280744-09-4 Usage
Description
SB216763, also known as 280744-09-4, is a potent and selective inhibitor of glycogen synthase kinase-1 (GSK-3) with an IC50 value of 34.3 nM. It acts at the ATP-binding domain and has been shown to display protective effects in lung fibrosis mouse models, neuroprotective effects on cultured neurons, and maintain mouse embryonic stem cells in a pluripotent state. SB216763 is a cell-permeable compound.
Uses
1. Used in Cell Biology Research:
SB216763 is used as a research tool for inhibiting GSK-3α to study its role in various cellular processes and pathways.
2. Used in Liver Cell Research:
SB216763 is used as a stimulator of glycogen synthesis in Chang human liver cells, aiding in the understanding of glycogen metabolism and its regulation.
3. Used in Neuroprotection Studies:
SB216763 is used as a neuroprotective agent in cultured neurons, helping researchers investigate its potential in treating neurodegenerative diseases.
4. Used in Embryonic Stem Cell Research:
SB216763 is used to maintain mouse embryonic stem cells in a pluripotent state, which is crucial for studying stem cell biology and potential therapeutic applications.
5. Used in Human Brain Microvascular Endothelial Cell Line:
SB216763 is used as an inhibitor of GSK-3β in human brain microvascular endothelial cell lines, providing insights into the role of GSK-3β in the endothelial cells of the brain.
6. Used in Colorectal Cancer Research:
SB216763 is used to inhibit GSK-3β in colorectal cancer cells, assisting researchers in understanding the role of GSK-3β in cancer progression and potential therapeutic strategies.
Biological Activity
Potent 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 Actions
SB-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.
References
1) 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
Check Digit Verification of cas no
The CAS Registry Mumber 280744-09-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 2,8,0,7,4 and 4 respectively; the second part has 2 digits, 0 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 280744-09:
(8*2)+(7*8)+(6*0)+(5*7)+(4*4)+(3*4)+(2*0)+(1*9)=144
144 % 10 = 4
So 280744-09-4 is a valid CAS Registry Number.
InChI:InChI=1/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)
