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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V69812 | TAT-MEK1 | 566872-16-0 | TAT-MEK1 is an inhibitor (blocker/antagonist) of ERK2, consisting of TAT and MEK1 (N-terminal). |
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V3178 | Temuterkib (LY3214996) | 1951483-29-6 | Temuterkib (formerly LY3214996; LY-3214996) is a selective, ATP-competitive and orally bioavailable inhibitor of the ERK1 (extracellular signal-regulated kinase) and ERK2 with potential anticancer activity. It inhibits ERK1/2 with IC50 value of 5 nM in biochemical assays. |
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V3642 | Trametinib DMSO solvate | 1187431-43-1 | Trametinib DMSO solvate is the solvated form of trametinib (trametinib: dimethyl sulfoxide=1:1) and a potent MEK inhibitor that specifically inhibits MEK1/2 with an IC50 value of about 2 nM. |
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V0470 | Ulixertinib (BVD-523; VRT752271) | 869886-67-9 | Ulixertinib (formerly also known as BVD-523 and VRT752271) is a novel,potent, orally bioactive, highly selective, ATP-competitive and reversible ERK1/ERK2 inhibitor with potential antineoplastic activity. |
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V27837 | Ulixertinib HCl | 1956366-10-1 | Ulixertinib (formerly also known as BVD-523 and VRT752271) is a novel,potent, orally bioactive, highly selective, ATP-competitive and reversible ERK1/ERK2 inhibitor with IC50 of<0.3 nM for ERK2. |
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V0468 | VX-11e | 896720-20-0 | VX-11e is a novel, potent, selective, and orally bioavailable ERK2 (extracellular signal-related kinase 2) inhibitor with potential anticancer activity. |
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V50989 | WAY-357997 | 39582-96-2 | ERK1/2 inhibitor |
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V0467 | XMD17-109 | 1435488-37-1 | XMD17-109, a pyrimido-diazepinone analog, is a novel, potent, specific,cell-permeable and ATP-competitive inhibitor of ERK-5 with important biological activity. |
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V20691 | XMD8-85 | 1234479-76-5 | ERK5-IN-1 is a potent ERK5 inhibitor (antagonist) with IC50 of 87±7 nM. |
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V0464 | XMD8-92 | 1234480-50-2 | XMD8-92 (XMD-8-92) is a novel, potent and highly selective dual inhibitor of BMK1/ERK5 (big mitogen activated protein kinase 1 / extracellular-signal-regulated kinase) with potential antineoplastic activity. |
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