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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. Grade: ≥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
ERK1/2 inhibitor 1
ERK1/2 inhibitor 1 is a potent and orally bioavailable ERK1/2 inhibitor, inhibiting ERK1 up to 60% at 1 nM and inhibiting ERK2 with an IC50 of 3.0 nM. Synonyms: 2H-Isoindole-2-acetamide, 6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-1,3-dihydro-N-[(1S)-2-hydroxy-1-(3-methylphenyl)ethyl]-α-methyl-1-oxo-, (αR)-; (2R)-2-{6-[5-Chloro-2-(tetrahydro-2H-pyran-4-ylamino)-4-pyrimidinyl]-1-oxo-1,3-dihydro-2H-isoindol-2-yl}-N-[(1S)-2-hydroxy-1-(3-methylphenyl)ethyl]propanamide. Grade: ≥95%. CAS No. 2095719-90-5. Molecular formula: C29H32ClN5O4. Mole weight: 550.05.
ERK1/2 inhibitor 1
ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2095719-90-5. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-112287.
ERK1/2 inhibitor 3
ERK1/2 inhibitor 3, a potent ERK1/2 inhibitor, has the potential to study or prevent cancer, inflammation, or other proliferative diseases. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of MAPK family. (Extracted from patent WO2021218912A1, compound 1). Synonyms: (S)-2-(6-(5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1,1-dioxidobenzo[d]isothiazol-2(3H)-yl)-N-((S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl)propanamide. CAS No. 2737294-99-2. Molecular formula: C28H31ClFN5O6S. Mole weight: 620.09.
ERK1/2 inhibitor 4
ERK1/2 inhibitor 5, a potent ERK1/2 inhibitor, has the potential to study or prevent cancer, inflammation, or other proliferative diseases. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of MAPK family. (Extracted from patent WO2020238776A1). Synonyms: Thieno[3,2-c]pyridine-5(4H)-acetamide, 2-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-6,7-dihydro-α-methyl-4-oxo-, (αR)-. CAS No. 2490396-99-9. Molecular formula: C28H31ClFN5O5S. Mole weight: 604.09.
ERK1/2 inhibitor 6
ERK1/2 inhibitor 6, a potent ERK1/2 inhibitor, has the potential to study or prevent cancer, inflammation, or other proliferative diseases. Mitogen-activated protein kinase (MAPK) plays an extremely important role in the signal transduction pathway, and extracellular signal regulated kinase (ERK) is a member of MAPK family. (Extracted from patent WO2021063335A1, compound 1). Synonyms: (R)-2-(6-(5-chloro-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-4-oxopyrrolo[2,1-f][1,2,4]triazin-3(4H)-yl)-N-((S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl)propanamide. CAS No. 2634816-13-8. Molecular formula: C27H29ClFN7O5. Mole weight: 586.01.
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. Grade: ≥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. Grade: ≥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. Grade: >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. Grade: 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.
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. Synonyms: ASTX 029; ASTX029; ERK1/2 inhibitor 2. CAS No. 2095719-92-7. Molecular formula: C29H31ClFN5O5. Mole weight: 584.04.
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.
AX-15836
AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 2035509-96-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-101846.
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. Grade: ≥98%. CAS No. 2097416-76-5. Molecular formula: C24H24F2N8O2. Mole weight: 494.50.
BAY-885
BAY-885 is a potent and selective ERK5 inhibitor with IC50 of 35 nM. BAY-885 induced apoptosis in breast cancer cells via ER stress/Mcl-1/Bim axis. Synonyms: BAY 885; BAY885. CAS No. 2307249-33-6. Molecular formula: C25H28F3N7O2. Mole weight: 515.53.
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. Grade: 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. Grade: ≥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. Grade: 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.
BIX02189
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 1265916-41-3. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-12056.
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. Grade: >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. Grade: >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). Grade: >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. Grade: ≥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. Grade: ≥98%. CAS No. 1621999-82-3. Molecular formula: C22H21F3N6O2. Mole weight: 458.44.
CCR6 inhibitor 1
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50 >30000 nM), and CCR7 (IC50 = 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation and is used in the study of autoimmune diseases and cancer. Synonyms: 2-Pyridinecarboxamide, 4-[4-[[trans-4-[[5-(trifluoromethyl)-2-pyridinyl]amino]cyclohexyl]sulfonyl]phenyl]-; 4-{4-[(trans-4-{[5-(Trifluoromethyl)-2-pyridinyl]amino}cyclohexyl)sulfonyl]phenyl}-2-pyridinecarboxamide. Grade: ≥98%. CAS No. 2437547-04-9. Molecular formula: C24H23F3N4O3S. Mole weight: 504.52.
CCR6 inhibitor 1
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 2437547-04-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-112701.
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. Grade: 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. Grade: 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. Grade: >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. Grade: >98%. CAS No. 522629-08-9. Molecular formula: C11H9FN6. Mole weight: 244.23.
CHIR-98014
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3? and GSK-3?, respectively; it shows less potent activities against cdc2 and erk2. Uses: Scientific research. Group: Signaling pathways. CAS No. 252935-94-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-13076.
Chrysophanol
Chrysophanic acid (Chrysophanol) is a natural anthraquinone with anticancer activity in EGFR-overexpressing SNU-C5 human colon cancer cells. Chrysophanic acid preferentially blocked proliferation in SNU-C5 cells but not in other cell lines (HT7, HT29, KM12C, SW480, HCT116 and SNU-C4) with low levels of EGFR expression. Chrysophanic acid treatment in SNU-C5 cells inhibited EGF-induced phosphorylation of EGFR and suppressed activation of downstream signaling molecules, such as AKT, extracellular signal-regulated kinase (ERK) and the mammalian target of rapamycin (mTOR)/ribosomal protein S6 kinase (p70S6K). Chrysophanic acid (80 and 120 μm) significantly blocked cell proliferation when combined with the mTOR inhibitor, rapamycin. These findings offer the first evidence of anticancer activity for chrysophanic acid via EGFR/mTOR mediated signaling transduction pathway. Chrysophanol is a natural compound found in the roots and rhizomes of Rheum palmatum L. It can be used in cosmetics material. Uses: Anti-inflammatory. Synonyms: 1,8-dihydroxy-3-methylanthracene-9,10-dione. Grade: ≥ 98 %. CAS No. 481-74-3. Molecular formula: C15H10O4. Mole weight: 254.24.
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.
CK2/ERK8-IN-1
CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 μM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 ?M. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 μM, 15.25 μM, and 11.9 μM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1085822-09-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-135906.
CK2/ERK8-IN-1
CK2/ERK8-IN-1 is a dual inhibitor of casein kinase 2 (CK2) and ERK8. It also binds to Pim-1, HIPK2, and DYRK1A. CK2/ERK8-IN-1 induces apoptosis in Jurkat cells when used at concentrations ranging from 10 to 50 μM. Synonyms: TMCB; 4,5,6,7-Tetrabromo-2-(dimethylamino)-1H-benzimidazole-1-acetic acid. Grade: ≥99%. CAS No. 1085822-09-8. Molecular formula: C11H9Br4N3O2. Mole weight: 534.82.
CMC2.24
CMC2.24 is an orally active tricarbonylmethane agent. It is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. Synonyms: TRB-N0224. Grade: 96%. CAS No. 1255639-43-0. Molecular formula: C26H21NO5. Mole weight: 427.45.
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. Grade: ≥95%. CAS No. 1781742-22-0. Molecular formula: C18H22N6O.3HCl. Mole weight: 447.79.
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