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 |
|---|---|---|---|---|
|
V69836 | ERK-IN-2 free base | 2743576-55-6 | ERK-IN-2 free base is an ERK2 inhibitor (antagonist) with IC50 of 1.8 nM. |
|
V69834 | ERK-IN-4 | 1049738-54-6 | ERK-IN-4 is an ERK inhibitor that preferentially binds to ERK2 with a Kd of 5 μM. |
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V69832 | ERK-IN-7 | 2494010-63-6 | RK-IN-7 (Example 10) is an analog of SHR2415 and a potent ERK inhibitor (antagonist) with IC50s of 5 nM and 7 nM for ERK1 and ERK2, respectively. |
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V69806 | ERK1/2 inhibitor 3 | 2737294-99-2 | ERK1/2 inhibitor 3 is a potent ERK1/2 inhibitor. |
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V69820 | ERK1/2 inhibitor 4 | 2490396-99-9 | ERK1/2 inhibitor 5 is a potent ERK1/2 inhibitor. |
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V69810 | ERK1/2 inhibitor 6 | 2634816-13-8 | ERK1/2 inhibitor 6 is a potent ERK1/2 inhibitor. |
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V69826 | ERK1/2 inhibitor 9 | 2169302-75-2 | ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. |
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V4799 | ERK5-IN-2 | 1888305-96-1 | ERK5-IN-2 is a novel, potent, orally bioavailable, sub-micromolar, and selective ERK5 inhibitor with selectivity over p38α and BRD4. |
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V69837 | ERK5-IN-5 | 2318792-30-0 | ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor (antagonist) with anti-cancer activity. |
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V69805 | ERK5-IN-6 | 2734916-64-2 | ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor (antagonist) with anti-cancer activity. |
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V69815 | ERKtide | 287721-17-9 | ERKtide is a biologically active peptide. |
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V0465 | FR 180204 | 865362-74-9 | FR-180204 (FR180204) is a novel, potent, selectiveand ATP-competitive inhibitor of ERK (extracellular signal-regulated kinase) with potential anti-inflammatory activity and has the potential to be used as a new therapy for rheumatoid arthritis. |
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V52068 | Gardenin A (Gardenia (yellow) element A) | 21187-73-5 | Gardenin A is an orally bioavailable, synthetic PMF analog with neurotrophic effects on neurite outgrowth and neuronal differentiation. |
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V69818 | Glycinexylidide (GX) | 18865-38-8 | Glycinexylidide (GX) is the bioactive metabolite of Lidocaine. |
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V69105 | HA-1004 | 91742-10-8 | HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. |
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V8622 | Hypaphorine | 487-58-1 | Hypaphorine is a naturally occurring indole alkaloid found in Caragana korshinskii and has neurological effects and hypoglycemic effects on rodents. |
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V69819 | ikB | 593267-11-9 | mSIRK (G-Protein βγ Binding Peptide) is a cell-permeable (penetrable) activator of ERK1/2 with EC50 of 2.5-5 μM. |
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V40505 | JWG-071 | 2250323-50-1 | JWG-071 is the first reported chemical probe selective for ERK5 kinase. |
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V4753 | KO-947 | 1695533-89-1 | KO-947 is a novel, potent and selective inhibitor of ERK1/2 kinases with potential usefulness in MAPK pathway dysregulated tumors. |
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V74708 | KRAS G12C inhibitor 61 | 2300967-40-0 | KRAS G12C inhibitor 61 (Example 3) inhibits ERK 1/2 phosphorylation in MIA PaCa-2 cells with IC50 of 9 nM. |
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