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
