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Sotrastaurin
- AEB071 - NVP-AEB071
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C25H22N6O2
- MW: 438.48
Description
Sotrastaurin (AEB071) is a potent protein kinase C inhibitor with subnanomolar to low-nanomolar reported Ki values across several PKC isoforms.
PKC isoforms regulate T-cell activation, cytokine production, proliferation and signaling downstream of antigen receptors. Sotrastaurin is useful for studying PKC-dependent immune activation, transplantation pharmacology and inflammatory disease mechanisms.
Key Features
- Potent inhibitor of multiple PKC isoforms
- Subnanomolar to low-nanomolar Ki values reported for several PKC targets
- Blocks T-cell activation and immune signaling pathways
- Relevant to transplantation and autoimmune pharmacology research
Applications
- PKC kinase assays
- T-cell activation and cytokine signaling studies
- Transplantation immunology models
- Autoimmune and inflammatory pathway research
More Information
| Parent CAS No. | 425637-18-9 |
|---|---|
| Chemical Name | 3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione |
| SMILES | O=C1NC(=O)C(C2=CNC3=CC=CC=C23)=C1C1=NC(N2CCN(C)CC2)=NC2C=CC=CC1=2 |
| MFCD | N.A. |
| InChi | InChI=1S/C25H22N6O2/c1-30-10-12-31(13-11-30)25-27-19-9-5-3-7-16(19)22(28-25)21-20(23(32)29-24(21)33)17-14-26-18-8-4-2-6-15(17)18/h2-9,14,26H,10-13H2,1H3,(H,29,32,33) |
| InChiKey | OAVGBZOFDPFGPJ-UHFFFAOYSA-N |
| CID | 10296883 |
| Short Description | PKC inhibitor |
References
- G Weckbecker et al. Effects of the novel protein kinase C inhibitor AEB071 (Sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or FTY720. Transplant Int. 2010, 23(5), 543-552.
- K Budde et al. Sotrastaurin, a novel small molecule inhibiting protein kinase C: first clinical results in renal-transplant recipients. Am. J. Transplant. 2010, 10(3), 571-581.
- M McCall et al. Sotrastaurin. Drugs Fut. 2009, 34(8), 618-623.
- JP Evenou et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J. Pharm. Exp. Ther. 2009, 330(3), 792-801.
- H Skvara et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J. Clin. Invest. 2008, 118(9), 3151–3159.
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