557514

Ro-31-8425

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

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₂₆H₂₄N₄O₂ · xHCl
• Número de CAS: 131848-97-0
• Peso molecular: 424.49 (free base basis)
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥94% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: red to orange-red
• solubilidad: DMSO: 10 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 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)
• Clave InChI: QQKKPWJFHBFCTH-UHFFFAOYSA-N

Descripción

Descripción general

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.

Acciones bioquímicas o fisiológicas

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

Advertencia

Toxicity: Irritant (B)

Reconstitución

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 1
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable