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ERK

ERK

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.The ERK pathway is activated by a wide range of stimuli, including as growth factors, cytokines, viral infection, ligands for heterotrimeric G protein-coupled receptors, transforming agents, and carcinogens. Ras stimulates c-Raf in the MAPK/ERK pathway, which is subsequently joined by mitogen-activated protein kinase kinase (also known as MKK, MEK, or MAP2K), followed by MAPK1/2 (see below).

Ras can be triggered by additional cues in addition to growth hormones through GRB2/SOS and receptor tyrosine kinases. Many transcription factors, including ELK1, and some downstream protein kinases are known to be activated by ERKs. Ras, c-Raf, and receptors like HER2 are known to cause disruption of the ERK pathway, which is frequently seen in malignancies.

ERK related products

Structure Cat No. Product Name CAS No. Product Description
(7R)-Eras-4001 V121655 (7R)-Eras-4001 3024878-21-2 (7R)-Eras-4001 is an orally effective KRAS mutant inhibitor with significant selectivity for H-RAS and N-RAS.
(R)-MK-8353 V120232 (R)-MK-8353 2748457-30-7 (R)-MK-8353 ((R)-SCH900353) is the R-enantiomer of MK-8353.
(R)-VX-11e V69825 (R)-VX-11e 1680187-43-2 (R)-VX-11e (Compound 1) is an ERK2 inhibitor.
(S)-BAY 2965501 V69801 (S)-BAY 2965501 2732902-09-7 (S)-BAY 2965501 is the left-handed isomer of BAY 2965501.
(S)-IP-DK143 V122177 (S)-IP-DK143 (S)-IP-DK143 is a polymer micelle formulation.
3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles V87086 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles 287196-91-2 3-Hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles is an inhibitor of bone morphogenetic protein 2 (BMP2) with IC50 of 2.2 μM.
7α,15-Dihydroxydehydroabietic acid V69817 7α,15-Dihydroxydehydroabietic acid 155205-64-4 7α,15-Dihydroxydehydroabietic acid is a natural abietane diterpenoid with anti-angiogenic effects.
AB19 V115625 AB19 AB19 is a potent Vav1 inhibitor.
ADTL-EI1712 V69823 ADTL-EI1712 2414916-45-1 ADTL-EI1712 is an orally bioactive selective dual-target inhibitor of ERK1 and ERK5.
AG126 V33675 AG126 118409-62-4 AG126 is a tyrosine kinase inhibitor (TKI) that can suppress the phosphorylation of ERK1 and ERK2 at 25-50 μM.
Ambuic acid V86914 Ambuic acid 340774-69-8 Ambuic acid has antibacterial activity against Staphylococcus aureus ATCC 6538 strain with an IC50 of 43.9 μM.
Angiogenesis inhibitor 7 V128835 Angiogenesis inhibitor 7 922029-50-3 Angiogenesis inhibitor 7 is a potent angiogenesis inhibitor.
Anticancer agent 231 V87067 Anticancer agent 231 128519-30-2 Anticancer agent 231 (compound P5) is a tyrosine protein kinase inhibitor with an IC50 value of 3.95 μM.
Anticancer agent 301 V128975 Anticancer agent 301 Anticancer agent 301 is an anticancer drug.
Anticancer agent 319 V128991 Anticancer agent 319 Anticancer agent 319 is an anticancer drug.
APS03118 V117507 APS03118 2598870-24-5 APS03118 is an orally effective, potent, and highly selective transfection rearrangement (RET) inhibitor.
ASN-007 benzenesulfonate V51049 ASN-007 benzenesulfonate 2055597-39-0 ERK1/2 inhibitor
ASN007 V41199 ASN007 2055597-12-9 ASN007 (ASN-007) is a novel, potent, orally bioavailable and selective inhibitor of ERK1/2 with robust antitumor activity.
ASTX029 V3493 ASTX029 2095719-92-7 ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50= 2.7 nM).
AX15836 V11971 AX15836 2035509-96-5 AX-15836 is a potent and specific ERK5 inhibitor (antagonist) with IC50 of 8 nM.
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