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Bisindolylmaleimide XI hydrochloride

CAS No. : 145333-02-4

MCE 站：Bisindolylmaleimide XI hydrochloride

产品活性：Bisindolylmaleimide XI hydrochloride (Ro 32-0432) 是一种有效、选择性和具有口服活性的 PKC 抑制剂，对 PKCα、PKCβI、PKCβII、PKCγ 的 IC₅₀ 分别为 9 nM、28 nM、31 nM、37 nM 和 108 nM。

研究领域：Epigenetics  |  TGF-beta/Smad

作用靶点：PKC

In Vitro: Bisindolylmaleimide XI hydrochloride (Ro 32-0432) inhibits 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 Bisindolylmaleimide XI hydrochloride.
PKC inhibition with Bisindolylmaleimide XI hydrochloride (Ro 32-0432; 1 μM) decreases the proportion of apoptotic cells (-21%) in retinal progenitor cells (RPCs).

In Vivo: Oral administration of Bisindolylmaleimide XI hydrochloride inhibits subsequent phorbol ester-induced edema in ratss. 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 Bisindolylmaleimide XI hydrochloride.

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