Bisindolylmaleimide VIII acetate

Names

[ Name ]:
Bisindolylmaleimide VIII acetate

[Synonym ]:
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

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Signaling Pathways >> TGF-beta/Smad >> PKC

[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]

[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.

[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.

Chemical & Physical Properties

[ 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

MSDS

Click to get detail MSDS

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.