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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
Endothelin-1 (1-31) (Human) TFA V77039 Endothelin-1 (1-31) (Human) TFA Endothelin-1 (1-31) (Human) TFA is a potent vasoconstrictor and blood pressure increase.
ERK-IN-2 V69835 ERK-IN-2 2743576-56-7 ERK-IN-2 is an ERK2 inhibitor (antagonist) with IC50 of 1.8 nM.
ERK-IN-2 free base 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.
ERK-IN-4 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.
ERK-IN-7 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.
ERK-IN-8 V88086 ERK-IN-8 2226293-75-8 ERK-IN-8 (compound I-1) is an aniline pyrimidine derivative that acts as an ERK inhibitor.
ERK1/2 inhibitor 10 V89609 ERK1/2 inhibitor 10 ERK1/2 inhibitor 10 (Compound 36c) is a potent inhibitor of ERK1 and ERK2 (IC50 of 0.11/0.08 nM, respectively).
ERK1/2 inhibitor 3 V69806 ERK1/2 inhibitor 3 2737294-99-2 ERK1/2 inhibitor 3 is a potent ERK1/2 inhibitor.
ERK1/2 inhibitor 4 V69820 ERK1/2 inhibitor 4 2490396-99-9 ERK1/2 inhibitor 5 is a potent ERK1/2 inhibitor.
ERK1/2 inhibitor 6 V69810 ERK1/2 inhibitor 6 2634816-13-8 ERK1/2 inhibitor 6 is a potent ERK1/2 inhibitor.
ERK1/2 inhibitor 9 V69826 ERK1/2 inhibitor 9 2169302-75-2 ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor.
ERK2 allosteric-IN-1 V89775 ERK2 allosteric-IN-1 872591-16-7 ERK2 allosteric-IN-1 (compound 1) is a selective allosteric ERK2 inhibitor with IC50 of 11 μM.
ERK2 IN-5 V105113 ERK2 IN-5 353250-09-6 ERK2 IN-5 (compound 5g) is an inhibitor of ERK2 and exhibits good affinity for ERK2 and JNK3 with Ki of 86 and 550 nM, respectively.
ERK2-IN-4 V87069 ERK2-IN-4 933786-58-4 ERK2-IN-4 (Compound 6o) is a potent and selective ERK2 inhibitor with a Ki of 0.006 μM for ERK2.
ERK5-IN-2 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.
ERK5-IN-5 V69837 ERK5-IN-5 2318792-30-0 ERK5-IN-5 (compound 4a) is an ERK5 kinase inhibitor (antagonist) with anti-cancer activity.
ERK5-IN-6 V69805 ERK5-IN-6 2734916-64-2 ERK5-IN-6 (compound 5J) is an ERK5 kinase inhibitor (antagonist) with anti-cancer activity.
ERKtide V69815 ERKtide 287721-17-9 ERKtide is a biologically active peptide.
ETP-45835 dihydrochloride V102550 ETP-45835 dihydrochloride 2136571-30-5 D-106669 is an inhibitor of Erk2 with IC50 of 18.7 μM.
FR 180204 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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