RO-31-7549

Product NameRO-31-7549
CAS125313-65-7
MFC24H22N4O2
MW398.46
EINECS
MOL File125313-65-7.mol

Chemical Properties

storage temp.	−20°C
solubility	DMSO: soluble
form	Red to reddish-orange solid
color	red to red-orange

Safety Information

WGK Germany

MSDS

Provider	Language
SigmaAldrich	English

Usage And Synthesis

Uses

It is a potent inhibitor of protein kinase C (PKC) activity.

General Description

A cell permeable, reversible, selective protein kinase C (PKC) inhibitor (IC₅₀ = 158 nM for rat brain PKC) that acts at the ATP binding site of PKC. Does not inhibit the tyrosine phosphorylation or the activation of phospholipase Cγ₁. Exhibits some degree of PKC isozyme specificity (IC₅₀ = 53 nM for PKC_α, 195 nM for PKC_βI, 163 nM for PKC_βII, 213 nM for PKC_γ, and 175 nM for PKC_ε). Inhibits carbachol-evoked noradrenaline release (IC₅₀ = 600 nM).

Biochem/physiol Actions

Cell permeable: yes

in vivo

Bisindolylmaleimide VIII (100 μg; i.p; every other day for three doses) results in nearly complete tumor regression combined toTRA-8. With Bisindolylmaleimide VIII alone does not induce significant tumor regression^[2].

Animal Model:	6-8-week-old female NOD/SCID mice^[2].
Dosage:	100 μg
Administration:	i.p.; every other day for three doses
Result:	Resulted in nearly complete tumor regression combined toTRA-8.

IC 50

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)