Signaling Pathway

ERK

ERK

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ERKs (Extracellular-signal-regulated 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. Many different stimuli, including growth factors, cytokines, virus infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens, activate the ERK pathway. In the MAPK/ERK pathway, Ras activates c-Raf, followed by mitogen-activated protein kinase kinase (abbreviated as MKK, MEK, or MAP2K) and then MAPK1/2 (below). Ras is typically activated by growth hormones through receptor tyrosine kinases and GRB2/SOS, but may also receive other signals. ERKs are known to activate many transcription factors, such as ELK1, and some downstream protein kinases. Disruption of the ERK pathway is common in cancers, especially Ras, c-Raf and receptors such as HER2.

ERK Inhibitors & Modulators (21)

Product Name Catalog No. Brief Description
APS-2-79

HY-100627

APS-2-79 is an antagonist of MEK phosphorylation by RAF through direct binding of the KSR active site.

Astragaloside IV

HY-N0431

Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.

Corynoxeine

HY-N0590

Corynoxeine is a potent ERK1/2 inhibitor of key PDGF-BB-induced VSMC proliferation; a useful and prospective compound in the prevention and treatment for vascular diseases.

DEL-22379

HY-18932

DEL-22379 is an ERK dimerization inhibitor with IC50 of 0.5 μM.

ERK5-IN-1

HY-14403

ERK5-IN-1 exhibits potent inhibition of ERK5 with cellular EC50 values of 0.19 μM and enzymatic IC50 values of 0.087 μM and of LRRK2[G2019S] with enzymatic IC50 values of 0.026μM.

FR 180204

HY-12275

FR180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2 with Ki value of 0.31 uM and 0.14 uM respectively; has IC50 values of 0.51 and 0.33 μM in enzymatic assays against ERK1 and ERK2, respectively.

GDC-0994

HY-15947

GDC-0994 is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.

GDC-0994 hydrochloride

HY-15947A

GDC-0994 hydrochloride is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively.

Mogrol

HY-N2312

Mogrol is a biometabolite of mogrosides, and acts via inhibition of the ERK1/2 and STAT3 pathways, or reducing CREB activation and activating AMPK signaling.

Pachymic acid

HY-N0371

Pachymic acid is a lanostrane-type triterpenoid, which possesses anti-emetic, anti-inflammatory, and anti-cancer properties.

Sanguinarine

HY-N0052

Sanguinarine(Pseudochelerythrine) is a benzophenanthridine alkaloid which has anti-microbial, anti-oxidant and anti-inflammatory properties; specific inhibitor of Rac1b.

Sanguinarine chloride

HY-N0052A

Sanguinarine (chloride) is natural product.

SCH772984

HY-50846

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 of 4 nM and 1 nM, respectively.

Tauroursodeoxycholate Sodium

HY-19696A

Tauroursodeoxycholate (TUDCA) inhibits neointimal hyperplasia by reducing proliferation and inducing apoptosis of smooth muscle cells by suppression of ERK via PKCα-mediated MKP-1 induction.

TIC10

HY-15615A

TIC10(ONC-201) is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.

TIC10 isomer

HY-15615

TIC10 isomer(ONC201 isomer) is an isomer of TIC10; TIC10 is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.

Tomatidine

HY-N2149

Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-κB.

VRT752271

HY-15816

VRT752271 is a pyrrole inhibitors of ERK protein kinase.

VX-11e

HY-14178

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK (Extracellular Signal-Regulated Kinase); antitumor agent.

XMD17-109

HY-15665

XMD17-109 is a novel, specific ERK-5 inhibitor with an EC50 4.2 uM in HEK293 cells.