557514

Ro-31-8425

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

• Synonyme(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
• Formule empirique (notation de Hill) : C₂₆H₂₄N₄O₂ · xHCl
• Numéro CAS: 131848-97-0
• Poids moléculaire : 424.49 (free base basis)
• MDL number: MFCD00906977
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥94% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propriétés

• Quality Segment: 100
• assay: ≥94% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: red to orange-red
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: [n]21c3c(c(c2CC(CC1)CN)C4=C(C(=O)NC4=O)c5c6c([n](c5)C)cccc6)cccc3
• 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)
• InChI key: QQKKPWJFHBFCTH-UHFFFAOYSA-N

Description

General description

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.

Biochem/physiol Actions

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

Preparation Note

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

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

Informations sur la sécurité

• Classe de stockage: 11 - Combustible Solids
• WGK: WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable