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531167 GSK-3 Inhibitor XXIX, CHIR98014 - CAS 252935-94-7 - Calbiochem

A cell-permeable, highly potent, ATP-competitive, reversible inhibitor of both GSK-3α and β (IC₅₀ = 650 and 580 pM, respectively).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N²-(2-(4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine, N⁶-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl)amino}ethyl)-3-nitro-2,6-pyridinediamine, CHIR-98014, CT-98014

Primary Target: GSK-3 α & β
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Overview

Key Spec Table

CAS #Empirical Formula
252935-94-7C₂₀H₁₇Cl₂N₉O₂

Products

Catalogue NumberPackaging Qty/Pack
5.31167.0001 Glass bottle 5 mg
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Description
OverviewA cell-permeable, brain permeant aminopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of both GSK-3α and β (IC50 = 650 and 580 pM, respectively; Ki = 870 pM for human GSK-3β) and significantly affects downstream effects of GSK-3. Displays excellent selectivity over closely related Cdc2 and Erk2 (IC50 = 3.7 µM & > 10 µM, respectively). Does not affect the activity of several other protein kinases studied. Acutely sensitizes glycogen synthase activity in isolated skeletal muscle from insulin-sensitive lean Zucker and insulin-resistant Zucker diabetic fatty (ZDF) rats and can also augment insulin-stimulated glucose uptake in ZDF rats. However, it does not affect the basal glucose uptake rate. Induces a significant reduction in fasting hyperglycemia in diabetic and insulin-resistant db/db mice (~30 mg/kg, s.c.). Reduces Tau phosphorylation (Ser396) in the cortex and hippocampus of postnatal rats. Also shown to activate Wnt/β-catenin signaling and direct the differentiation of human pluripotent stem cells into cardiomyocytes.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number531167
Brand Family Calbiochem®
SynonymsN²-(2-(4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine, N⁶-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl)amino}ethyl)-3-nitro-2,6-pyridinediamine, CHIR-98014, CT-98014
References
ReferencesGrigoryan, T., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 18174.
Lian, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, E1848.
Selenica, M.L., et al. 2007. Br. J. Pharmacol. 152, 959.
Ring, D.B., et al. 2003. Diabetes. 52, 588.
Nikoulina, S.E., et al. 2002. Diabetes. 51, 2190.
Product Information
CAS number252935-94-7
FormYellow powder
Hill FormulaC₂₀H₁₇Cl₂N₉O₂
Chemical formulaC₂₀H₁₇Cl₂N₉O₂
ReversibleY
Quality LevelMQ100
Biological Information
Primary TargetGSK-3 α & β
Primary Target IC<sub>50</sub>650 and 580 pM for GSK-3&alpha
Primary Target K<sub>i</sub>870 pM for human GSK-3&beta
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
5.31167.0001 04055977283150