SB216763

SB216763 Basic information
Product Name:SB216763
Synonyms:CS-332;GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem;SB 216763;3-(2,4-DICHLOROPHENYL)-4-(1-METHYL-1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE;3-(2,4-Dichlorophenyl)-4-...;3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione;SB-216763(SB 216763);GSK-3 Inhibitor IV, SB-216763
CAS:280744-09-4
MF:C19H12Cl2N2O2
MW:371.22
EINECS:
Product Categories:Inhibitors;Akt;Protein Kinase;Signalling;mTOR;PI3K
Mol File:280744-09-4.mol
SB216763 Structure
SB216763 Chemical Properties
Melting point 287-288.6 °C(lit.)
Boiling point 598.1±50.0 °C(Predicted)
density 1.47±0.1 g/cm3(Predicted)
storage temp. -20°C
solubility DMSO: 20 mg/mL, soluble
pka7.27±0.60(Predicted)
form Orange solid
color orange
Stability:Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38
Safety Statements 26-36
WGK Germany 3
HS Code 29339900
MSDS Information
ProviderLanguage
SigmaAldrich English
SB216763 Usage And Synthesis
DescriptionSB-216763 (280744-09-4) is a potent and selective inhibitor of glycogen synthase kinase-1 (GSK-3) IC50=34.3 nM.1 Acts at the ATP-binding domain. Displays protective effects in lung fibrosis mouse model.2 Displays neuroprotective effects on cultured neurons.3 SB-216763 maintains mouse embryonic stem cells in a pluripotent state.4?Cell permeable.
UsesSB 216763 is a potent and selective cell permeale ATP-competitive inhibitor of GSK3a. It stimulates glycogen synthesis in Chang human liver cells.
UsesSB-216763 was used to inhibit GSK-3β in human brain microvascular endothelial cell line and colorectal cancer cells.
DefinitionChEBI: 3-(2,4-dichlorophenyl)-4-(1-methyl-3-indolyl)pyrrole-2,5-dione is a member of indoles and a member of maleimides.
Biological ActivityPotent and selective glycogen synthase kinase-3 (GSK-3) inhibitor (K i = 9 nM for GSK-3 α ); competes with ATP. Has minimal activity against 24 other protein kinases (IC 50 > 10 μ M). Stimulates glycogen synthesis, gene transcription and is neuroprotective.
Biochem/physiol ActionsSB-216763 is a small molecule that competes with ATP and potently inhibits the activity α and β isozymes of GSK-3. It acts as neuroprotectant and prevents neuronal cell death induced by PI3-kinase pathway. It also delays preconditioning, reduces infarct size and prevents cardiac ischemia.
storageRoom temperature
References1) Coghlan et al. (2000), Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription; Chem. Biol., 7 793 2) Gurrieri et al. (2010), 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., 332 785 3) Cross et al. (2001), Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurons from death; J. Neurochem., 77 94 4) Kirby et al. (2012), Glycogen synthase kinase 3 (GSK3) inhibitor , SB-216763, promotes pluripotency in mouse embryonic stem cells; PLoS One, 7 e39329
SB216763 Preparation Products And Raw materials
Z-VAD-FMK Ibrutinib 2-THIO(3-IODOBENZYL)-5-(1-PYRIDYL)-[1,3,4]-OXADIAZOLE CAFESTOL 2,6-PYRIDINEDIAMINE, N6-[2-[[4-(2,4-DICHLOROPHENYL)-5-(1H-IMIDAZOL-1-YL)-2-PYRIMIDINYL]AMINO]ETHYL]-3-NITRO- LDE225 (NVP-LDE225,Erismodegib) S-[N-(3-PHENYLPROPYL)(THIOCARBAMOYL)]-L-CYSTEINE SEDANOLIDE KAHWEOL Saracatinib 1-AZAKENPAULLONE MK-2206 2HCl SB 415286 4-BENZYL-2-METHYL-1,2,4-THIADIAZOLIDINE-3,5-DIONE WIN 55,212-2 MESYLATE JWH-015 Benzeneacetamide, N-(2-(3-indolyl)ethyl)- SB216763

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