557514

Ro-31-8425

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

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

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥94% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: red to orange-red
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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)
• chave InChI: QQKKPWJFHBFCTH-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/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

Advertência

Toxicity: Irritant (B)

Reconstituição

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

Outras 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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable