Bisindolylmaleimide VIII acetate 是一种选择性蛋白激酶 C 抑制剂。它促进 Fas 介导的细胞凋亡,并抑制 T 细胞介导的自身免疫性疾病。
产品描述
Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively.
体外活性
Bisindolylmaleimide VIII acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases. Bisindolylmaleimide VIII acetate (5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners. Bisindolylmaleimide VIII acetate (5 μM; 6 hours) significantly decreases procaspase-8 at 4 h and completely disappears at 6 h after the combined treatment with TRA-8 [2].
体内活性
Bisindolylmaleimide VIII acetate (100 μg; i.p.; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. The alone treatment with Bisindolylmaleimide VIII acetate does not induce significant tumor regression [2].
Cas No.
138516-31-1
分子式
C26H26N4O4
分子量
458.51
别名
Bis VIII acetate;Ro 31-7549 acetate
储存和溶解度
DMSO:55 mg/ml (119.95 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years