A cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 µM); blocks ERK-specific phosphorylation of Rsk-1 and TCF/Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2; completely prevents proliferation of several cancer cell lines

ERK Inhibitor – 5 mg

Brand:
Cayman
CAS:
1049738-54-6
Storage:
-20
UN-No:
Non-Hazardous - /

ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 µM).{25905} This prevents its interaction with protein substrates without inhibiting catalytic activity.{25905} ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2.{25905} Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC50 = 15-20 µM), A549 lung carcinoma cells (IC50 = 25 µM), Sum-159 estrogen receptor-negative breast cancer cells and HT1080 fibrosarcoma cells.{25905}  

 

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Description

A cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 µM); blocks ERK-specific phosphorylation of Rsk-1 and TCF/Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2; completely prevents proliferation of several cancer cell lines

Formal name: 3-(2-aminoethyl)-5-[(4-ethoxyphenyl)methylene]-2,4-thiazolidinedione, monohydrochloride

Synonyms:  Extracellular Regulated Kinase Inhibitor

Molecular weight: 328.8

CAS: 1049738-54-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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