Bisindolylmaleimide VIII acetate

SKU: orb1218870

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.

Key Properties

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

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro 31-7549 acetate | Bis VIII acetate

Quick Database Links

Gene Symbol

Apoptosis