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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Related PDK1 Products |
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PDKtide
PDKtide is a biological active peptide. |
PDK1-IN-RS2
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1. |
PS47
PS47 is an inactive E-isomer of PS48. PS48 is an activator of PDK1. PS47 can be used as a negative control for PS48. |
PS210
PS210 is a potent activator of PDK1 that binds to the PIF-pocket and allosterically modulates the active site of PDK1. |
WAY-299338
WAY-299338 is a modulator of the Protein Kinase PDK1. |
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