(S)-Ro 32-0432
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of (S)-Ro 32-0432 for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. (S)-Ro 32-0432 is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. (S)-Ro 32-0432 prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
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- CAS No.: 1781828-85-0
- Formule: C28H29ClN4O2
- Masse moléculaire:489.01
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
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PKCα 9.3 nM (IC50) |
PKC-βI 28 nM (IC50) |
PKC-βII 30 nM (IC50) |
PKCγ 36.5 nM (IC50) |
PKCε 108.3 nM (IC50) |
G protein-coupled receptor kinase 5 (GRK5) |
In Vitro
(S)-Ro 32-0432 inhibits interleukin-2 (IL-2) secretion, IL-2 receptor expression in, and proliferation of, peripheral human T-cells stimulated with phorbol ester together with phytohemagglutin or anti-CD3, but does not inhibit IL-2 induced proliferation in cells already stimulated to express IL-2 receptors. Proliferation of the influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) after exposure to antigen-pulsed autologous presenting cells is also inhibited by (S)-Ro 32-0432. (S)-Ro 32-0432 inhibits HA27 proliferation with an IC50 of 0.15 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female AHH/R rats (200-250 g) induced with phorbol ester[1]
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Dosage:10 mg/kg, 30 mg/kg, 50 mg/kg
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Administration:Oral administration; once
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Result:Inhibited subsequent phorbol ester-induced edema in rats.
Chemical Information
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CAS No. 1781828-85-0
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Masse moléculaire 489.01
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Formule C28H29ClN4O2
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SMILES
O=C(C(C1=C(C[C@@H](CN(C)C)CC2)N2C3=C1C=CC=C3)=C4C5=CN(C)C6=C5C=CC=C6)NC4=O.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
[1]. A M Birchall, et al. Ro 32-0432, a Selective and Orally Active Inhibitor of Protein Kinase C Prevents T-cell Activation. J Pharmacol Exp Ther. 1994 Feb;268(2):922-9. [Content Brief]
[2]. Thakur Gurjeet Singh, et al. Ro 32-0432 Attenuates Mecamylamine-Precipitated Nicotine Withdrawal Syndrome in Mice. Naunyn Schmiedebergs Arch Pharmacol. 2013 Mar;386(3):197-204. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-Ro 32-0432 Related Classifications
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