For research use only. Not for therapeutic Use.
SB 216763（Cat No.:I002954）is a selective inhibitor of glycogen synthase kinase-3 (GSK-3), targeting both GSK-3α and GSK-3β isoforms. By inhibiting GSK-3, SB 216763 modulates various signaling pathways, including the Wnt/β-catenin pathway, which is crucial for cell proliferation, differentiation, and survival. This compound is widely used in research for its neuroprotective properties and potential therapeutic applications in neurodegenerative diseases such as Alzheimer’s and Parkinson’s. Additionally, SB 216763 has shown promise in cancer research and diabetes management by promoting cell survival and regulating glucose metabolism, making it a valuable tool in diverse biological studies.
| Catalog Number | I002954 |
| CAS Number | 280744-09-4 |
| Synonyms | 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione |
| Molecular Formula | C₁₉H₁₂Cl₂N₂O₂ |
| Purity | ≥95% |
| Target | Stem Cell/Wnt |
| 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 |
| Reference | </br>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 </br>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 Article</br>3:[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 </br>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 Article</br>5: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 </br>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 Article</br>7: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 |
