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CHIR-98014

Catalog No. T2608   CAS 252935-94-7
Synonyms: Glycogen synthase kinase-3, CHIR98014, CHIR 98014, GSK-3, CHIR-98014, Inhibitor, CT98014, inhibit, Glycogen synthase kinase 3

CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.

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CHIR-98014, CAS 252935-94-7
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Purity: 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
Targets&IC50 GSK-3α:0.65 nM, GSK-3β:0.58 nM
Kinase Assay Kinase assays: Polypropylene 96-well plates are ?lled with 300 μL/well buffer (50 mM tris HCl, 10 mM MgCl2, 1 mM EGTA, 1 mM dithiothreitol, 25 mM β-glycerophosphate, 1 mM NaF, 0.01% BSA, pH 7.5) containing kinase, peptide substrate, and any activators. CHIR-98014 or controls are added in 3.5 μL of DMSO, followed by 50 μL of ATP stock to yield a ?nal concentration of 1 μM ATP in all cell-free assays. After incubation, triplicate 100-μL aliquots are transferred to Combiplate eight plates containing 100 μL/well 50 μM ATP and 20 mM EDTA. After 1 hour, the wells are rinsed ?ve times with PBS, ?lled with 200 μL of scintillation ?uid, sealed, left 30 min, and counted in a scintillation counter. All steps are performed at room temperature.
Cell Research CHO-IR cells expressing human insulin receptor are grown to 80% con?uence in Hamm’s F12 medium with 10% fetal bovine serum and without hypoxanthine. Trypsinized cells are seeded in 6-well plates at 1 × 106 cells/well in 2 mL of medium without fetal bovine serum. After 24 hours, medium is replaced with 1 mL of serum-free medium containing GSK-3 inhibitor CHIR 98014 or control (?nal DMSO concentration 0.1%) for 30 min at 37 °C. Cells are lysed by freeze/thaw in 50 mM tris (pH 7.8) containing 1 mM EDTA, 1 mM DTT, 100 mM NaF, 1 mM phenylmethylsulfonyl ?uoride, and 25 μg/mL leupeptin (buffer A) and centrifuged 15 min at 4 °C/14000 g. The activity ratio of GS is calculated as the GS activity in the absence of glucose-6-phosphate divided by the activity in the presence of 5 mM glucose-6-phosphate. (Only for Reference)
Synonyms Glycogen synthase kinase-3, CHIR98014, CHIR 98014, GSK-3, CHIR-98014, Inhibitor, CT98014, inhibit, Glycogen synthase kinase 3
Molecular Weight 486.32
Formula C20H17Cl2N9O2
CAS No. 252935-94-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: <1 mg/mL

H2O: <1 mg/mL

DMSO: 8 mg/mL (16.45 mM), warmed

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Ring DB,et al. Diabetes. 2003, 52(3), 588-595. 2. Selenica ML, et al. Br J Pharmacol. 2007, 152(6), 959-979.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Anti-Lung Cancer Compound Library HIF-1 Signaling Pathway Compound Library Cancer Cell Differentiation Compound Library Glycometabolism Compound Library Anti-Cancer Metabolism Compound Library Anti-Obesity Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Wnt/Hedgehog/Notch Compound Library

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