GSK-2334470

• CAT Number: I000880
• CAS Number: 1227911-45-6
• Molecular Formula: C₂₅H₃₄N₈O
• Molecular Weight: 462.59
• Purity: ≥95%
• Target: PDK-1
• Solubility: 10 mM in DMSO
• Storage: 2-8°C
• IC50: 10 nM
• IUPAC Name: (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl]-N-cyclohexyl-6-methylpiperidine-3-carboxamide
• InChI: InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
• InChIKey: QLPHOXTXAKOFMU-WBVHZDCISA-N
• SMILES: CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5

GSK2334470 is a novel, highly specific PDK1 inhibitor with an IC50 of about 10 nM and is inactive against other AGC-kinase-related proteins. GSK2334470 also inhibited PDK1 by phosphorylating PDKtide peptide substrates, with an IC50 of 10 nM.

Reference

1:PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242. Yang C, Huang X, Liu H, Xiao F, Wei J, You L, Qian W.Oncotarget. 2017 Mar 29. doi: 10.18632/oncotarget.16642. [Epub ahead of print] PMID: 28402933 Free Article2:Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Najafov A, Sommer EM, Axten JM, Deyoung MP, Alessi DR.Biochem J. 2011 Jan 15;433(2):357-69. doi: 10.1042/BJ20101732. PMID: 21087210