1781828-85-0
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PKCα 9.3 nM (IC 50 ) |
PKC-βI 28 nM (IC 50 ) |
PKC-βII 30 nM (IC 50 ) |
PKCγ 36.5 nM (IC 50 ) |
PKCε 108.3 nM (IC 50 ) |
G protein-coupled receptor kinase 5 (GRK5)
|
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 Ro 32-0432. Ro 32-0432 inhibits HA27 proliferation with an IC 50 of 0.15 μM.
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.
Animal Model: | Female AHH/R rats (200-250 g) induced with phorbol ester |
Dosage: | 10 mg/kg, 30 mg/kg, 50 mg/kg |
Administration: | Oral administration; once |
Result: | Inhibited subsequent phorbol ester-induced edema in rats. |