SB 216763

SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

Product Specifications

CAS Number

[280744-09-4]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Autophagy; GSK-3

Type

Reference compound

Related Pathways

Autophagy; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/SB-216763.html

Concentration

10mM

Purity

99.37

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL

Smiles

O=C(NC1=O)C(C2=CC=C(C=C2Cl)Cl)=C1C3=CN(C4=C3C=CC=C4)C

Molecular Formula

C19H12Cl2N2O2

Molecular Weight

371.22

Precautions

H315, H319, H335

References & Citations

[1]Gurrieri, et al. 3- (2,4-dichlorophenyl) -4- (1-methyl-1H-indol-3-yl) -1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther.2010|[2]Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.PLoS One. 2012;7 (6) :e39329. Epub 2012 Jun 26.|[3]Wang M, et al. The first synthesis of [ (11) C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3) .Bioorg Med Chem Lett. 2011 Jan 1;21 (1) :245-9. Epub 2010 Nov 11.|[4]The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3- (2,4-dichlorophenyl) -4 (1-methyl-1H-indol-3-yl) -1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening.|[5]Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7 (10) :793-803.|[6]Wang W, et al. Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.