1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Ro 32-0432 hydrochloride

Ro 32-0432 hydrochloride 

Cat. No.: HY-108601A
Handling Instructions

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.

For research use only. We do not sell to patients.

Ro 32-0432 hydrochloride Chemical Structure

Ro 32-0432 hydrochloride Chemical Structure

CAS No. : 1781828-85-0

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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].

IC50 & Target[1][2]

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.
Molecular Weight

489.01

Formula

C₂₈H₂₉ClN₄O₂

CAS No.

1781828-85-0

SMILES

O=C(C(C1=C(C[[email protected]@H](CN(C)C)CC2)N2C3=C1C=CC=C3)=C4C5=CN(C)C6=C5C=CC=C6)NC4=O.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Ro 32-0432PKCProtein kinase CAnti-inflammatoryT-cellsATP-competitivePKCαIL-2anti-proliferationsystemicGRK5Inhibitorinhibitorinhibit

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