Bisindolylmaleimide VIII  (Synonyms: Ro 31-7549; Bis VIII)

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-β_I, PKC-β_II, PKC-γ, PKC-ε, respectively^[1]. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases^[1][2].

Bisindolylmaleimide VIII (5 μM; 8, 12 hours) dramatically increases TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners^[2].
Bisindolylmaleimide VIII (5 μM; 6 hours) significantly decreases procaspase-8 at 4 h and completely disappeares at 6 h after the combined treatment with TRA-8^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Bisindolylmaleimide VIII (100 μg; i.p; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. With Bisindolylmaleimide VIII alone does not induce significant tumor regression^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

398.46

C₂₄H₂₂N₄O₂

125313-65-7

O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC=C5)NC3=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]