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Ro 32-0432 hydrochloride

CAS No. : 1781828-85-0

MCE 站：Ro 32-0432 hydrochloride

产品活性：Ro 32-0432 hydrochloride 是一种有效的，选择性的，ATP 竞争性和具有口服活性的 PKC 抑制剂，对 PKCα，PKCβI，PKCβII，PKCγ 和 PKCε 的 IC₅₀ 值分别为 9.3 nM，28 nM，30 nM，36.5 nM 和 108.3 nM。Ro 32-0432 hydrochloride 也是一种选择性 GRK5 的抑制剂。Ro 32-0432 hydrochloride 可防止 T 细胞活化，并可用于慢性炎症和自身免疫性疾病的研究。

研究领域：Epigenetics  |  TGF-beta/Smad

作用靶点：PKC

In Vitro: 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 IC₅₀ of 0.15 μM.

In Vivo: 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.

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