
The ERK Inhibitor II, FR180204, also referenced under CAS 865362-74-9, controls the biological activity of ERK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
TCS ERK 11e (Potent and Selective ERK2 Inhibitor, 4-[2-[(2-Chloro-4-fluorophenyl)amino]-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide)
Potent and selective extracellular signal-related kinase 2 (ERK2) inhibitor (Ki values are <2, 395, 540 and 852nm for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively). Potently blocks proliferation of HT29 cells (IC50 = 48nm). Orally bioavailable. Group: Biochemicals. Grades: Highly Purified. CAS No. 896720-20-0. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
10Z-Hymenialdisine
10Z-Hymenialdisine is a pan kinase inhibitor (IC50 values are 6, 10, 22, 28, 35, 40, 70, 80, 100, 470, 500, 600, 700 and 700 nM for MEK1, GSK-3β, Cdk1/cyclin B, Cdk5/p25, CK1, Cdk2/cyclin A, Cdk2/cyclin E, ASK-γ, Cdk3/cyclin E, Erk1, PKCγ, Cdk4/cyclin D1, Cdk6/cyclin D2 and PKCα, respectively). 10Z-Hymenialdisine inhibits NF-κB activation and suppresses inflammatory gene expression. Synonyms: Hymenialdisine; (Z)-Hymenialdisine; 4-(2-amino-4-oxo-1H-imidazol-5(4H)-ylidene)-2-bromo-4,5,6,7-tetrahydropyrrolo[2,3-c]azepin-8(1H)-one. Grades: ≥97% by HPLC. CAS No. 82005-12-7. Molecular formula: C11H10BrN5O2. Mole weight: 324.13.
3-(2-Aminoethyl)-5-((4-ethoxyphenyl)meth
3-(2-Aminoethyl)-5-((4-ethoxyphenyl)meth. Uses: Designed for use in research and industrial production. Additional or Alternative Names: Erk Inhibitor. Product Category: Heterocyclic Organic Compound. CAS No. 294675-79-9. Molecular formula: C14H16N2O3S??·HCl. Mole weight: 328.81. Purity: 0.96. IUPACName: 5-[4-chloro-3-(dimethylaminodiazenyl)phenyl]-6-ethylpyrimidine-2,4-diamine. Canonical SMILES: CCC1=C(C(=NC(=N1)N)N)C2=CC(=C(C=C2)Cl)N=NN(C)C. Product ID: ACM294675799. Alfa Chemistry ISO 9001:2015 Certified.
3-Bromo-1H-indazol-5-amine
3-Bromo-1H-indazol-5-amine acts as a reagent for the preparation of Polycyclic indazole derivatives that are ERK inhibitors and their use in the treatment and prevention of cancer, anilino quinazolines as antitumor agents. Group: Biochemicals. Grades: Highly Purified. CAS No. 478837-59-1. Pack Sizes: 100mg, 250mg. Molecular Formula: C7H6BrN3, Molecular Weight: 212.05. US Biological Life Sciences.
An intermediate for polycyclic indazole derivatives that are ERK inhibitors. Group: Biochemicals. Alternative Names: 4-Formyl-1-piperidinecarboxylic Acid 1,1-Dimethylethyl Ester; 1,1-Dimethylethyl 4-Formyl-1-piperidinecarboxylate; 1-(tert-Butoxycarbonyl)-4-formylpiperidine; 1-Boc-4-formylpiperidine; 1-Boc-4-piperidinecarboxalde hyde. Grades: Highly Purified. CAS No. 137076-22-3. Pack Sizes: 1mg. US Biological Life Sciences.
KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K. It blocks Akt signalling through the PI3K pathway, and inhibits cell proliferation while inducing apoptosis of thyroid cancer cells. Synonyms: 6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one. Grades: ≥95%. CAS No. 1374996-60-7. Molecular formula: C20H8N12O2. Mole weight: 448.4.
6-Hydroxyflavone
6-Hydroxyflavone is an orally effective flavonoid compound. 6-Hydroxyflavone can inhibit LPS (HY-D1056) -induced NO production and has anti-inflammatory effects. 6-Hydroxyflavone promotes osteoblast differentiation by activating AKT , ERK 1/2 and JNK signaling pathways. 6-Hydroxyflavone has an inhibitory effect on bovine hemoglobin (BHb) glycosylation. 6-Hydroxyflavone has a kidney protective effect. In addition, 6-Hydroxyflavone enhances GABA-induced current through the Benzodiazepine sites of γ-aminobutyric acid (GABA A ) receptors. 6-Hydroxyflavone shows a clear preference for α2 - and α3 - subtypes, which play an anti-anxiety role [1] [2] [3] [4] [5] [6]. Uses: Scientific research. Group: Natural products. CAS No. 6665-83-4. Pack Sizes: 10 mM * 1 mL; 100 mg. Product ID: HY-N7110.
AAL-993
AAL-993 is a VEGFR tyrosine kinase inhibitor that possesses dual inhibition of VEGFR signaling and HIF-1α expression through ERK inhibition without affecting Akt phosphorylation. Synonyms: AAL 993; AAL993; 2-((4-pyridyl)methyl)amino-N-(3-(trifluoromethyl)phenyl)benzamide. Grades: >98%. CAS No. 269390-77-4. Molecular formula: C20H16F3N3O. Mole weight: 371.36.
Abituzumab
Abituzumab (DI17E6) is a humanised anti- integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK , Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer [1]. Uses: Scientific research. Group: Inhibitory antibodies. Alternative Names: EMD 525797; DI17E6. CAS No. 1105038-73-0. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-P99183.
AG 126
Tyrphostins are protein tyrosine kinase inhibitors developed to inhibit cell growth through blocking the activity of certain GFRK (growth factor receptor kinases). AG 126 selectively inhibits the phosphorylation of ERK1 and ERK2 at 25-50 μM. It also inhibits the production of TNF-α (tumor necrosis factor-α), attenuating signaling through NF-κB, the induced expression of COX-2 and iNOS, and the inflammatory response in animal models. AG 126 is a poor inhibitor of epidermal GFRK with IC50 of 450 μM and platelet-derived GFRK with IC50 > 100 μM. AG 126 may represent a new approach for the therapy of inflammation. Uses: Anti- inflammation. Synonyms: AG126; AG-126; Tyrphostin AG 126; UNII-7YA4AMD1JC; Tyrphostin A 10; alpha-Cyano-(3-hydroxy-4-nitro)cinnamonitrile. Grades: 95%. CAS No. 118409-62-4. Molecular formula: C10H5N3O3. Mole weight: 215.16.
ASN007
ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC 50 values. ASN007 can be used for the research of cancers driven by RAS mutations [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ERK-IN-3. CAS No. 2055597-12-9. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136579.
ASN007 benzenesulfonate
ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC 50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: ERK-IN-3 benzenesulfonate. CAS No. 2055597-39-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-136579A.
Asperosaponin Vi
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP-2/p38 and ERK1/2 pathway. Asperosaponin ? inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: White powder. CAS No. 39524-08-8. Molecular formula: C47H76O18. Mole weight: 929.1. Purity: 0.98. IUPACName: [(3R,4S,5S,6R)-3,4,5-trihydroxy-6-[[(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxymethyl]oxan-2-yl] (6aS,9R)-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-10-[(2S,3R,4S,5S)-3,4,5-trihydroxyoxan-2-yl]oxy-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylate. Canonical SMILES: CC1(CCC2(CCC3(C(=CCC4C3(CCC5C4(CCC(C5(C)CO)OC6C(C(C(CO6)O)O)O)C)C)C2C1)C)C(=O)OC7C(C(C(C(O7)COC8C(C(C(C(O8)CO)O)O)O)O)O)O)C. Product ID: ACM39524088. Alfa Chemistry ISO 9001:2015 Certified.
ASTX029
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor ( IC 50 : 2.7 nM). ASTX029 has anti-cancer activity [1] [2]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2095719-92-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-126288.
ASTX-029
ASTX029 is a highly potent and selective dual-mechanism ERK inhibitor. ASTX029 inhibits both ERK catalytic activity and the phosphorylation of ERK itself by MEK, despite not directly inhibiting MEK activity. ASTX029 preferentially inhibited the proliferation of MAPK-activated cell lines, including those with BRAF or RAS mutations. ASTX029 also demonstrated activity in both in vitro and in vivo models of acquired resistance to MAPK pathway inhibitors. Uses: Designed for use in research and industrial production. Additional or Alternative Names: ASTX-029; ASTX029; ASTX 029. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 2095719-92-7. Molecular formula: C29H31ClFN5O5. Mole weight: 584.05. Purity: >98%. IUPACName: (R)-2-(6-(5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1-oxoisoindolin-2-yl)-N-((S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl)propanamide. Canonical SMILES: ClC(C(C1=CC=C2C(C(N([C@H](C)C(N[C@H](CO)C3=CC(OC)=CC(F)=C3)=O)C2)=O)=C1)=N4)=CN=C4NC5CCOCC5. Product ID: ACM2095719927. Alfa Chemistry ISO 9001:2015 Certified.
AX-15836
AX-15836 is a highly potent and selective ERK5 inhibitor (IC50 = 8 nM) with >1,000-fold selectivity for ERK5 over a panel of over 200 kinases. Synonyms: 2-[2-ethoxy-4-[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]anilino]-5-methyl-11-methylsulfonylpyrimido[4,5-b][1,4]benzodiazepin-6-one; AKOS030210962; ZINC669678933; AX15836; AX 15836; AX-15836. CAS No. 2035509-96-5. Molecular formula: C32H40N8O5S. Mole weight: 648.78.
AZD0364
AZD-0364 is a potent and selective ERK2 inhibitor, which has an IC50 value of 0.6 nM. AZD-0364 is measured in the A375 phospho-p90RSK assays with IC50s of 5.7 nM. AZD-0364 can inhibit the growth of a panel of cancer cell lines. The combination of Selumetinib and AZD-0364 ethanesulfonic acid results in a reduction in tumor growth. Synonyms: AZD-0364; AZD 0364; tizaterkib. Grades: ≥98%. CAS No. 2097416-76-5. Molecular formula: C24H24F2N8O2. Mole weight: 494.50.
Bavachalcone
Bavachalcone inhibited osteoclast formation from precursor cells with the IC(50) of approximately 1.5 microg ml(-1). The activation of MEK, ERK, and Akt by receptor activator of nuclear factor kappaB ligand (RANKL), the osteoclast differentiation factor, was prominently reduced in the presence of bavachalcone. The induction of c-Fos and NFATc1, key transcription factors for osteoclastogenesis, by RANKL was also suppressed by bavachalcone. Bavachalcone exhibited a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro. Bavachalcone had stronger inhibition on UGT1A1 and UGT1A7 than corylin which did not inhibit UGT1A1, UGT1A3, UGT1A7, UGT1A8, UGT1A10, and UGT2B4. Data fitting using Dixon and Lineweaver-Burk plots demonstrated the noncompetitive inhibition of bavachalcone against UGT1A1 and UGT1A7-mediated 4-MU glucuronidation reaction. The values of inhibition kinetic parameters (Ki) were 5.41 μ M and 4.51μ M for UGT1A1 and UGT1A7, respectively. Synonyms: Broussochalcone B. Grades: >98%. CAS No. 28448-85-3. Molecular formula: C20H20O4. Mole weight: 324.37.
BCI
BCI is an allosteric inhibitor of dual-specificity phosphatases (DUSP). BCI treatment of DUSP6-Myc-transfected cells suppresses DUSP6 or DUSP1 activity. BCI induces expansion of myocardial progenitors that ultimately increases heart size in zebrafish embryos via inhibiting DUSP6. BCI also inhibits lung cancer and uveal melanoma cells viability (IC50 = 0.1 to 90 μM). DUSP6 functions a feedback regulator of fibroblast growth factor (FGF) signaling to limit the activity of extracellular signal-regulated kinases (ERKs) 1 and 2. Synonyms: (E)-2-benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one; (2E)-2-Benzylidene-3-(cyclohexylamino)-1-indanone. Grades: 99%. CAS No. 1245792-51-1. Molecular formula: C22H23NO. Mole weight: 317.42.
BCI hydrochloride
BCI hydrochloride is an allosteric inhibitor of Dusp6, acting within the phosphatase domain to prevent the catalytic stimulation of phosphatase activity induced by ERK2 substrate binding. BCI also inhibits lung cancer and uveal melanoma cells viability (IC50 values ranging from 0.1 to 90 μM). It prevents pERK2 dephosphorylation induced by Dusp6 in vitro. It is selective for Dusp6 and Dusp1 over Dusp3/VHR, Cdc25B, and PTP1B, for which it has no activity. Synonyms: 2-Benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one hydrochloride. Grades: ≥95%. CAS No. 95130-23-7. Molecular formula: C22H23NO·HCl. Mole weight: 353.9.
BGB-283
BGB-283 is a selective Epidermal growth factor receptor and Proto oncogene protein b raf inhibitor under the development of BeiGene. BGB-283 shows antitumor activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 can inhibit B-RAFV600E-activated ERK phosphorylation and cell proliferation. In vivo, BGB-283 can lead to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. Phase I clinical trials for the treatment of solid tumours are on-going. Uses: Solid tumours. Synonyms: UNII-8762XZS5ZF; 8762XZS5ZF; BGB-283; BGB 283; BGB283; Beigene-283; Beigene283; Beigene 283; Lifirafenib; Compound 2.2b; Beigene-283; GTPL8958;5-[[(1R,1aS,6bR)-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl]oxy]-3,4-dihydro-1H-1,8-naphthyridin-2-one. Grades: 98%. CAS No. 1446090-77-2. Molecular formula: C25H17F3N4O3. Mole weight: 478.31.
BIX-02188
BIX02188 is a potent MEK5-selective inhibitor with an IC50 of 4.3 nM. BIX02188 inhibits ERK5 catalytic activity, with an IC50 of 810 nM. Synonyms: BIX02188; BIX-02188; BIX 02188. CAS No. 334949-59-6. Molecular formula: C25H24N4O2. Mole weight: 412.493.
BIX 02189
BIX02189 is a selective inhibitor of MEK5 with IC50 of 1.5 nM, also inhibits ERK5 catalytic activity with IC50 of 59 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2. Synonyms: BIX02189; BIX-02189; (Z)-3- ( (3- ( (dimethylamino)methyl)phenylamino) (phenyl)methylene)-N, N-dimethyl-2-oxoindoline-6-carboxamide. Grades: >98%. CAS No. 1094614-85-3. Molecular formula: C27H28N4O2. Mole weight: 440.54.
Bohemine
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. CAS No. 189232-42-6. Molecular formula: C18H24N6O. Mole weight: 340.42. Purity: ≥97%. Product ID: ACM189232426. Alfa Chemistry ISO 9001:2015 Certified. Categories: Bohemanella.
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.
Worldwide
B-Raf inhibitor 1
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 μM and 2 nM for A375 proliferation and A375 p-ERK respectively. Synonyms: B-Raf Inhibitor 1; B-Raf-Inhibitor 1; B-Raf-Inhibitor-1; MDK0403; MDK-0403; MDK 0403. Grades: >98%. CAS No. 1093100-40-3. Molecular formula: C26H19ClN8. Mole weight: 478.94.
B-Raf inhibitor 1 dihydrochloride
B-Raf inhibitor 1 is an inhibitor of B-Raf kinase with IC50 values of 0.31μM and 0.72μM for cell proliferation, respectively in A375 and HCT116. B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model. Synonyms: 1,5-Isoquinolinediamine, N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-, hydrochloride (1:2). Grades: >98%. CAS No. 1191385-19-9. Molecular formula: C26H21Cl3N8. Mole weight: 551.86.
Broussonin E
Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: Powder. CAS No. 90902-21-9. Molecular formula: C17H20O4. Mole weight: 288.3. Purity: 0.98. IUPACName: 5-[3-(2-hydroxy-4-methoxyphenyl)propyl]-2-methoxyphenol. Canonical SMILES: COC1=CC(=C(C=C1)CCCC2=CC(=C(C=C2)OC)O)O. Product ID: ACM90902219. Alfa Chemistry ISO 9001:2015 Certified. Categories: Broussonneti.
Butein
Butein is a cAMP-specific PDE inhibitor with an IC 50 of 10.4 μM for PDE4 [1]. Butein is a specific protein tyrosine kinase inhibitor with IC 50 s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells [2]. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a [3]. Butein is a SIRT1 activator (STAC). Uses: Scientific research. Group: Natural products. Alternative Names: 2,3,4,4-tetrahydroxy Chalcone. CAS No. 487-52-5. Pack Sizes: 10 mM * 1 mL; 2 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-16558.
Cafestol
Cafestol is an orally active diterpenoid and an inhibitor of ERK2. Cafestol has elevated blood lipids, anti-inflammatory, anti-angiogenic and anti-diabetic activities. In addition, Cafestol induces tumor cell apoptosis and autophagy , which can be used in the study of cancer [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. CAS No. 469-83-0. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 20 mg. Product ID: HY-N6257.
Capmatinib
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280; INCB28060. CAS No. 1029712-80-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-13404.
Capmatinib dihydrochloride hydrate
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate. CAS No. 1865733-40-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13404C.
Capmatinib hydrochloride
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor ( IC 50 =0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase [1] [2] [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: INC280 hydrochloride; INCB-28060 hydrochloride. CAS No. 1029714-89-3. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13404B.
CAY10561
The extracellular signal-regulated kinases (ERKs) or classical MAP kinases are widely expressed protein kinase intracellular signalling molecules that are involved in functions including the regulation of meiosis, mitosis, and postmitotic functions in differentiated cells. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 with Ki of 2 nM. It is highly selective for ERK2 and inhibits proliferation of COLO 205 cells with IC50 of 0.54 μM. Synonyms: Pyrazolylpyrrole ERK Inhibitor; CAY 10561; CAY-10561. Grades: ≥98%. CAS No. 933786-58-4. Molecular formula: C22H17Cl2FN4O2. Mole weight: 459.3.
CC-90003
CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity. Uses: Scientific research. Group: Signaling pathways. CAS No. 1621999-82-3. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-112570.
CC-90003
Extracellular-signal regulated kinases (ERKs) are a specific subtype of MAPK that have been extensively linked to regulation of synaptic plasticity and memory formation in many systems. CC-90003 is an irreversible and selective inhibitor of ERK1/2 with IC50s in the 10-20 nM range, which shows good kinase selectivity and antitumor activity in a 258-kinase biochemical assay. Synonyms: CC90003; CC 90003. Grades: ≥98%. CAS No. 1621999-82-3. Molecular formula: C22H21F3N6O2. Mole weight: 458.44.
CCT196969
This active molecular is a novel , paradox-breaking pan-RAF inhibitor with anti-SRC activity and it blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK -ERK. CCT196969 also prevented growth of xenografts derived from patient tumours with resistance to BRAF and MEK inhibitors. Uses: Effective in drug-resistant braf mutant melanoma. Synonyms: CCT196969; CCT-196969; CCT 196969. N-[4-[(3,4-Dihydro-3-oxopyrido[2,3-b]pyrazin-8-yl)oxy]-2-fluorophenyl]-N'-[3-(1,1-dimethylethyl)-1-phenyl-1H-pyrazol-5-yl]urea. Grades: 98%. CAS No. 1163719-56-9. Molecular formula: C27H24FN7O3. Mole weight: 513.52.
CCT241161
This active molecular is a novel , paradox-breaking pan-RAF inhibitor with anti-SRC activity and it blocked growth of BRAF-mutant and NRAS-mutant melanoma cells, inhibiting MEK -ERK. CCT 241161 also prevented growth of xenografts derived from patient tumours with resistance to BRAF and MEK inhibitors. Uses: Effective in drug-resistant braf mutant melanoma. Synonyms: CCT241161; CCT-241161; CCT 241161. 1-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl)-3-(2-(methylthio)-4-((3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yl)oxy)phenyl)urea. Grades: 98%. CAS No. 1163719-91-2. Molecular formula: C28H27N7O3S. Mole weight: 541.62.
CEP 1347
Inhibitor of c-jun N-terminal kinase (JNK) signaling. Rescues motor neurons undergoing apoptosis (EC50 = 20nM). Blocks A β-induced cortical neuron apoptosis (EC50 ~51nM). Does not inhibit ERK1 activity. Neuroprotective. Group: Biochemicals. Alternative Names: (9S,10R,12R)-5-16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester. Grades: Highly Purified. CAS No. 156177-65-0. Pack Sizes: 1mg. Molecular Formula: C33H33N3O5S2.1?2H2O, Molecular Weight: 624.77. US Biological Life Sciences.
Worldwide
CEP-32496
CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2. Phase 1/2. Synonyms: 1-(3-((6,7-dimethoxyquinazolin-4-yl)oxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea; RXDX-105; RXDX 105; RXDX105; CEP32496; CEP-32496; CEP 32496; AC013773; AC 013773; AC-013773 Agerafenib. Grades: >98%. CAS No. 1188910-76-0. Molecular formula: C24H22F3N5O5. Mole weight: 517.46.
CEP-32496 hydrochloride
CEP-32496, also known as AC013773, is an orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. CEP-32496 specifically and selectively inhibits the activity of the mutated form (V600E) of B-raf kinase. This inhibits the activation of the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway and may result in a decrease in the proliferation of tumor cells expressing the mutated B-raf gene. The Raf mutation BRAF V600E, in which valine is substituted for glutamic acid at residue 600, is frequently found in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Synonyms: CEP-32496; CEP32496; CEP 32496; AC013773; AC 013773; AC-013773. CAS No. 1227678-26-3. Molecular formula: C24H23ClF3N5O5. Mole weight: 553.92.
CGP 57380
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC 50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases. Uses: Scientific research. Group: Signaling pathways. CAS No. 522629-08-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10520.
CGP 57380
CGP 57380 is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. Synonyms: CGP-57380; CGP57380; CGP 57380. Grades: >98%. CAS No. 522629-08-9. Molecular formula: C11H9FN6. Mole weight: 244.23.
Cis-Mulberroside A
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: Powder. CAS No. 166734-06-1. Molecular formula: C26H32O14. Mole weight: 568.52. Purity: 0.98. IUPACName: (2S,3R,4S,5S,6R)-2-[3-hydroxy-4-[(Z)-2-[3-hydroxy-5-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyphenyl]ethenyl]phenoxy]-6-(hydroxymethyl)oxane-3,4,5-triol. Canonical SMILES: C1=CC(=C(C=C1OC2C(C(C(C(O2)CO)O)O)O)O)C=CC3=CC(=CC(=C3)OC4C(C(C(C(O4)CO)O)O)O)O. Product ID: ACM166734061. Alfa Chemistry ISO 9001:2015 Certified.
Corynoxeine
Corynoxeine is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation and a useful and prospective compound in the prevention and treatment for vascular diseases. Uses: Antihypertension. Synonyms: corynoxeine; (7R,16E,20α)-16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester; (alphaE,1'R,6'R,7'S,8'aS)-6'-Ethenyl-1,2,2',3',6',7',8',8'a-octahydro-alpha-(methoxymethylene)-2-oxospiro[3H-indole-3,1'(5'H)-indolizine]-7'-acetic acid methyl ester; 16,17,18,19-Tetradehydro-17-methoxy-2-oxocorynoxan-16-carboxylic acid methyl ester; Spiro[3H-indole-3,1'(5'H)-indolizine]-7'-aceticacid, 6'-ethenyl-1,2,2',3',6',7',8',8'a-octahydro-a-(methoxymethylene)-2-oxo-, methyl ester, (aE,1'R,6'R,7'S,8'aS)-. Grades: >98%. CAS No. 630-94-4. Molecular formula: C22H26N2O4. Mole weight: 382.45.
CRT 0066101
Potent inhibitor of protein kinase D (PKD); inhibits all PKD isoforms (IC50 values are 1, 2 and 2.5nM for PKD1, PKD3 and PKD2 respectively). Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKC-alpha, MEK, ERK, c-Raf and c- Src. Reduces proliferation and cell viability of pancreatic cancer cells expressing moderate levels of endogenous PKD1/2. Orally bioavailable. Group: Biochemicals. Alternative Names: 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)phenol dihydrochloride. Grades: Purified. CAS No. 1883545-60-5. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
CRT0066101 hydrochloride
CRT0066101 is an inhibitor of all three PKD isoforms (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively). It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. Synonyms: Phenol, 2-[4-[[(2R)-2-aminobutyl]amino]-2-pyrimidinyl]-4-(1-methyl-1H-pyrazol-4-yl)-, hydrochloride (1:3); (R)-2-(4-((2-Aminobutyl)amino)pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol trihydrochloride; 2-(4-{[(2R)-2-Aminobutyl]amino}pyrimidin-2-yl)-4-(1-methyl-1H-pyrazol-4-yl)phenol trihydrochloride. Grades: ≥95%. CAS No. 1781742-22-0. Molecular formula: C18H22N6O.3HCl. Mole weight: 447.79.
Cudraflavone B
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells. Uses: Designed for use in research and industrial production. Product Category: Inhibitors. Appearance: Powder. CAS No. 19275-49-1. Molecular formula: C25H24O6. Mole weight: 420.45. Purity: 0.98. IUPACName: 8-(2,4-dihydroxyphenyl)-5-hydroxy-2,2-dimethyl-7-(3-methylbut-2-enyl)pyrano[3,2-g]chromen-6-one. Canonical SMILES: CC(=CCC1=C(OC2=CC3=C(C=CC(O3)(C)C)C(=C2C1=O)O)C4=C(C=C(C=C4)O)O)C. Product ID: ACM19275491. Alfa Chemistry ISO 9001:2015 Certified.
Defactinib
Defactinib, also known as VS-6063 and PF-04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is , a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation. Synonyms: N-methyl-4-((4-(((3-(N-methylmethylsulfonamido)pyrazin-2-yl)methyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)benzamide; VS6063; VS 6063; VS-6063; PF04554878; PF-04554878; PF 04554878; PF4554878; PF-4554878. Grades: >98%. CAS No. 1073154-85-4. Molecular formula: C20H21F3N8O3S. Mole weight: 510.496.
DEL22379
DEL22379, also known as NPX800, is ERK dimerization inhibitor. DEL-22379 has been reported to inhibit ERK dimerization which was unaffected by drug-resistant mechanism reactivating the ERK signaling. Uses: Designed for use in research and industrial production. Additional or Alternative Names: DEL22379; DEL-22379; DEL 22379; NPX800; NPX 800; NPX-800. Product Category: Inhibitors. Appearance: To be determined. CAS No. 1693734-80-3. Molecular formula: C26H28N4O3. Mole weight: 444.53. Purity: >98%. IUPACName: N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide. Canonical SMILES: O=C(NC1=CC2=C(NC(/C2=C/C3=CNC4=C3C=C(OC)C=C4)=O)C=C1)CCN5CCCCC5. Product ID: ACM1693734803. Alfa Chemistry ISO 9001:2015 Certified.
DEL-22379
DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ?0.5 μM. Synonyms: DEL-22379; DEL 22379; DEL22379. Grades: 98%. CAS No. 181223-80-3. Molecular formula: C26H28N4O3. Mole weight: 444.53.
Diazepinomicin
Diazepinomicin, also known as TLN-4601, is a small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types cells, inducing cell cycle arrest and apoptosis in PBR-expressing cells. Diazepinomicin can cross the blood-brain barrier (BBB). Synonyms: TLN-4601; TLN 4601; TLN4601; ECO 4601; ECO4601; BU 4664L; ECO 04601; BU4664L; BU-4664L; 4,6,8-trihydroxy-10-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yl)-5H-dibenzo[b,e][1,4]diazepin-11(10H)-one. CAS No. 733035-26-2. Molecular formula: C28H34N2O4. Mole weight: 462.59.
Dosimertinib mesylate
Dosimertinib-d 5 (mesylate) is a potent and orally active EGFR inhibitor. Dosimertinib-d 5 (mesylate) decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d 5 (mesylate) shows antiproliferative and anti-tumor activity. Dosimertinib-d 5 (mesylate) has the potential for the research of non-small-cell lung cancer (NSCLC)[1]. Uses: Scientific research. Group: Isotope-labeled compounds. CAS No. 2403760-72-3. Pack Sizes: 1 mg; 5 mg; 10 mg. Product ID: HY-142283AS.
EBPC
EBPC is a potent and selective aldose reductase inhibitor. It is used to improve the cytotoxicity of anticancer reagents such as cisplatin and doxorubicin in HeLa cervical carcinoma cells via an increase in ERK activity. Synonyms: Ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate; 1-Benzyl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrole-3-carboxylic acid ethyl ester; MFCD00179167; 1-benzyl-4-[ethoxy (hydroxy)methylidene]pyrrolidine-2, 3-dione. Grades: ≥99% by HPLC. CAS No. 4450-98-0. Molecular formula: C14H15NO4. Mole weight: 261.28.
Encorafenib
Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells. The Raf mutation BRAF V600E is frequently upregulated in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival. Synonyms: LGX818; LGX-818; LGX 818; Methyl N-[(2S)-1-[[4-[3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-propan-2-ylpyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate. Grades: ≥98%. CAS No. 1269440-17-6. Molecular formula: C22H27ClFN7O4S. Mole weight: 540.011.
EO 1428
EO 1428 is a selective inhibitor of p38α and p38β2 MAP kinase, but displays no activity at p38γ, p38δ, ERK1/2 and JNK1. EO 1428 inhibits production of inflammatory cytokines including IL-8, TNF-α, IL-6, IL-1β and IL-10 (IC50 - 4, 5, 17, 30 and 74 nM, respectively) and acts against inflammation in murine models of acute and chronic dermatitis. Synonyms: EO-1428; EO 1428; EO1428; (2-Methylphenyl)-[4-[(2-amino-4-bromophenyl)amino]-2-chlorophenyl]methanone. Grades: ≥98% by HPLC. CAS No. 321351-00-2. Molecular formula: C20H16BrClN2O. Mole weight: 415.71.
ERK5-IN-2
ERK5-IN-2 is a submicromolar selective ERK5 inhibitor with oral activity, which can inhibit tumor xenograft growth and basic fibroblast growth factor (bFGF)-driven Matrigel plug angiogenesis. Synonyms: 4-(2-Bromanyl-6-Fluoranyl-Phenyl)Carbonyl-{N}-Pyridin-3-Yl-1{H}-Pyrrole-2-Carboxamide; SCHEMBL17607180; BCP32587; EX-A4938. Grades: 98%. CAS No. 1888305-96-1. Molecular formula: C17H11BrFN3O2. Mole weight: 388.2.
ERK5-IN-5
ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor with anticancer activity. ERK5-IN-5 exhibits good anti-proliferative activity with the IC 50 value of 6.23 μg/mL for A549 cells [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2318792-30-0. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-156450.
FC 99 hydrochloride
FC 99 hydrochloride is an inhibitor of TLR3 expression and suppresses inflammatory responses induced by a synthetic dsRNA (poly(I:C)) and by exogenous IFN-α via IRF3. It inhibits the phosphorylation levels of ERK, JNK, and p38 in varying degrees without altering the total protein. Synonyms: FC 99 hydrochloride; FC99 hydrochloride; FC-99 hydrochloride. Grades: 98%. CAS No. 2734014-73-2. Molecular formula: C15H18N2O.xHCl. Mole weight: 242.32 (free base).
FF-10102-01
FF-10102-01 is a novel and selective inhibitor of spleen tyrosine kinase (Syk). Syk plays a role in downstream pathways in signaling from B-cell receptor (BCR) in B cells and Fc-gamma receptors in macrophages. FF-10102-01 exhibits an inhibitory effect on the phosphorylation of SLP76 and ERK1/2 in THP-1 cells, and on inflammation as well as thrombocytopenia. FF-10102-01 is promisingly to be a drug used for the treatment of autoimmune disease. Uses: The potential treatment of autoimmune disease.
FIPI
FIPI, a derivative of halopemide, is a potent and selective phospholipase D (PLD) inhibitor with IC50 values of 20 and 25 nM for PLD2 and PLD1 respectively. It attenuate mercury-induced lipid signaling leading to protection against cytotoxicity in aortic endothelial cells. It rapidly blocks in vivo PA production with subnanomolar potency. It has good pharmacokinetic parameters in rats. It did not significantly inhibit p38 or ERK phosphorylation in bone marrow-derived macrophages stimulated with lipopolysaccharide. It prevents PLD regulation of F-actin cytoskeleton reorganization, cell spreading, and chemotaxis. Synonyms: 5-Fluoro-2-Indolyl des-Chlorohalopemide; N-[2-[4-(2,3-Dihydro-2-oxo-1H-benzimidazol-1-yl)-1-piperidinyl]ethyl]-5-fluoro-1H-indole-2-carboxamide; 5-Fluoro-N-(2-(4-(2-Oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)piperidin-1-yl)ethyl)-1H-indole-2-carboxamide. Grades: >98 %. CAS No. 939055-18-2. Molecular formula: C23H24FN5O2. Mole weight: 421.47.
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