<Suppliers Price>

Bisindolylmaleimide VIII acetate

Names

[ CAS No. ]:
138516-31-1

[ 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