الصفحة الرئيسية>>Signaling Pathways>> TGF-β / Smad Signaling>> PKC>>(S)-Ro 32-0432

(S)-Ro 32-0432

رقم الكتالوجGC70295

(S)-Ro 32-0432 هو مثبط قوي، انتقائي، ATP تنافسي و نشط فمويا PKC.

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(S)-Ro 32-0432 التركيب الكيميائي

Cas No.: 1781828-85-0

الحجم السعر المخزون الكميّة
1 mg
535٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (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.

(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].

(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].

References:
[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.
[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.

Chemical Properties of (S)-Ro 32-0432

Cas No. 1781828-85-0 SDF
Formula C28H29ClN4O2 M.Wt 489.01
الذوبان Storage
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (S)-Ro 32-0432

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1 mg 5 mg 10 mg
1 mM 2.0449 mL 10.2247 mL 20.4495 mL
5 mM 0.409 mL 2.0449 mL 4.0899 mL
10 mM 0.2045 mL 1.0225 mL 2.0449 mL
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