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Ro 32-0432 hydrochloride

Potent, orally active PKC inhibitor CAS# 151342-35-7

Ro 32-0432 hydrochloride

Catalog No. BCC7122----Order now to get a substantial discount!

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Chemical structure

Ro 32-0432 hydrochloride

3D structure

Chemical Properties of Ro 32-0432 hydrochloride

Cas No. 151342-35-7 SDF Download SDF
PubChem ID 127757 Appearance Powder
Formula C28H28N4O2 M.Wt 452.5
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in DMSO with gentle warming
Chemical Name 3-[(8S)-8-[(dimethylamino)methyl]-6,7,8,9-tetrahydropyrido[1,2-a]indol-10-yl]-4-(1-methylindol-3-yl)pyrrole-2,5-dione
SMILES CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C5CC(CCN5C6=CC=CC=C64)CN(C)C
Standard InChIKey FXGHOAZJQNLNFD-KRWDZBQOSA-N
Standard InChI InChI=1S/C28H28N4O2/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)/t17-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Ro 32-0432 hydrochloride

DescriptionSelective cell-permeable protein kinase C inhibitor. Displays slight selectivity for conventional PKC isoforms over Ca2+ and atypical PKC isoforms; binding affinities for rat isoforms are 9, 28, 31, 37 and 108 nM for PKC's α, βΙ, βΙΙ, γ and ε respectively. Orally available and prevents T cell chronic inflammation in vivo.

Ro 32-0432 hydrochloride Dilution Calculator

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Ro 32-0432 hydrochloride Molarity Calculator

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Preparing Stock Solutions of Ro 32-0432 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2099 mL 11.0497 mL 22.0994 mL 44.1989 mL 55.2486 mL
5 mM 0.442 mL 2.2099 mL 4.4199 mL 8.8398 mL 11.0497 mL
10 mM 0.221 mL 1.105 mL 2.2099 mL 4.4199 mL 5.5249 mL
50 mM 0.0442 mL 0.221 mL 0.442 mL 0.884 mL 1.105 mL
100 mM 0.0221 mL 0.1105 mL 0.221 mL 0.442 mL 0.5525 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Ro 32-0432 hydrochloride

Ro 32-0432, a selective and orally active inhibitor of protein kinase C prevents T-cell activation.[Pubmed:8114006]

J Pharmacol Exp Ther. 1994 Feb;268(2):922-9.

Several lines of circumstantial evidence support the assumption that protein kinase C (PKC) activation together with elevated levels of cytosolic Ca++ are necessary for T-cell activation and proliferation in response to a physiological stimulus, i.e., MHC class II restricted antigen presentation. By using a potent, cell-permeable and selective inhibitor of PKC, Ro 32-0432, we have tested this hypothesis. 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 was also inhibited by Ro 32-0432. Oral administration of Ro 32-0432 inhibited 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 were also inhibited by Ro 32-0432. These data demonstrate the crucial role for PKC in T-cell activation and that selective p.o. bioavailable PKC inhibitors are efficacious in preventing T-cell driven chronic inflammatory responses in vivo. Inhibition of PKC represents an important mechanistic approach to prevent T-cell activation and compounds of this class may have important therapeutic applicability to chronic inflammatory and autoimmune diseases.

Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.[Pubmed:8373348]

Biochem J. 1993 Sep 1;294 ( Pt 2):335-7.

The protein kinase C (PKC) family of isoenzymes is believed to mediate a wide range of signal-transduction pathways in many different cell types. A series of bisindolylmaleimides have been evaluated as inhibitors of members of the conventional PKC family (PKCs-alpha, -beta, -gamma) and of a representative of the new, Ca(2+)-independent, PKC family, PKC-epsilon. In contrast with the indolocarbazole staurosporine, all the bisindolylmaleimides investigated showed slight selectivity for PKC-alpha over the other isoenzymes examined. In addition, bisindolylmaleimides bearing a conformationally restricted side-chain were less active as inhibitors of PKC-epsilon. Most noticeable of these was Ro 32-0432, which showed a 10-fold selectivity for PKC-alpha and a 4-fold selectivity for PKC-beta I over PKC-epsilon.

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