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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.
| Molecular Weight | 471.35 |
| Formula | C20H23BrN8O |
| CAS Number | 702674-56-4 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PDK1 Products |
|---|
| OSU-03012
OSU-03012 is a novel and potent, blood-brain permeable inhibitor of PDK-1 with an IC50 of 5 µM. |
| GSK2334470
GSK2334470 is a highly specific and potent inhibitor of PDK1 with IC50 of 10 nM. |
| BX-795
BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor with IC50 of 6 nM, 41 nM and 111 nM, respectively. |
| AZD7545
AZD7545 is a potent PDHK inhibitor with IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. |
| NVP-BAG956
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). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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