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Catalog No.
PDK1 inhibitor,potent and ATP-competitive
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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].

[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
Cas No.702674-56-4
Solubility≥23.55 mg/mL in DMSO; insoluble in H2O; ≥10.25 mg/mL in EtOH
Chemical NameN-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
SDFDownload SDF
Canonical SMILESC1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCC4=CN=CN4)Br
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description BX-912 is a potent, ATP-competitive inhibitor of PDK-1 with IC50 value of 26 nM.
Targets PDK-1          
IC50 26 nM          

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