MilliporeSigma™ Calbiochem™ ERK Inhibitor VIII

Catalog No.	Quantity
32-801-110MG	10 mg

Catalog No. 32-801-110MG Supplier MilliporeSigma™ Supplier No. 32801110MG

Description

A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor ( K _I <2nM against Erk2; [ATP] = 65μM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations ( K _I = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases ( K

A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor ( K _I <2nM against Erk2; [ATP] = 65μM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations ( K _I = 395, 540, and 852 nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases ( K _I ≥1.4μM; IC₅₀ ≥1μM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC₅₀ = 48nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100nM WZ4002 with or without 1μM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo .

Specifications

• Color: Yellowish-white
• Description: 98% by Chiral HPLC
• Target Proteins: ERK
• Molecular Formula: C₂₄H₂₀Cl₂FN₅O₂
• Formula Weight: 500.4g/mol
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 10 mg