BX-912 is a potent and selective inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) with IC50 value of 26nM [1]. BX-912 has shown 9-fold selectivity for PDK1 relative to PKA and 105-fold selectivity against PKC [1].
BX-912 has been revealed to suppress the MDA-468 cells (one kind of breast tumor cell expressing high levels of activated Akt) growth and increase?caspase-3/7 activity. On the contrary, BX-912 had no effect on caspase-3/7 activation in normal primary PrECs and primary HMECs. Moreover, BX-912 has been demonstrated to induce cell cycle arrest of MDA-468 cells at the G2/M phase [1].
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.
