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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V120232 | (R)-MK-8353 | 2748457-30-7 | (R)-MK-8353 ((R)-SCH900353) is the R-enantiomer of MK-8353. |
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V69825 | (R)-VX-11e | 1680187-43-2 | (R)-VX-11e (Compound 1) is an ERK2 inhibitor. |
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V69801 | (S)-BAY 2965501 | 2732902-09-7 | (S)-BAY 2965501 is the left-handed isomer of BAY 2965501. |
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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. |
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V69817 | 7α,15-Dihydroxydehydroabietic acid | 155205-64-4 | 7α,15-Dihydroxydehydroabietic acid is a natural abietane diterpenoid with anti-angiogenic effects. |
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V115625 | AB19 | AB19 is a potent Vav1 inhibitor. | |
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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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V86914 | Ambuic acid | 340774-69-8 | Ambuic acid has antibacterial activity against Staphylococcus aureus ATCC 6538 strain with an IC50 of 43.9 μM. |
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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. |
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V117507 | APS03118 | 2598870-24-5 | APS03118 is an orally effective, potent, and highly selective transfection rearrangement (RET) inhibitor. |
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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. |
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V3493 | ASTX029 | 2095719-92-7 | ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50= 2.7 nM). |
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V11971 | AX15836 | 2035509-96-5 | AX-15836 is a potent and specific ERK5 inhibitor (antagonist) with IC50 of 8 nM. |
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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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V119007 | Biotin-ERK2 Recombinant Human Active Protein Kinase | ERK2 is a serine/threonine-specific protein kinase that can phosphorylate a variety of intracellular protein substrates. | |
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V116066 | BTX-6654 formate | BTX-6654 formate is a highly targeted and specific bifunctional SOS1 protein-encoded degrader based on CRBN. | |
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V116433 | C3 sodium | Sodium C3 is a nucleic acid aptamer that can bind to Erk2. |