BMS-243117

BMS-243117 is a potent, and selective benzothiazole based p56Lck inhibitor with an IC50 of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC50 of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck[1].

Product Specifications

CAS Number

[225521-80-2]

UNSPSC

12352005

Target

Src

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bms-243117.html

Smiles

O=C(C1=CC=C2N=C(NC(NC(C)(C)C)=O)SC2=C1)NC3=C(C)C=CC=C3Cl

Molecular Formula

C20H21ClN4O2S

Molecular Weight

416.92

References & Citations

[1]Jagabandhu Das, et al. Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56 (lck) inhibitor BMS-243117. Bioorg Med Chem Lett. 2003 Jul 7;13 (13) :2145-9.