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.

• Sinonimo/i: Ro-31-7549, Monohydrate, 2-[1-3(Aminopropyl)indol-3-yl]-3(1-methyl-1H-indol-3-yl)maleimide, Acetate, Bisindolylmaleimide VIII, Acetate
• Formula empirica (notazione di Hill): C₂₄H₂₂N₄O₂ · xC₂H₄O₂ · yH₂O
• Numero CAS: 125313-65-7
• Peso molecolare: 398.46 (anhydrous free base basis)
• Numero MDL: MFCD00886999
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥93% (HPLC)
• Stato: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: red to red-orange
• Solubilità: DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: N1C(=O)C(=C(C1=O)c4c5c([n](c4)C)cccc5)c2c3c([n](c2)CCCN)cccc3
• 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); UQHKJRCFSLMWIA-UHFFFAOYSA-N

Descrizione

Descrizione generale

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).

Azioni biochim/fisiol

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

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

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