SB-216763 A potent, selective and ATP-competitive inhibitor of GSK-3α and GSK-3β

SB-216763 (CAS 280744-09-4)

SB-216763 | CAS 280744-09-4 is rated 5.0 out of 5 by 1.
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Synonym: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Application: A potent, selective and ATP-competitive inhibitor of GSK-3α and GSK-3β
CAS Number: 280744-09-4
Purity: ≥98%
Molecular Weight: 371.22
Molecular Formula: C19H12Cl2N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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SB 216763 is a cell-permeable, potent, selective and ATP-competitive inhibitor of GSK-3 (Glycogen Synthase Kinase) with an IC50 value of 34 nM for GSK-3α and with similar potency for GSK-3β. In PC-12 cells, SB-216763 exhibits neuroprotective properties and protects cultured central and peripheral nervous system neurones from cell death. Furthermore, SB-216763 increases the concentration of cytoplasmic β-catenin through a GSK-3 dependent manner. These inhibitory effects are similar to those of Wnt.


References

1. Lochhead, P.A., et al. 2001. Diabetes. 50: 937-946. PMID: 11334436
2. Culbert, A.A., et al. 2001. FEBS Lett. 507: 288-294. PMID: 11696357
3. Cross, D.A., et al. 2001. J. Neurochem. 77: 94-102. PMID: 11279265
4. Schmöle, A.C., et al. 2010. Bioorg. Med. Chem. 18: 6785-6795. PMID: 20708937

Physical State :
Solid
Solubility :
Soluble in DMSO (>25 mg/ml), ethanol (1 mM), water (0.3 mg/ml) at 25.0° C, DMF, and 1:2 DMSO:PBS (pH 7.2) (30 µg/ml). Sparingly soluble in aqueous buffers.
Storage :
Store at room temperature
Melting Point :
288-290° C
Boiling Point :
~598.1° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.70
IC50 :
GSK-3β: IC50 = 7 nM (human); GSK-3α: IC50 = 34 nM (human); Cyclin A2: IC50 = 269 nM (human); Cyclin-dependent kinase 2: IC50 = 269 nM (human); Cyclin A1: IC50 = 269 nM (human)
Ki Data :
GSK-3α: Ki= 9 nM
pK Values :
pKa: 7.27
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
UX9565000
PubChem CID :
176158
MDL Number :
MFCD09753369
SMILES :
CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl

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Certificate of Analysis

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SB-216763  Product Citations

See how others have used SB-216763. Click on the entry to view the PubMed entry .

Citations 1 to 10 of 14 total

PMID: # 28207787  Ouyang, X. et al. 2017. PLoS ONE. 12: e0171898.

PMID: # 27619995  Wu, Y. et al. 2016. J. Immunol.

PMID: # 26445356  2015. Biochem. Pharmacol. 98: 511-21.

PMID: # 26381174  So, KY. et al. 2015. Biochem. Biophys. Res. Commun. 466: 541-6.

PMID: # 25354204  2015. Int. J. Cancer. 136: 2304-15.

PMID: # 25273023  2015. Arch. Toxicol. 89: 1271-84.

PMID: # 25437872  2014. Cell Reprogram. 16: 456-66.

PMID: # 23897984  2013. Toxicol. Sci. 135: 380-9.

PMID: # 22482760  2012. J. Surg. Res. 178: 96-104.

PMID: # 22310719  2012. Biochem. Biophys. Res. Commun. 418: 759-64.

Citations 1 to 10 of 14 total
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Rated 5 out of 5 by from Bentley et al Bentley et al. (PubMed ID 19011050) used SB-216763, a competitive inhibitor of GSK-3 , to decrease iGSK-3 phosphorylation while also increasing levels of pGSK and NFATc3 in both the cytoplasm and cell nucleus. -SCBT Publication Review
Date published: 2015-02-16
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