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Bioactive Molecules

BX517 CAS:850717-64-5

BX517 CAS:850717-64-5
CAS NO.850717-64-5
Product Name BX517
SynonymsPDK1 Inhibitor II; [(3Z)-2-Oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]urea
FormulaC15H14N4O2
Molecular Weight282.3
Spec / Purity
Supply Capacity
Details A cell-permeable indolinone compound that acts as a potent, ATP site-targeting PDK1 inhibitor (IC50 = 6 nM) and effectively suppresses cellular Akt Thr308 phosphorylation level in PC-3 cultures (IC50 ≤1 μM), while affecting PKA (IC50 = 1.6 μM) and 7 other kinases (IC50 ≥600 nM) only at much higher concentrations. Its in vivo applicability is limited by a low aqueous solubility (2 μg/ml in PBS) and poor pharmacokinetics.


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