BX-912
CAS No. : 702674-56-4
| Size | Price | Stock |
|---|---|---|
| 1mg | $70 | In-stock |
| 5mg | $102 | In-stock |
| 10mg | $180 | In-stock |
| 25mg | $380 | In-stock |
| 50mg | $630 | In-stock |
| 100mg | $950 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-11005 |
| M.Wt: | 471.35 |
| Formula: | C20H23BrN8O |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 100 mg/mL |
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].
IC50 & Target: IC50: 26 nM (PDK1)[1]
In Vitro: 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].
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