ERK Extracellular signal-regulated kinase

Inhibitors

Cat.No.	Name	Information
M2084	SCH772984	SCH772984 is a novel and selective inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.
M5158	Tauroursodeoxycholic acid（Ursodoxicoltaurine）	Tauroursodeoxycholic acid (Ursodoxicoltaurine) is an endoplasmic reticulum stress inhibitor. It can significantly reduce the expression of apoptotic molecules such as caspase-3 and caspase-12. Tauroursodeoxycholate also suppresses ERK. It is a taurine conjugate of usodeoxycholic acid.
M21097	RLX-33	RLX-33 is a non-peptide relaxin-3/RXFP3 system antagonist.
M20811	XMD8-85 (ERK5-IN-1)	XMD8-85 (ERK5-IN-1) is a selective and potent inhibitor of ERK5 and LRRK2 with IC50s of 0.162 μM and 0.339 μM, respectively.
M20330	WAY-340245	WAY-340245 is a ERK inhibitor.
M14155	Ulixertinib hydrochloride	Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC₅₀ of <0.3 nM against ERK2.
M14154	Magnolin	Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
M14153	Ravoxertinib hydrochloride	Ravoxertinib hydrochloride (GDC-0994 hydrochloride) is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.
M14152	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.
M14151	CC-90003	CC-90003 is an irreversible and selective inhibitor of ERK 1/2 with antitumor activity.
M14150	AX-15836	AX-15836 is a potent and selective ERK5 inhibitor with an IC50 of 8 nM.
M11529	Temuterkib	Temuterkib (LY3214996) is a selective, novel erK1/2 inhibitor with an IC50 of 5 nM against ERK1 and ERK2. It can effectively inhibit intracellular P-RSK1 in cancer cell lines with BRAF and RAS mutations. Temuterkib has strong antitumor activity in cancer models with altered MAPK pathways.
M11181	2,5-Dihydroxyacetophenone	2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers used in food flavoring. 2',5'-Dihydroxyacetophenone significantly inhibits the production of NO by inhibiting the expression of iNOS. 2',5'-Dihydroxyacetophenone significantly reduces the expression levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
M11099	Tenuifoliside A	Tenuifoliside A is isolated from Yuanzhi and has anti-apoptotic and antidepressant effects. In C6 cells, Tenuifoliside A exhibits its neurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signaling pathway.
M11050	Tauroursodeoxycholate dihydrate	Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum stress inhibitor. Tauroursodeoxycholate significantly reduces the expression of apoptotic molecules such as caspase-3 and caspase-12. Tauroursodeoxycholate also suppresses ERK.
M11022	DMU-212	DMU-212 is a resveratrol methylated derivative with anti-division, antiproliferative, antioxidant and apoptosis-promoting activities. DMU-212 causes mitosis to stop by inducing apoptosis and activating the ERK1/2 protein.
M11021	(rel)-AR234960	(rel)-AR234960 is the relatively active configuration of AR234960. AR234960 is a non-peptide MAS (a G protein coupling receptor) agonist that upregulates CTGF mRNA and protein levels through the ERK1/2 signaling pathway in HEK293-MAS cells and adult myocardial fibroblasts.
M10880	Rineterkib hydrochloride	Rineterkib hydrochloride (compound B) is an orally active inhibitor of ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF.
M10741	ERK1/2 inhibitor 2	ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
M10733	Rineterkib	Rineterkib (compound B) is an orally active inhibitor of ERK1/2 that exerts an antiproliferative effect by activating mutations in the MAPK pathway. This activity is particularly associated with KRAS-mutant non-small cell lung cancer, BRAF-mutant non-small cell lung cancer, KRAS-mutant pancreatic cancer, KRAS-mutant colon cancer, and KRAS-mutant ovarian cancer.
M10597	Pamoic acid disodium	Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively.
M10071	KO-947	KO-947 is a potent and selective ERK inhibitor with slow dissociation kinetics.

Signaling Pathways

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ERK Extracellular signal-regulated kinase

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