557514

Ro-31-8425

A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC₅₀ = 15 nM for rat brain PKC).

• Sinonimo/i: Ro-31-8425, 2-[8-(Aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, HCl, Bisindolylmaleimide X, HCl
• Formula empirica (notazione di Hill): C₂₆H₂₄N₄O₂ · xHCl
• Numero CAS: 131848-97-0
• Peso molecolare: 424.49 (free base basis)
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥94% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: red to orange-red
• Solubilità: DMSO: 10 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 1S/C26H24N4O2/c1-29-14-18(16-6-2-4-8-19(16)29)23-24(26(32)28-25(23)31)22-17-7-3-5-9-20(17)30-11-10-15(13-27)12-21(22)30/h2-9,14-15H,10-13,27H2,1H3,(H,28,31,32); QQKKPWJFHBFCTH-UHFFFAOYSA-N

Descrizione

Descrizione generale

A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC₅₀ = 15 nM for rat brain PKC). Exhibits some degree of isozyme specificity (IC₅₀ = 8 nM for PKC_α, 8 nM for PKC_βI, 14 nM for PKC_βII, 13 nM for PKC_γ, and 39 nM for PKC_ε). Shows slight selectivity for the conventional PKC isozymes PKC_α, PKC_β, and PKC_γ over the Ca²⁺-independent PKC isozyme PKC_ε. Upregulates CD11a expression and enhances mesenchymal stromal cell adhesion under flow.

A potent, cell-permeable, reversible, ATP-competitive, and selective protein kinase C inhibitor (IC₅₀ = 15 nM for rat brain PKC). Exhibits some degree of isozyme specificity (IC₅₀ = 8 nM for PKC_α, 8 nM for PKC_βI, 14 nM for PKC_βII, 13 nM for PKC_γ, and 39 nM for PKC_ε). Upregulates CD11a expression and enhances mesenchymal stromal cell adhesion under flow.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PKC

Product competes with ATP.

Reversible: yes

Target IC₅₀: 15 nM for rat brain PKC; 8 nM for PKCα, 8 nM for PKCβI, 14 nM for PKCβII, 13 nM for PKCγ, and 39 nM for PKCε

Attenzione

Toxicity: Irritant (B)

Ricostituzione

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Altre note

Levy, O., et al. 2015. Cell Reports10, In press.
Merritt, J.E., et al. 1997. Cell Signal 9, 53.
Wilkinson, S.E., et al. 1993. Biochem. J. 294, 335.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable