SB216763
| Code | Size | Price |
|---|
| AG-CR1-3659-M001 | 1 mg | £40.00 |
Quantity:
| AG-CR1-3659-M005 | 5 mg | £70.00 |
Quantity:
| AG-CR1-3659-M025 | 25 mg | £250.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Storage:
Short Term: +4°C. Long Term: -20°C
Documents
Further Information
Alternate Names/Synonyms:
3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Appearance:
Orange powder.
CAS:
280744-09-4
EClass:
32160000
Form (Short):
liquid
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
Long Description:
Chemical. CAS: 280744-09-4. Formula: C19H12Cl2N2O2. MW: 371.2. Synthetic. Potent and selective cell permeable, ATP-competitive inhibitor of GSK3alpha with an IC50 value of 34nM (and similar potency for GSK3beta). DYRK1A inhibitor (IC50=0.8µM). Stimulates glycogen synthesis in liver cells and induces beta-catenin-dependent gene transcription. Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. Anticancer agent with antiproliferative activity. Reduces pulmonary inflammation and fibrosis in a mouse model. Shown to delay preconditioning, reduces infarct size and prevents cardiac ischemia. Promotes pluripotency in mouse embryonic stem cells. Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis and inflammation.
MDL:
MFCD09753369
Molecular Formula:
C19H12Cl2N2O2
Molecular Weight:
371.2
Package Type:
Plastic Vial
Product Description:
Potent and selective cell permeable, ATP-competitive inhibitor of GSK3alpha with an IC50 value of 34nM (and similar potency for GSK3beta). DYRK1A inhibitor (IC50=0.8µM). Stimulates glycogen synthesis in liver cells and induces beta-catenin-dependent gene transcription. Acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. Anticancer agent with antiproliferative activity. Reduces pulmonary inflammation and fibrosis in a mouse model. Shown to delay preconditioning, reduces infarct size and prevents cardiac ischemia. Promotes pluripotency in mouse embryonic stem cells. Glycogen synthase kinase 3 (GSK3) is a serine/threonine protein kinase that is inhibited by an assortment of extracellular stimuli such as insulin, growth factors, cell specification factors and cell adhesion. Its activity regulates many cell functions including the control of cell division, apoptosis and inflammation.
Purity:
>98% (HPLC)
SMILES:
O=C(N1)C(C2=CN(C)C3=C2C=CC=C3)=C(C4=C(Cl)C=C(Cl)C=C4)C1=O
Solubility Chemicals:
Soluble in DMSO (20mg/ml) or ethanol.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription: M.P. Coghlan, et al.; Chem. Biol. 7, 793 (2000) | Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death: D.A. Cross, et al.; J. Neurochem. 77, 94 (2001) | GSK3 inhibitors: development and therapeutic potential: P. Cohen & M. Goedert; Nat. Rev. Drug Discov. 3, 479 (2004) | The selectivity of protein kinase inhibitors: a further update: J. Bain, et al.; Biochem. J. 408, 297 (2007) | Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival: M.H. Liang & D.M. Chuang; J. Biol. Chem. 282, 3904 (2007) | Delayed cardioprotection afforded by the glycogen synthase kinase 3 inhibitor SB-216763 occurs via a KATP- and MPTP-dependent mechanism at reperfusion: E.R. Gross, et al.; Am. J. Physiol. Heart Circ. Physiol. 294, H1497 (2008) | 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: C. Gurrieri, et al.; J. Pharmacol. Exp. Ther. 332, 785 (2010) | Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells: L.A. Kirby, et al.; PLoS One 7, e39329 (2012) | GSK-3 inhibitor inhibits cell proliferation and induces apoptosis in human osteosarcoma cells: H. Nishimura, et al.; Oncol. Rep. 35, 2348 (2016)
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