| Bioactivity | BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[1]. | ||||||||||||
| Invitro | BX-912 promotes a block at the G2/M phase of the cell cycle in MDA-468 cells[1].BX-912 binds to the ATP binding site of PDK1, and is 9-fold selective for PDK1 relative to PKA. BX-912 blocks PDK1 activity in PTEN-negative PC-3 cells. PTEN-negative PC-3 cells display constitutive activation of Akt which is reflected in high levels of the PDK1 product, phospho-Thr308-Akt[1].BX-912 is identified in a coupled assay measuring PDK1- and PtdIns-3,4-P2-mediated Akt activation, which can detect inhibitors of PDK1, AKT2, or other steps critical for activation of AKT2[1]. | ||||||||||||
| Name | BX-912 | ||||||||||||
| CAS | 702674-56-4 | ||||||||||||
| Formula | C20H23BrN8O | ||||||||||||
| Molar Mass | 471.35 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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BX-912
CAS: 702674-56-4 F: C20H23BrN8O W: 471.35
BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumo
Data collection：peptidedb@qq.com
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