BX912 is a selective potent PDK1 inhibitor with an IC50 of 12 nM. BX912 also inhibits other kinases such as ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 potently prevents PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 < 10 μM). BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP. BX912 promotes a pronounced increase in the population of MDA-468 cells with 4 N DNA content, indicative of a block at the G2/M phase of the cell cycle. BX912 also potently inhibits the growth of HCT-116 cells in soft agar, showing a 96% inhibitory effect at a dose of 1 μM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL
Ethanol 60 mg/mL
|Related PDK1 Products|
NVP-BAG956 is a potent, ATP-competitive and selective dual PDK1 and class I PI 3-K inhibitor (IC50 values are 245, 56, 446, 35 and 117 nM for PDK1 and PI 3-K p110 -α, -β, -δ, and -γ respectively).
HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.
BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor with IC50 of 6 nM, 41 nM and 111 nM, respectively.
GSK2334470 is a highly specific and potent inhibitor of PDK1 with IC50 of 10 nM.
OSU-03012 is a novel and potent inhibitor of PDK-1 with an IC50 of 5 µM.
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