Molecular structure of SB-216763, CAS Number: 280744-09-4
SB-216763 (CAS 280744-09-4)
See product citations (18)
Alternate Names:
3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Application:
SB-216763 is 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
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
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-3alpha and with similar potency for GSK-3beta. 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 beta-catenin through a GSK-3 dependent manner. These inhibitory effects are similar to those of Wnt. It exhibits promising anti-inflammatory properties and acts as an inhibitor of the enzyme cyclooxygenase-2 (COX-2). The compound has proven valuable in studying SB-216763 inhibition′s impact on inflammation, pain, cell proliferation, and apoptosis. Moreover, it has been employed in synthesizing organic compounds and explored for potential use in drug design.
SB-216763 (CAS 280744-09-4) References
- Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death. | Cross, DA., et al. 2001. J Neurochem. 77: 94-102. PMID: 11279265
- Inhibition of GSK-3 selectively reduces glucose-6-phosphatase and phosphatase and phosphoenolypyruvate carboxykinase gene expression. | Lochhead, PA., et al. 2001. Diabetes. 50: 937-46. PMID: 11334436
- GSK-3 inhibition by adenoviral FRAT1 overexpression is neuroprotective and induces Tau dephosphorylation and beta-catenin stabilisation without elevation of glycogen synthase activity. | Culbert, AA., et al. 2001. FEBS Lett. 507: 288-94. PMID: 11696357
- Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion. | Gross, ER., et al. 2008. Am J Physiol Heart Circ Physiol. 294: H1497-500. PMID: 18223186
- 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., et al. 2009. J Pharmacol Exp Ther. 329: 1134-41. PMID: 19318592
- Novel indolylmaleimide acts as GSK-3beta inhibitor in human neural progenitor cells. | Schmöle, AC., et al. 2010. Bioorg Med Chem. 18: 6785-95. PMID: 20708937
- The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3). | Wang, M., et al. 2011. Bioorg Med Chem Lett. 21: 245-9. PMID: 21115250
- Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells. | Kirby, LA., et al. 2012. PLoS One. 7: e39329. PMID: 22745733
- [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., et al. 2012. Zhonghua Wai Ke Za Zhi. 50: 1003-6. PMID: 23302485
- Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3. | Li, L., et al. 2015. ACS Med Chem Lett. 6: 548-52. PMID: 26005531
- 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., et al. 2017. Behav Pharmacol. 28: 262-271. PMID: 27984209
- SB-216763, a GSK-3β inhibitor, protects against aldosterone-induced cardiac, and renal injury by activating autophagy. | Zhang, YD., et al. 2018. J Cell Biochem. 119: 5934-5943. PMID: 29600538
- Inhibition of GSK-3β restores delayed gastric emptying in obesity-induced diabetic female mice. | Sampath, C., et al. 2020. Am J Physiol Gastrointest Liver Physiol. 319: G481-G493. PMID: 32812777
Inhibitor of:
α-internexin, β-Arrestin-2, β-defensin 10, β-defensin 11, β-defensin 13, β-defensin 17, β-Dystrobrevin, ΔN p63, 1700090G07Rik, 2900016B01Rik, 2B28, 3110043O21Rik, 4933403O03Rik, 4933439F11Rik, 9130008F23Rik, Alsin, ANKRD2, ANKRD50, Ape2, ARD1, Ataxin-10, Ataxin-2, Bag-3, BBS3, BC056474, BC060267, BC061212, BC066028, BC068157, BC080695, BC094916, BC100530, BC106175, Bcl-9L, Bex3, BTEB1, C030039L03Rik, C030046E11Rik, C11orf21, C11orf24, C11orf61_BC024479, C230052I12Rik, C230055K05Rik, C230057M02Rik, C330006A16Rik, C330006K01Rik, C3orf43, C3orf72, C6orf183, C8orf59, cadherin-29, cadherin-7, Calponin 1, CC2D2A, CCDC121, CCDC9, CDR2L, claudin-12, Collapsin Response Mediator Protein (CRMP), CUL-4A, Cypt6, D6Mm5e, D830030K20Rik, Daf2, Dapper3, DBX2, Dcpp3, DIP2C, E130120F12Rik, E130311K13Rik, EG194588, EG224763, EG225058, EG229879, EG245440, EG245651, EG270499, EG432502, EG546325, ER81, FAM155A, FAM48B2, FARP1, FBXW26, Fe65, FHL-2, FLJ10489, FNIP2, FOXJ1, GADD 45β, GCK, GCP5, Gliomedin, Gm609, GPB5, GSK-3 alpha, GSKIP, HCNP, ILVBL, INSC, KIAA0280, KLHL10, Laforin, LLGL2, LOC100039995, LOC100041343, LOC643678, LOC729991-MEF2B, MEF-2A, MEF-2D, MIS12, MKS3, MrgA7, Myocyte enhancer factor (MEF2), nArgBP2, NBPF, neuroligin X/Y, Nlk, Olfr611, Olfr614, Olfr615, Olfr616, Olfr617, Olfr618, Olfr653, Olfr981, Olr264, OTTMUSG00000011290, OTTMUSG00000016784, p63, PC-LKC, PCDH20_Pcdh20, PCDHA4, PCDHAC1_Pcdhac1, PCDHB5, PCDHB8, PEBP2αA, Podocin, Prickle4, protein 4.2, PSP, Puratrophin 1, Reelin, Ripply2, S-100A5, SBK2, SCAI, SLITRK1, SMPD5, SP140, Sp4, Sp6, Stannin, Strumpellin, Synip, TAP, TFEB, TMCC3, TRIM3, TTC12, TTC25, ULK2, utrophin, Vmn1r113, Vmn2r105, WDPCP, X11γ, YSK1, ZMAT4, ZNF665, ZNRF1, and ZSWIM6.Activator of:
14-3-3 η, 14-3-3 σ, 1700016H13Rik, 1700022C21Rik, 2700078E11Rik, 4930422G04Rik, 4931431F19Rik, 6330545A04Rik, AA408296, ABCE1, ADAM15, ADAM29, ADP ribosylation factor (ARF), AIDA, AK4, ANKRD11, ANKRD15, ANKRD52, AP1GBP1, ARKL1_Arkadia 2, ARP-1, B9D1, BACE2, BAF170, BBS4, BC061194, Bex5, Bex6, Bhlhb9, BTBD16, C030017K20Rik, C14orf108, C16orf57, C17orf47, C1orf80, C87499, C87977, casein kinase Iγ1, casein kinase Iγ3, CCDC136, Cdc16, Cdc26, CDKL5, CELSR1, CEP97, Chibby, CLEC-16A, Clusterin, Conductin, CSMD1, CstF-77, CTTNBP2NL, cyclin J, Cypt2, Cypt6, Dapper1, Dapper3, DBNDD1, DCAF16, DEC2, Diversin, DIXDC1, Dkk-2, Dkk-3, Doublecortin, DRAM, Dvl-1, Dvl-3, E130309D14Rik, Eapa2, Ear7, EAT-2B, EBV LMP-1, EG245174, EG382275, EG625480, FAM154A, FAM21A, FAM65A, FBXO10, FBXO47, Fbxw12, Fbxw21, FGF-18, FKHRL1, Freud-1, frizzled-1, frizzled-6, frizzled-7, frizzled-8, fzr, GABARAPL2, GITRL, GKAP1, GKLF, GLCCI1, GLUD2, glycogen synthase 1, glypican-6, Gm1078, Gm1381, Gm628, golgin 245, GPR153, GPR154, GRAMD3, HGTD-P, HisRS, HNF-3γ, HSP 27, ICAT, IFT46, IL-3, INTU, Josephin-1, KBTBD7, KIAA1737, KLHL10, KLHL17, KLHL28, Kremen-1, Kremen-2, Lce1h, LEF-1, LGR4, LGR6, LNX4, LOC644070, LOC728110, LOC728677, LRFN2, LRG-47, LRP6, LRRTM3, LUZP2, LUZP4, MA1, Manic Fringe, MEGF10, MOM-4, MRP-L33, MRP-S2, MRP-S7, NAB2, NAT-15, NCoA-7, NCOAT, Ndfip1, Neuregulin-1, Neurotrypsin, Ninjurin-2, NKD1, NKD2, NKR-P1F, NOL10, NRSF, NTR3, NUDE1, Nup214, OR1Q1, ORP-3, OTTMUSG00000016789, OTTMUSG00000016790, OTUD7A, pan 14-3-3, PCTAIRE-1, PIWIL2, PLEKHH3, PMFBP1, POLR3K, Polyserase-1, PPAPDC2, PRAX-1, Prickle1, Prickle4, pro-MCH, PROCA1, Protamine 3, PTN, PTRH1, Puratrophin 1, Pygopus 1, Pygopus 2, R-Spondin3, R-Spondin4, RAG-1, RBM10, Reg γ, RG9MTD3, RGPD2, RNase T2, RNF115, RNF166, ROR1, RPRML, RSAD1, SBF2, SEL-10, SETD3, SIRP-γ, Six2, Slfn14, SLTM, SMG9, Snf5, Sox-7, SPAG7, SPZ1, SUSD2, Svs7, TAFA5, TBX15, TCEAL1, TCF-1, TCF-4, TEF-3, TEF-4, TLE1, TMEM186, TRABID, TRIAD3, Trichohyalin, TRIM32, TRIM37, TTBK2, UBL4A, UBTD1, USP37, USPL1, Vangl1, VPS45, VPS8, WDFY2, Wnt-10a, Wnt-10b, Wnt-16, Wnt-5a, Wnt-5b, Wnt-6, WRM-1, ZBTB24, ZBTB43, ZC3H12D, ZC3H14, ZFHX2, ZNF454, and ZNF746.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
SB-216763, 1 mg | sc-200646 | 1 mg | $71.00 | |||
SB-216763, 5 mg | sc-200646A | 5 mg | $202.00 |