Ro 32-0432 hydrochloride

Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. It 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 treatment.

Product information

CAS Number: 1781828-85-0

Molecular Weight: 489.01

Formula: C28H29ClN4O2

Synonym:

Ro 32-0432 hydrochloride

Chemical Name:  (S)-3-(8-((dimethylamino)methyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride

Smiles: Cl.CN(C)C[C@@H]1CC2=C(C3=CC=CC=C3N2CC1)C1=C(C2=CN(C)C3=CC=CC=C32)C(=O)NC1=O

InChiKey: HSPRASOZRZDELU-LMOVPXPDSA-N

InChi: InChI=1S/C28H28N4O2.ClH/c1-30(2)15-17-12-13-32-22-11-7-5-9-19(22)24(23(32)14-17)26-25(27(33)29-28(26)34)20-16-31(3)21-10-6-4-8-18(20)21;/h4-11,16-17H,12-15H2,1-3H3,(H,29,33,34);1H/t17-;/m0./s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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.

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.

References:

1. Birchall AM, Bishop J, Bradshaw D, et al. Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation. J Pharmacol Exp Ther. 1994;268(2):922-929.
2. Singh TG, Rehni AK, Arora S. Ro 32-0432 attenuates mecamylamine-precipitated nicotine withdrawal syndrome in mice. Naunyn Schmiedebergs Arch Pharmacol. 2013;386(3):197-204. doi:10.1007/s00210-012-0825-0.

Products are for research use only. Not for human use.