Bioactivity | Bisindolylmaleimide VIII (Ro 31-7549) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII has IC50s of 53, 195, 163, 213, and 175 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, PKC-ε, respectively[1]. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[1][2]. |
Invitro | Bisindolylmaleimide VIII (5 μM; 8, 12 hours) 显著增加 TRA-8 诱导的细胞死亡,呈时间依赖性和剂量依赖性[2]。Bisindolylmaleimide VIII (5 μM; 6 hours) 与 TRA-8 联合处理后,4 h procaspase-8 显著降低,6 h完全消失[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Bisindolylmaleimide VIII 相关抗体: Western Blot Analysis[2] Cell Line: |
In Vivo | Bisindolylmaleimide VIII (100 μg;i.p;每隔一天服用三次),结合 toTRA-8,肿瘤几乎完全消退。单独使用 Bisindolylmaleimide VIII未引起肿瘤明显消退[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 125313-65-7 |
Formula | C24H22N4O2 |
Molar Mass | 398.46 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7. [2]. Ohtsuka T, et al. Bisindolylmaleimide VIII enhances DR5-mediated apoptosis through the MKK4/JNK/p38 kinase and the mitochondrial pathways. J Biol Chem. 2002 Aug 9;277(32):29294-303. |