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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Blk; Fyn; Lck
Curated Selection
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