| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C28H29ClN4O2 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
(S)-Ro 32-0432 is a potent, selective, ATP-competitive and orally active PKC inhibitor, with IC50 values of 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM against PKCα, PKCβI, PKCβII, PKCγ and PKCε, respectively. It also selectively inhibits G protein-coupled receptor kinase 5 (GRK5) and prevents T-cell activation, giving it potential for chronic inflammatory and autoimmune disease research[1][2].
It has the molecular formula C28H29ClN4O2 and a molecular weight of 489.01 g/mol.
Physical & Chemical Properties
| CAS Number | 1781828-85-0 |
|---|---|
| Molecular Formula | C28H29ClN4O2 |
| Molecular Weight | 489.01 g/mol |
| 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 |
| Target | PKCα, PKC-βI, PKC-βII, PKCγ, PKCε, G protein-coupled receptor kinase 5 (GRK5) |
| Signaling Pathway | Epigenetics; TGF-beta/Smad |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
(S)-Ro 32-0432 suppresses secretion of interleukin-2 (IL-2), expression of the IL-2 receptor, and proliferation in peripheral human T-cells stimulated with phorbol ester plus phytohemagglutinin or anti-CD3, yet it does not suppress IL-2 induced proliferation in cells already stimulated to express IL-2 receptors. (S)-Ro 32-0432 also inhibits proliferation of the influenza peptide antigen HA 307-319-specific human T-cell clone (HA27) following exposure to antigen-pulsed autologous presenting cells. The IC50 of (S)-Ro 32-0432 for HA27 proliferation is 0.15 μM[1].
In Vivo
In female AHH/R rats, (S)-Ro 32-0432 (10-50 mg/kg; oral administration; once) treatment inhibits subsequent phorbol ester-induced edema, demonstrating systemic efficacy of the compound against PKC-driven responses. Ro 32-0432 also inhibits more physiologically T-cell driven responses, such as host vs. graft responses and secondary paw swelling in adjuvant-induced arthritis[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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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