| Identification | Back Directory | [Name]
RO-31-7549 | [CAS]
125313-65-7 | [Synonyms]
RO-31-7549
RO 31-7549 ACETATE SALT
Bisindolylmaleimide VIII
BISINDOLYLMALEIMIDE VIII ACETATE
BIDINDOLYLMALEIMIDE VIII, ACETETE
Ro-31-7549, Monohydrate - CAS 125313-65-7 - Calbiochem
2-[1-3(AMINOPROPYL)INDOL-3-YL]-3(1-METHYL-1H-INDOL-3-YL)MALEIMIDE, ACETATE
3-(1-(3-Aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-(1-(3-aminopropyl)-1H-indol-3-yl)-4-(1-methyl-1H-indol-3-yl)- | [Molecular Formula]
C24H22N4O2 | [MOL File]
125313-65-7.mol | [Molecular Weight]
398.46 |
| Hazard Information | Back Directory | [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) |
|
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck Millipore
|
| Tel: |
1-400-889-1988 400-889-1988 |
| Website: |
http://www.merckmillipore.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|