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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
(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.
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.
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.
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.
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.
AZD-0364 V3801 AZD-0364 2097416-76-5 AZD0364 is a potent and selective oral inhibitor of ERK1/2 that is efficacious in both monotherapy and combination therapy in models of NSCLC.
BAY885 V4176 BAY885 2307249-33-6 BAY-885 is a novel, highly potent and selective ERK5/MAPK7 inhibitor with IC50 of 40 nM.
CC-90003 V4221 CC-90003 1621999-82-3 CC-90003 is a novel, potent, selective, orally bioavailable, and irreversible (covalent) inhibitor of ERK1/2 (extracellular signal-regulated kinase) with IC50s in the 10-20 nM range, and displays good kinase selectivity in a 258-kinase biochemical assay.
DEL-22379 V0469 DEL-22379 181223-80-3 DEL-22379 is a novel, potent,selective, and water-soluble ERK (extracellular signal-related kinase 2) dimerization inhibitor with potential antitumor activity.
Edaxeterkib V69804 Edaxeterkib 1695534-88-3 Edaxeterkib is a potent ERK kinase inhibitor used in cancer-related research.
Endothelin-1 (1-31) (Human) acetate V79303 Endothelin-1 (1-31) (Human) acetate Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and blood pressure increase.
Endothelin-1 (1-31) (Human) TFA V77039 Endothelin-1 (1-31) (Human) TFA Endothelin-1 (1-31) (Human) TFA is a potent vasoconstrictor and blood pressure increase.
ERK-IN-2 V69835 ERK-IN-2 2743576-56-7 ERK-IN-2 is an ERK2 inhibitor (antagonist) with IC50 of 1.8 nM.
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