SB 216763

• CAT Number: I002954
• CAS Number: 280744-09-4
• Molecular Formula: C₁₉H₁₂Cl₂N₂O₂
• Molecular Weight: 371.22
• Purity: ≥95%
• Target: GSK-3
• Solubility: DMSO ≥25mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: 3 years -20℃ powder
• IC50: 9 nM (Ki)
• IUPAC Name: 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione
• InChI: InChI=1S/C19H12Cl2N2O2/c1-23-9-13(11-4-2-3-5-15(11)23)17-16(18(24)22-19(17)25)12-7-6-10(20)8-14(12)21/h2-9H,1H3,(H,22,24,25)
• InChIKey: JCSGFHVFHSKIJH-UHFFFAOYSA-N
• SMILES: CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl

SB 216763 (Cat.No:I002954) is a specific and potent inhibitor of glycogen synthase kinase-3 (GSK-3). GSK-3 is a key enzyme involved in various cellular processes, including glycogen metabolism and cell signaling pathways. SB 216763 has been widely used in research to study GSK-3-related mechanisms and potential therapeutic applications in various diseases, including cancer and neurodegenerative disorders.

Reference

1:Inhibition of glycogen synthase kinase-3 by SB 216763 affects acquisition at lower doses than expression of amphetamine-conditioned place preference in rats. Wickens RH, Quartarone SE, Beninger RJ.Behav Pharmacol. 2017 Jun;28(4):262-271. doi: 10.1097/FBP.0000000000000283. PMID: 27984209 2:Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3. Li L, Shao X, Cole EL, Ohnmacht SA, Ferrari V, Hong YT, Williamson DJ, Fryer TD, Quesada CA, Sherman P, Riss PJ, Scott PJ, Aigbirhio FI.ACS Med Chem Lett. 2015 Mar 10;6(5):548-52. doi: 10.1021/acsmedchemlett.5b00044. eCollection 2015 May 14. PMID: 26005531 Free PMC Article3:[Effects of glycogen synthase kinase 3β overexpression in rat and glycogen synthase kinase 3β inhibitor SB-216763 on proliferation of hepatic oval cells]. Zhong JQ, Xie YK, Ji XK, Fu JH, Wang Y, Zhang QY, Shi HQ, Shan YF.Zhonghua Wai Ke Za Zhi. 2012 Nov;50(11):1003-6. Chinese. PMID: 23302485 4:Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. Kirby LA, Schott JT, Noble BL, Mendez DC, Caseley PS, Peterson SC, Routledge TJ, Patel NV.PLoS One. 2012;7(6):e39329. doi: 10.1371/journal.pone.0039329. Epub 2012 Jun 26. PMID: 22745733 Free PMC Article5:The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3). Wang M, Gao M, Miller KD, Sledge GW, Hutchins GD, Zheng QH.Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. doi: 10.1016/j.bmcl.2010.11.026. Epub 2010 Nov 11. PMID: 21115250 6: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. Couvreur N, Tissier R, Pons S, Chenoune M, Waintraub X, Berdeaux A, Ghaleh B.J Pharmacol Exp Ther. 2009 Jun;329(3):1134-41. doi: 10.1124/jpet.109.152587. Epub 2009 Mar 24. PMID: 19318592 Free Article7:Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion. Gross ER, Hsu AK, Gross GJ.Am J Physiol Heart Circ Physiol. 2008 Mar;294(3):H1497-500. doi: 10.1152/ajpheart.01381.2007. Epub 2008 Jan 25. PMID: 18223186 Free Article