1781828-85-0
1781828-85-0 structure
- Name: Ro 32-0432 hydrochloride
- Chemical Name: Ro 32-0432 hydrochloride
- CAS Number: 1781828-85-0
- Molecular Formula: C28H29ClN4O2
- Molecular Weight: 489.01
- Catalog: Signaling Pathways Epigenetics PKC
- Create Date: 2020-08-07 15:13:11
- Modify Date: 2024-01-13 17:01:54
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Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research[1][2].
| Name | Ro 32-0432 hydrochloride |
|---|
| Description | Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research[1][2]. |
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| Related Catalog | |
| Target |
PKCα:9.3 nM (IC50) PKC-βI:28 nM (IC50) PKC-βII:30 nM (IC50) PKCγ:36.5 nM (IC50) PKCε:108.3 nM (IC50) G protein-coupled receptor kinase 5 (GRK5) |
| 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[1]. |
| 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[1]. Animal Model: Female AHH/R rats (200-250 g) induced with phorbol ester[1] Dosage: 10 mg/kg, 30 mg/kg, 50 mg/kg Administration: Oral administration; once Result: Inhibited subsequent phorbol ester-induced edema in rats. |
| References |
| Molecular Formula | C28H29ClN4O2 |
|---|---|
| Molecular Weight | 489.01 |