Description
A p38 MAPK inhibitor (IC50 = 9 nM for p38α); 10-fold selective for p38α over p38β MAPK and 2,000-fold selective over a panel of 20 additional kinases; inhibits secretion of IL-6 from multiple myeloma patient-derived BMSCs in a concentration-dependent manner; increases PS-341-induced growth inhibition, DNA fragmentation, and caspase-8 and PARP cleavage in MM.1S cells at 100 and 200 nM; reduces microvessel density and tumor load and increases survival in a 5T33MM murine myeloma model at 150 and 450 mg/kg
Formal name: 6-chloro-5-[[(2R,5S)-4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-N,N,1-trimethyl-α-oxo-1H-indole-3-acetamide
Synonyms: Talmapimod
Molecular weight: 513
CAS: 309913-83-5
Purity: ≥98%
Formulation: A crystalline solid
