557508

Ro-31-7549, Monohydrate

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.

• Sinônimo(s): Ro-31-7549, Monohydrate, 2-[1-3(Aminopropyl)indol-3-yl]-3(1-methyl-1H-indol-3-yl)maleimide, Acetate, Bisindolylmaleimide VIII, Acetate
• Fórmula empírica (Notação de Hill): C₂₄H₂₂N₄O₂ · xC₂H₄O₂ · yH₂O
• Número CAS: 125313-65-7
• Peso molecular: 398.46 (anhydrous free base basis)
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥93% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: red to red-orange
• solubilidade: DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• InChI: 1S/C24H22N4O2/c1-27-13-17(15-7-2-4-9-19(15)27)21-22(24(30)26-23(21)29)18-14-28(12-6-11-25)20-10-5-3-8-16(18)20/h2-5,7-10,13-14H,6,11-12,25H2,1H3,(H,26,29,30)
• chave InChI: UQHKJRCFSLMWIA-UHFFFAOYSA-N

Descrição

Descrição geral

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 PKC_α, 195 nM for PKC_βI, 163 nM for PKC_βII, 213 nM for PKC_γ, and 175 nM for PKC_ε). Inhibits carbachol-evoked noradrenaline release (IC₅₀ = 600 nM).

A cell-permeable, reversible, selective protein kinase C (PKC) inhibitor that acts at the ATP binding site of PKC (IC₅₀ = 158 nM for rat brain PKC). Does not inhibit the tyrosine phosphorylation or the activation of phospholipase C_γ1 unlike staurosporine and other serine/threonine kinase inhibitors. IC₅₀ values for individual PKC isozymes are as follows: 53 nM for PKC_α, 195 nM for PKC_βI, 163 nM for PKC_βII, 213 nM for PKC_γ, and 175 nM for PKC_ε. Inhibits carbachol-evoked noradrenaline release (IC₅₀ = 0.6 µM).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
rat brain PKC

Product competes with ATP.

Reversible: yes

Target IC₅₀: 158 nM against rat brain PKC; 53 nM for PKCα, 195 nM for PKCβ, 163 nM for PKCβII, 213 nM for PKCγ, and 175 nM for PKCε

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following initial use, aliquot and refrigerate (4°C). Stock solutions are stable for up to 3 months at -20°C.

Outras notas

Zhang, C., et al. 1997. J. Immunol. 158, 4968.
Turner, N.A., et al. 1996. J. Neurochem. 66, 2381.
Ozawa, K., et al. 1993. J. Biol. Chem. 268, 1749.
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