Bisindolylmaleimide VIII (acetate)
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 158 nM for rat brain PKC
Bisindolylmaleimide VIII is a protein kinase C (PKC) inhibitor.
The protein kinase C (PKC) consists of a family of closely related isoenzymes mediating various signal transduction processes. The ten isoenzymes that have been currently identified can be divided into three families on the basis of their different requirements for activation. Members of the conventional PKC family are Ca2+ and phospholipid-dependent and are activated by diacylglycerols and phorbol esters.
In vitro: Previous study found that bisindolylmaleimides carrying a straight-chain alkyl side-chain bearing a cationic substituent, such as Ro 31-7549 (bisindolylmaleimide VIII) and Ro 31-8220, showed a significant improvement in potency over the simple bisindolylmaleimides. For bisindolylmaleimide VIII, a further improvement in potency was obtained by restricting the position of the amine substituent. Moreove, unlike the indolocarbazole, staurosporine, which displayed 2-fold selectivity for PKC-β over the other examined isoenzymes, bisindolylmaleimide VIII exhibited a slight selectivity for PKC-α over the other isoenzymes. Compounds such as bisindolylmaleimide VIII carrying a straight-chain alkyl side-chain with the cationic substituent were found to be equipotent as inhibitors of PKC-β, PKC-γ and PKC-ε .
In vivo: Animal study found that, in neonatal rats, high glucose levels could induce the hypertrophy of cardiomyocytes. Ro-31-8220, a analog of bisindolylmaleimide VIII, was able to reverse the effect of high glucose on the cardiac myocytes,which might be through PKC/NF-κB/c-Fos pathway .
Clinical trial: So far, no clinical study has been conducted.
 Wilkinson, S. E.,Parker, P.J. and Nixon, J.S. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochemistry Journal 294, 335-337 (1993).
 Zhang, W. B. et al. Reverse effect of protein kinase C inhibitor Ro-31-8220 on the hypertrophy of cardiomyocytes of neonatal rats induced by high glucose levels. Chinese Journal of Pathophysiology. 2009-08.
|Storage||Store at -20°C|
|Formula||C24H22N4O2 • C2H4O2|
|Synonyms||BIM VIII,Ro 31-7549|
|Solubility||Soluble in DMSO|
|Chemical Name||3-[1-(3-aminopropyl)-1H-indol-3-yl]-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione, acetate|