Brief Description

SB 415286 is a potent and selective cell-permeable, ATP-competitive inhibitor of GSK3α with an IC50 value of 78 nM (similar potency for GSK3β) and a Ki value of 31 nM.
IC50 value: 78 nM
Target: GSK3α
As a result of GSK3 inhibition, SB 415286 stimulates glycogen synthesis in the Chang human liver cell line with an EC50 value of 2.9 uM. SB 415286 also protects primary neurons from death induced by the PI3-kinase pathway.
References on SB 415286:
[1]. Pizarro JG, Yeste-Velasco M, Rimbau V et al. Neuroprotective effects of SB-415286 on hydrogen peroxide-induced cell death in B65 rat neuroblastoma cells and neurons. Int J Dev Neurosci. 2008 May-Jun;26(3-4):269-76.
[2]. Yeste-Velasco M, Folch J, Jiménez A et al. GSK-3 beta inhibition and prevention of mitochondrial apoptosis inducing factor release are not involved in the antioxidant properties of SB-415286. Eur J Pharmacol. 2008 Jul 7;588(2-3):239-43.
[3]. Pizarro JG, Folch J, Esparza JL et al. A molecular study of pathways involved in the inhibition of cell proliferation in neuroblastoma B65 cells by the GSK-3 inhibitors lithium and SB-415286. J Cell Mol Med. 2009 Sep;13(9B):3906-17.
[4]. Spinnler K, Mezger M, Steffens M et al. Role of glycogen synthase kinase 3 (GSK-3) in innate immune response of human immature dendritic cells to Aspergillus fumigatus. Med Mycol. 2010 Jun;48(4):589-97.
[5]. Mirlashari MR, Randen I, Kjeldsen-Kragh J. Glycogen synthase kinase-3 (GSK-3) inhibition induces apoptosis in leukemic cells through mitochondria-dependent pathway. Leuk Res. 2012 Apr;36(4):499-508.

Solubility

DMSO 50 mg/mL Ethanol 20 mg/mL

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light yellow to yellow solid