557525

Ro-32-0432

A selective cell-permeable protein kinase C inhibitor.

• Synonim(y): Ro-32-0432, 2-{8-[(Dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl}-3-(1-methyl-1H-indol-3-yl)maleimide, HCl, Bisindolylmaleimide XI, HCl, 3-(8-((dimethylamino)methyl)-6,7,8,9-tetrahydropyrido[1,2- a]indol-10-y1)-4-(1-methyl-1 H-indol-3
• Wzór empiryczny (zapis Hilla): C₂₈H₂₈N₄O₂ · xHCl
• Numer CAS: 145333-02-4
• Masa cząsteczkowa: 452.55 (free base basis)
• MDL number: MFCD01319127
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: red
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: Cl.[n]21c3c(cc2CC(CC1)CN(C)C)ccc(c3)C4=C(C(=O)NC4=O)c5c6c([n](c5)C)cccc6
• InChI: 1S/C28H28N4O2.ClH/c1-30(2)15-17-10-11-32-20(12-17)13-18-8-9-19(14-24(18)32)25-26(28(34)29-27(25)33)22-16-31(3)23-7-5-4-6-21(22)23;/h4-9,13-14,16-17H,10-12,15H2,1-3H3,(H,29,33,34);1H
• InChI key: WMVQGKBSNAIMHI-UHFFFAOYSA-N

Opis

General description

A selective cell-permeable protein kinase C inhibitor. Displays about 10-fold greater selectivity for PKC_α (IC₅₀ = 9 nM) and 4-fold greater selectivity for PKC_βI (IC₅₀ = 28 nM) over PKC_ε (IC₅₀ = 108 nM). Also prevents T cell-driven chronic inflammatory responses in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PKCα

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 9 nM, 28 nM, 108 nM, against PKCα, PKCβI, and PKCε, respectively

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 4 months at -20°C.

Other Notes

Birchall, A.M., et al. 1994. J. Pharmacol. Exp. Ther.268, 922.
Wilkinson, S.E., et al. 1993. Biochem. J.294, 335.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• wgk: WGK 3