ERK Inhibitor Chemical Properties

storage temp. 

+2C to +8C

solubility 

DMSO: 2 mg/ml

form 

Light yellow solid

ERK Inhibitor Usage And Synthesis

Description

ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (K_D = 5 μM). This prevents its interaction with protein substrates without inhibiting catalytic activity. 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. 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.

General Description

A cell-permeable and reversible thiazolidinedione compound that displays anti-proliferative properties (IC₅₀ ≤ 25 μM in HeLa, A549, and SUM-159 tumor cells). Preferentially binds to ERK2 with a K_D of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1 in HeLa cells, while exhibiting little effect on ERK1/2 phosphorylation by MEK1/2.

Biochem/physiol Actions

Primary TargetERK

ERK Inhibitor(1049738-54-6)Related Product Information

• N-[4-[5-(1,3-BENZODIOXOL-5-YL)-3-METHOXY-1H-1,2,4-TRIAZOL-1-YL]PHENYL]-2-(PHENYLTHIO)ACETAMIDE
• 2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
• Chk2 Inhibitor
• Trolox
• NSC 23766 TETRAHYDROCHLORIDE
• NSC697923
• MIF Antagonist, ISO-1
• GSK-3β Inhibitor XVIII
• Pictilisib
• JNJ-10198409
• Motesanib
• C2 CERAMIDE
• PD 173074
• Compound 28
• Glycogen Phosphorylase Inhibitor
• Compound 23
• MMP-9 INHIBITOR I
• 6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMAN-2-CARBOXYLIC ACID