BX-912
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 471.35 |
| Cas No. | 702674-56-4 |
| Formula | C20H23BrN8O |
| Solubility | ≥23.55 mg/mL in DMSO; insoluble in H2O; ≥10.25 mg/mL in EtOH |
| Chemical Name | N-[3-[[5-bromo-4-[2-(1H-imidazol-5-yl)ethylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCC4=CN=CN4)Br |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | BX-912 is a potent, ATP-competitive inhibitor of PDK-1 with IC50 value of 26 nM. | |||||
| Targets | PDK-1 | |||||
| IC50 | 26 nM | |||||
Quality Control & MSDS
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Chemical structure
