2. Epigenetics TGF-beta/Smad
  3. PKC
  4. (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.

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(S)-Ro 32-0432 Chemical Structure

(S)-Ro 32-0432 Chemical Structure

CAS No. : 1781828-85-0

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Based on 1 publication(s) in Google Scholar

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(S)-Ro 32-0432 Related Antibodies

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Description

(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[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

(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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(S)-Ro 32-0432 Related Antibodies
In Vivo

(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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
SMILES

O=C(C(C1=C(C[C@@H](CN(C)C)CC2)N2C3=C1C=CC=C3)=C4C5=CN(C)C6=C5C=CC=C6)NC4=O.[H]Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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(S)-Ro 32-0432 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(S)-Ro 32-04321781828-85-0PKCProtein kinase CAnti-inflammatoryT-cellsATP-competitivePKCαIL-2anti-proliferationsystemicGRK5Inhibitorinhibitorinhibit

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