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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V4122 | MK-8353 | 1184173-73-6 | MK-8353 (also known as SCH900353; SCH-900353) is a novel, potent, selective and orally bioavailable ERK inhibitor with anticancer activity. |
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V116036 | MK-8353 hydrochloride | 1951448-73-9 | MK-8353 (SCH900353) hydrochloride is a potent, selective, orally effective ERK1/2 inhibitor with IC50 values of 23.0 nM and 8.8 nM, respectively. |
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V69819 | mSIRK (G-Protein βγ Binding Peptide) | 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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V87065 | mSIRK TFA | mSIRK TFA (G-Protein βγ Binding Peptide) is a cell-permeable ERK1/2 activator with EC50 of 2.5-5 μM. | |
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V80864 | Myristoyl-MEK1 Derived Peptide Inhibitor 1 | Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of MEK1 Derived Peptide Inhibitor 1. | |
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V87066 | Napyradiomycin B4 | Napyradiomycin B4 is a napyradiomycin derivative that inhibits RANKL-induced MEK-ERK signaling pathway. | |
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V69800 | Pamoic acid disodium (disodium pamoate; disodium acetylate; disodium pamoic acid salt) | 6640-22-8 | Pamoic acid disodium is a potent GPR35 agonist/activator with EC50 of 79 nM. |
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V88085 | PKCδ substrate | 915155-20-3 | PKCδ substrate serves as a nuclear transport protein of ERK2 and participates in ERK2-mediated gene activation. |
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V69822 | POP-3MB | 1144114-27-1 | POP-3MB (compound 1b) is an isoprenylcysteine carboxyl methyltransferase (ICMT) inhibitor (IC50= 2.5 μM). |
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V69811 | Prolylserine | 71835-80-8 | Prolylserine is a dipeptide that is an inhibitor (blocker/antagonist) of melanin production in Mel-Ab cells. |
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V4794 | Rineterkib (LTT-462; ERK-IN-1) | 1715025-32-3 | Rineterkib (LTT-462; ERK-IN-1; ERK-IN1), the compound B extracted from WO2018051306A1, is a novel and potent RAF and ERK1/2 inhibitor with anticancer activity. |
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V51449 | Rineterkib hydrochloride | 1715025-34-5 | ERK1/2 inhibitor |
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V0463 | SCH772984 | 942183-80-4 | SCH772984 (SCH-772984) is a novel, potent and ATP-competitive inhibitor of ERK1/2 with potential antitumor activity. |
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V89649 | Serum thymic factor acetate | 125117-65-9 | Serum thymic factor acetate (Thymulin acetate) is the acetate form of Serum thymic factor. |
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V69743 | SHP2-IN-23 | 2415989-91-0 | SHP2-IN-23 (compound 30) is an orally bioactive SHP2 inhibitor (IC50=38 nM) with excellent in vivo activity and pharmacokinetic characteristics. |
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V69831 | SHR2415 | 2494010-42-1 | SHR2415 is a potent and specific ERK1/2 inhibitor (antagonist) with oral activity. |
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V104207 | SOS1 activator 2 | 2245237-54-9 | SOS1 activator 2 (compound 65) is a benzimidazole derivative and an activator of SOS1. |
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V69824 | STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide) | 566872-15-9 | STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH2) is a cell-penetrating/penetrable ERK1/2 inhibitor (IC50= 13-30μM). |
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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. |