Potent and specific inhibitor of protein kinase C (PKC) with Ki at subnanomolar to low nanomolar range for a variety of PKC isotypes while selective for >200 other kinases; an immunosuppressant that blocks early T-lymphocyte (T-cell) activation via protein kinase C inhibition.
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. [online]
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. [online]
M McCall et al. Sotrastaurin. Drugs Fut. 2009, 34(8), 618-623. [online]
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. [online]
H Skvara et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J. Clin. Invest. 2008, 118(9), 3151–3159. [online]
Chemical Name: 3-(1H-indol-3-yl)-4-(2-(4-methylpiperazin-1-yl)quinazolin-4-yl)-1H-pyrrole-2,5-dione
