(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^[1][2].

(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.

(S)-Ro 32-0432 (10-50 mg/kg; oral administration; once; female AHH/R rats) treatment inhibits subsequent phorbol ester-induced edema in rats demonstrating the systemic efficacy of the compound to inhibit PKC-driven responses. Induction of more physiologically T-cell driven responses such as host vs. graft responses and the secondary paw swelling in adjuvant-induced arthritis are also inhibited by Ro 32-0432^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

489.01

C₂₈H₂₉ClN₄O₂

1781828-85-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]