Description
3-
Phosphoinositide-
dependent protein kinase 1 (PDK1) is a serine-
threonine kinase that phosphorylates and activates a range of other kinases, including protein kinase (PK)B, PKA, and certain isoforms of PKC.
1 BX-
912 is a potent, ATP-
competitive inhibitor of PDK1 (IC
50 = 26 nM).
2 It less effectively inhibits a panel of related serine-
threonine kinases.
2 BX-
912 has been used to evaluate the role of PDK1 in kinase activation and cell survival.
3,4,5
References
[1] feldman ri1, wu jm, polokoff ma, kochanny mj, dinter h, zhu d, biroc sl, alicke b, bryant j, yuan s, buckman bo, lentz d, ferrer m, whitlow m, adler m, finster s, chang z, arnaiz do. novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. j biol chem. 2005 may 20;280(20):19867-74. epub 2005 mar 16.