BX912|cas 702674-56-4| DC Chem|Supplier|Price|Buy  

BX912|cas 702674-56-4| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: BX912|cas 702674-56-4,Purity: >98% ,Cat No. DC7093, In stock.

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BX912|cas 702674-56-4 ,Synonym: BX912; BX 912  ,Chemical name: N-(3-(4-(2-(1H-imidazol-5-yl)ethylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide ,Molecular Formula: C20H23BrN8O ,MW:471.35

BX912, cas 702674-56-4,Purity: >98%, Best Price and quality from DC Chemicals. BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc.

BX912 prevents ChcK1, PKA, c-kit, and KDR with IC50 of 0.83, 0.11, 0.85, and 0.41 μM, resepectively. BX912 blocks PDK1/Akt signaling in tumor cells and suppresses the anchorage-dependent growth of a variety of tumor cell lines (such as PC-3 cells ) in culture or induces apoptosis. A number of cancer cell lines (such as MDA-468 breast cancer) with elevated Akt activity are >30-fold more sensitive to growth inhibition by PDK1 inhibitor BX912 in soft agar than on tissue culture plastic, consistent with the cell survival function of the PDK1/Akt signaling pathway, which is particularly important for unattached cells. BX912 potently blocks PDK1 enzyme activity in a direct kinase assay format, although BX912 fails to block preactivated AKT2 activity (IC50 > 10 μM). Therefore, BX-912 is a direct inhibitor of PDK1. BX912 is a competitive inhibitor of PDK1 activity with respect to its substrate, ATP, suggesting that BX912 binds to the ATP binding pocket of PDK1. The aminopyrimidine backbone of BX912 adopts a similar orientation in the active site of PDK1. 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. BX912 potently inhibits the growth of PC-3 cells in soft agar, displaying IC50 of 0.32 μM. [1]