Bisindolylmaleimide I (hydrochloride) (Synonyms: BIM I, GF109203X, G 6850) |
カタログ番号GC18725 |
ビシンドリルマレイミドI(BIM I)は、高度に選択的で細胞浸透性があり、可逆的なPKC阻害剤(Ki = 14 nM)であり、低い選択性を持つPKC阻害剤スタウロスポリンと構造的に類似しています。
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Cas No.: 176504-36-2
Sample solution is provided at 25 µL, 10mM.
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 . 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). It also competitively antagonizes the serotonin (5-HT) receptor subtype 5-HT3 with a Ki value of 61 nM.
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