Formulation: A crystalline solid
Formal Name: 3-[1-[3-(dimethylamino)propyl]-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, monohydrochloride
Purity: ≥98%
Formula Markup: C25H24N4O2 • HCl
Formula Weight: 449
Shelf life (days): 1460
CAS Number: 176504-36-2
Notes: Bisindolylmaleimide I (BIM I) is a highly selective, cell-permeable, and reversible PKC inhibitor (Ki = 14 nM) that is structurally similar to the poorly selective PKC inhibitor staurosporine (Item No. 81590).{17275} It acts as a competitive inhibitor for the ATP binding site of PKC and shows high selectivity for PKCα, β1, β2, γ, δ, and ε isozymes. BIM I directly inhibits glycogen synthase kinase 3 (GSK3) in primary adipocyte lysates (IC50 = 360 nM) and in GSK3β immunoprecipitates derived from rat epididymal adipocytes (IC50 = 170 nM).{17379} It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.{17380}