Bisindolylmaleimide VIII
Based on 1 publication(s) in Google Scholar
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. Bisindolylmaleimide VIII facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 125313-65-7
- Formula: C24H22N4O2
- Molecular Weight:398.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Bisindolylmaleimide VIII
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Biological Activity
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Rat Brain PKC 158 nM (IC50) |
PKCα 53 nM (IC50) |
PKC-βI 195 nM (IC50) |
PKC-βII 163 nM (IC50) |
PKCγ 213 nM (IC50) |
PKCε 175 nM (IC50) |
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.
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Cell Line:1321N1 cells
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Concentration:5 μM
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Incubation Time:6 hours
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Result:Significantly decreased procaspase-8 at 4 h and completely disappeared at 6 h.
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Cell Line:1321N1 cells
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Concentration:5 μM
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Incubation Time:8, 12 hours
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Result:Dramatically increased TRA-8-induced cell death in time-dependent and TRA-8 dose-dependent manners.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8-week-old female NOD/SCID mice[2].
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Dosage:100 μg
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Administration:i.p.; every other day for three doses
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Result:Resulted in nearly complete tumor regression combined toTRA-8.
Chemical Information
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CAS No. 125313-65-7
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Molecular Weight 398.46
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Formula C24H22N4O2
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SMILES
O=C(C(C1=CN(CCCN)C2=C1C=CC=C2)=C3C4=CN(C)C5=C4C=CC=C5)NC3=O
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Synonyms
Ro 31-7549; Bis VIII
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
Desmoplakin loss leads to PKC-dependent insertion of series sarcomeres and contractile dysfunction in cardiomyocytes. [Abstract]2025 May 19:2025.05.15.654389. PMID: 40475450
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bisindolylmaleimide VIII Related Classifications
HY-129624 Related Classifications
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