"目錄號(hào): HY-13842

PI3K/Akt/mTOR-

BX517 是一種有效的，選擇性的PDK1抑制劑，IC50值為 6 nM。

PDK-1

相關(guān)產(chǎn)品

TEPP-46-BX795-GSK2334470-OSU-03012-PS48-PDK1 inhibitor-BX-912-NVP-BAG956-

生物活性

Description

BX517 is a potent and selective inhibitor ofPDK1withIC50of 6 nM.

IC50& Target

IC50: 6 nM (PDK1)

In Vitro

BX-517 blocks activation of Akt in tumor cells, is potent with IC50of 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].

References

[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.