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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > PI3K/Akt/mTOR > SB-216763CAS：280744-09-4
Molecular Formula：C19H12N2O2Cl2
Molecular Weight：371.22
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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| CAS | 280744-09-4 |
| Name | SB-216763 |
| Molecular Formula | C19H12N2O2Cl2 |
| Molecular Weight | 371.22 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00941298 |
| SMILES | O=C(NC1=O)C(C2=CC=C(C=C2Cl)Cl)=C1C3=CN(C4=C3C=CC=C4)C |
| Target Point | GSK-3 |
| Passage | PI3K/Akt/mTOR;Stem Cells |
| Background | SB 216763 is a potent, selective and ATP-competitive GSK-3 inhibitor. |
| Biological Activity | SB 216763是有效，选择性和ATP竞争性的 GSK-3 抑制剂，抑制GSK-3α和GSK-3β的 IC50 为34.3 nM。SB-216763（10-20μM）在HEK293细胞中以剂量依赖性方式诱导β-连环蛋白介导的转录。[1-6] |
| IC50 | GSK-3α:34.3nM;GSK-3β:34.3nM [1-6] |
| Data Literature Source | [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 |
| Unit | Bottle |
| Specification | 5mg 25mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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