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Bisindolylmaleimide VIII acetate

CAS No. 138516-31-1

Bisindolylmaleimide VIII acetate( Ro 31-7549 acetate | Bis VIII acetate )

Catalog No. M23542 CAS No. 138516-31-1

Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Bisindolylmaleimide VIII acetate
  • Note
    Research use only, not for human use.
  • Brief Description
    Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC).
  • Description
    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.
  • In Vitro
    Bisindolylmaleimide VIII acetate (Ro 31-7549 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 disappeares at 6 h after the combined treatment with TRA-8. Apoptosis Analysis Cell Line:1321N1 cells Concentration:5 μM Incubation Time:8, 12 hours Result: Dramatically increased TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners.Western Blot Analysis Cell Line:1321N1 cells Concentration:5 μM Incubation Time:6 hours Result:Significantly decreased procaspase-8 at 4 h and completely disappeared at 6 h.
  • In Vivo
    Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate; 100 μg; IP; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. The treatment with Bisindolylmaleimide VIII acetate alone does not induce significant tumor regression. Animal Model:6-8-week-old female NOD/SCID mice. Dosage:100 μg Administration:IP; every other day for three doses Result:Resulted in nearly complete tumor regression combined toTRA-8.
  • Synonyms
    Ro 31-7549 acetate | Bis VIII acetate
  • Pathway
    Apoptosis
  • Target
    Apoptosis
  • Recptor
    Apoptosis|PKC|PKCα|PKCβ1|PKCβ2|PKCγ|PKCε
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    138516-31-1
  • Formula Weight
    458.51
  • Molecular Formula
    C26H26N4O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (545.24 mM)
  • SMILES
    O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC=C5)NC3=O.CC(O)=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

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.
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