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ERK

ERK

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.

ERK related products

Structure Cat No. Product Name CAS No. Product Description
MK-8353 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.
MK-8353 hydrochloride 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.
mSIRK (G-Protein βγ Binding Peptide) 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.
mSIRK TFA V87065 mSIRK TFA mSIRK TFA (G-Protein βγ Binding Peptide) is a cell-permeable ERK1/2 activator with EC50 of 2.5-5 μM.
Myristoyl-MEK1 Derived Peptide Inhibitor 1 V80864 Myristoyl-MEK1 Derived Peptide Inhibitor 1 Myristoyl-MEK1 Derived Peptide Inhibitor 1 is the myristoylated form of MEK1 Derived Peptide Inhibitor 1.
Napyradiomycin B4 V87066 Napyradiomycin B4 Napyradiomycin B4 is a napyradiomycin derivative that inhibits RANKL-induced MEK-ERK signaling pathway.
Pamoic acid disodium (disodium pamoate; disodium acetylate; disodium pamoic acid salt) 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.
PKCδ substrate V88085 PKCδ substrate 915155-20-3 PKCδ substrate serves as a nuclear transport protein of ERK2 and participates in ERK2-mediated gene activation.
POP-3MB V69822 POP-3MB 1144114-27-1 POP-3MB (compound 1b) is an isoprenylcysteine carboxyl methyltransferase (ICMT) inhibitor (IC50= 2.5 μM).
Prolylserine V69811 Prolylserine 71835-80-8 Prolylserine is a dipeptide that is an inhibitor (blocker/antagonist) of melanin production in Mel-Ab cells.
Rineterkib (LTT-462; ERK-IN-1) 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.
Rineterkib盐酸盐 V51449 Rineterkib hydrochloride 1715025-34-5 ERK1/2 inhibitor
SCH772984 V0463 SCH772984 942183-80-4 SCH772984 (SCH-772984) is a novel, potent and ATP-competitive inhibitor of ERK1/2 with potential antitumor activity.
Serum thymic factor acetate V89649 Serum thymic factor acetate 125117-65-9 Serum thymic factor acetate (Thymulin acetate) is the acetate form of Serum thymic factor.
SHP2-IN-23 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.
SHR2415 V69831 SHR2415 2494010-42-1 SHR2415 is a potent and specific ERK1/2 inhibitor (antagonist) with oral activity.
SOS1 activator 2 V104207 SOS1 activator 2 2245237-54-9 SOS1 activator 2 (compound 65) is a benzimidazole derivative and an activator of SOS1.
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide) 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).
TAT-MEK1 V69812 TAT-MEK1 566872-16-0 TAT-MEK1 is an inhibitor (blocker/antagonist) of ERK2, consisting of TAT and MEK1 (N-terminal).
Temuterkib (LY3214996) 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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