For research use only. Not for therapeutic Use.
BX517 is a potent and selective inhibitor of PDK1 with IC50 of 6 nM.
BX-517 blocks activation of Akt in tumor cells, is potent with IC50 of 0.1-1.0 μM[1]. BX-517 blocks AKT2 activation in cells with submicromolar potency. BX-517 is 100-fold selective or better against a panel of seven additional Ser/Thr and Tyr kinases[2].
| Catalog Number | I005103 |
| CAS Number | 850717-64-5 |
| Synonyms | [(3Z)-2-oxo-3-[1-(1H-pyrrol-2-yl)ethylidene]-1H-indol-5-yl]urea |
| Molecular Formula | C15H14N4O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C15H14N4O2/c1-8(11-3-2-6-17-11)13-10-7-9(18-15(16)21)4-5-12(10)19-14(13)20/h2-7,17H,1H3,(H,19,20)(H3,16,18,21)/b13-8- |
| InChIKey | DFURSNCTQGJRRX-JYRVWZFOSA-N |
| SMILES | CC(=C1C2=C(C=CC(=C2)NC(=O)N)NC1=O)C3=CC=CN3 |
| Reference | [1]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 2: optimization of BX-517. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3819-25. [2]. Islam I, et al. Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3814-8. |
