SB 415286 Inhibitor CAS No. 264218-23-7

Cat. No.	Name	Size	Price	Add Cart
KI0494	SB 415286	10 mg	$208
KI0494	SB 415286	50 mg	$690

Chemical Characteristic

Product Name	SB 415286
CAS No.	264218-23-7
Molecular Weight	359.72
Formula	C₁₆H₁₀ClN₃O₅
Chemical Name	3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione
Smiles	N1C(=O)C(=C(C1=O)c1c(cccc1)[N](=O)O)Nc1cc(c(cc1)O)Cl
Chemical Structure

Biological activities

SB 415286 is a potent and selective cell permeable glycogen synthase kinase 3 (GSK3) inhibitor. The IC50 of SB 415286 is 78 nM against glycogen synthase kinase 3. SB 415286 protects primary neurones from death induced by reduced phosphatidylinositol 3-kinase pathway activity.^[1] SB 415286 suppresses GSK-3α with a Ki of 31 nM. SB 415286 is equally effective at blocking human GSK-3α and GSK-3β. In the presence of 0.1 mM ATP, 10 μM SB-415286 inhibits GSK-3β kinase activity by 83%. SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 of 2.9 μM. The maximum effective concentration of SB-415286 is 10 μM. SB 415286 activates glycogen synthase in Chang human liver cells and in HEK293 cells. SB 415286 induces transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells.^[2] SB 415286 activates glycogen synthase and decreases the relative phospho-GS (Ser640/1) level, more in glucose-depleted than -replete cells.^[3] mIMCD3 cells treated with SB 415286 significantly reduces expression of PC2 at the cell surface following GSK3 inhibition.^[4]

Protocols

SB 415286 is prepared in DMSO.^[3]

References

[1] Martinez A, et al. Glycogen synthase kinase 3 (GSK-3) inhibitors as new promising drugs for diabetes, neurodegeneration, cancer, and inflammation. Med Res Rev. 2002, 22(4): 373-384. [2] Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000, 7(10): 793-803. [3] Montori-Grau M, et al. Glucose dependence of glycogen synthase activity regulation by GSK3 and MEK/ERK inhibitors and angiotensin-(1-7) action on these pathways in cultured human myotubes. Cell Signal. 2013, 25(5): 1318-1327. [4] Streets AJ, et al. Identification of an N-terminal glycogen synthase kinase 3 phosphorylation site which regulates the functional localization of polycystin-2 in vivo and in vitro. Hum Mol Genet. 2006, 15(9): 1465-1473.

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