Bisindolylmaleimide VIII acetate
Modify Date: 2024-01-20 17:28:09
Bisindolylmaleimide VIII acetate structure
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Common Name | Bisindolylmaleimide VIII acetate | ||
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| CAS Number | 138516-31-1 | Molecular Weight | 458.509 | |
| Density | N/A | Boiling Point | 693ºC at 760 mmHg | |
| Molecular Formula | C26H26N4O4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 372.9ºC | |
Use of Bisindolylmaleimide VIII acetateBisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate 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 acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2]. |
| Name | acetic acid,3-[1-(3-aminopropyl)indol-3-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione |
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| Synonym | More Synonyms |
| Description | Bisindolylmaleimide VIII acetate (Ro 31-7549 acetate) is a potent and selective protein kinase C (PKC) inhibitor with an IC50 of 158 nM for rat brain PKC. Bisindolylmaleimide VIII acetate 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 acetate facilitates Fas-mediated apoptosis and inhibits T cell-mediated autoimmune diseases[2]. |
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| Related Catalog | |
| Target |
Rat Brain PKC:158 nM (IC50) PKC-α:53 nM (IC50) PKC-βI:195 nM (IC50) PKC-βII:163 nM (IC50) PKC-γ:213 nM (IC50) PKC-ε:175 nM (IC50) |
| 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[2]. 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[2]. Apoptosis Analysis[2] 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[2] 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[2]. Animal Model: 6-8-week-old female NOD/SCID mice[2]. Dosage: 100 μg Administration: IP; every other day for three doses Result: Resulted in nearly complete tumor regression combined toTRA-8. |
| References |
| Boiling Point | 693ºC at 760 mmHg |
|---|---|
| Molecular Formula | C26H26N4O4 |
| Molecular Weight | 458.509 |
| Flash Point | 372.9ºC |
| Exact Mass | 458.195404 |
| PSA | 119.35000 |
| LogP | 4.16900 |
| Vapour Pressure | 4.7E-19mmHg at 25°C |
| Ro 31-7549 acetate |
| Bisindolylmaleimide VIII acetate |
| 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione acetate (1:1) |
| BIMI0231 |
| 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione acetate |
| MFCD00909467 |
| bisindolylmaleimide viii |
| 1H-Pyrrole-2,5-dione, 3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-, acetate (1:1) |
| Bisindolylmaleimide VIII acetate salt |