BX795

BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy[1][2][3][4].

Product Specifications

CAS Number

[702675-74-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; IKK; PDK-1

Type

Reference compound

Related Pathways

Autophagy; NF-κB; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/BX795.html

Purity

99.84

Solubility

DMSO : 33.33 mg/mL (ultrasonic)

Smiles

O=C(NCCCNC1=C(C=NC(NC2=CC=CC(NC(N3CCCC3)=O)=C2)=N1)I)C4=CC=CS4

Molecular Formula

C23H26IN7O2S

Molecular Weight

591.47

Precautions

H302, H315, H319, H335

References & Citations

[1]Feldman RI, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280 (20) :19867-74.|[2]Clark K, et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J Biol Chem. 2009 May 22;284 (21) :141|[3]Dangelmaier C, et al. PDK1 selectively phosphorylates Thr (308) on Akt and contributes to human platelet functional responses. Thromb Haemost. 2014 Mar 3;111 (3) :508-17.