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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V69825 | (R)-VX-11e | 1680187-43-2 | (R)-VX-11e (Compound 1) is an ERK2 inhibitor. |
|
V69801 | (S)-BAY 2965501 | 2732902-09-7 | (S)-BAY 2965501 is the left-handed isomer of BAY 2965501. |
|
V69817 | 7α,15-Dihydroxydehydroabietic acid | 155205-64-4 | 7α,15-Dihydroxydehydroabietic acid is a natural abietane diterpenoid with anti-angiogenic effects. |
|
V9020 | Adjudin | 252025-52-8 | Adjudin, formerly known as AF-2364, is a drug which is under development as a potential non-hormonal male contraceptive drug, which acts by blocking the production of sperm in the testes, but without affecting testosterone production. |
|
V69823 | ADTL-EI1712 | 2414916-45-1 | ADTL-EI1712 is an orally bioactive selective dual-target inhibitor of ERK1 and ERK5. |
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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. |
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V10837 | Alobresib | 1637771-14-2 | Alobresib (GS-5829) is a novel and potent BET bromodomain inhibitor with anticancer activity. |
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V51049 | ASN-007 benzenesulfonate | 2055597-39-0 | ERK1/2 inhibitor |
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V41199 | ASN007 | 2055597-12-9 | ASN007 (ASN-007) is a novel, potent, orally bioavailable and selective inhibitor of ERK1/2 with robust antitumor activity. |
|
V7184 | Astragaloside IV | 84687-43-4 | Astragaloside IV (AS-IV), the major active component found in Astragalus membranaceus, has broad application prospects, especially in cardiovascular diseases, digestive diseases, cancer and other modern high incidence, high-risk diseases, and could be developed as a medicine. |
|
V3493 | ASTX029 | 2095719-92-7 | ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50= 2.7 nM). |
|
V11971 | AX15836 | 2035509-96-5 | AX-15836 is a potent and specific ERK5 inhibitor (antagonist) with IC50 of 8 nM. |
|
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. |
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V4176 | BAY885 | 2307249-33-6 | BAY-885 is a novel, highly potent and selective ERK5/MAPK7 inhibitor with IC50 of 40 nM. |
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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. |
|
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. |
|
V69804 | Edaxeterkib | 1695534-88-3 | Edaxeterkib is a potent ERK kinase inhibitor used in cancer-related research. |
|
V79303 | Endothelin-1 (1-31) (Human) acetate | Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and blood pressure increase. | |
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V77039 | Endothelin-1 (1-31) (Human) TFA | Endothelin-1 (1-31) (Human) TFA is a potent vasoconstrictor and blood pressure increase. | |
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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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