RO-31-7549
RO-31-7549 Basic information
- Product Name:
- RO-31-7549
- Synonyms:
-
- BISINDOLYLMALEIMIDE VIII ACETATE
- 1H-Pyrrole-2,5-dione, 3-(1-(3-aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-
- 3-(1-(3-Aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
- Bisindolylmaleimide VIII
- 2-[1-3(AMINOPROPYL)INDOL-3-YL]-3(1-METHYL-1H-INDOL-3-YL)MALEIMIDE, ACETATE
- RO-31-7549
- RO 31-7549 ACETATE SALT
- BIDINDOLYLMALEIMIDE VIII, ACETETE
- CAS:
- 125313-65-7
- MF:
- C24H22N4O2
- MW:
- 398.46
- Product Categories:
-
- Amines
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Protein Kinase Inhibitors and Activators
- Mol File:
- 125313-65-7.mol
RO-31-7549 Chemical Properties
- storage temp.
- −20°C
- solubility
- DMSO: soluble
- form
- Red to reddish-orange solid
- color
- red to red-orange
MSDS
- Language:English Provider:SigmaAldrich
RO-31-7549 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 PKCα, 195 nM for PKCβI, 163 nM for PKCβII, 213 nM for PKCγ, and 175 nM for PKCε). 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)
RO-31-7549Supplier
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