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Beschreibung

A cell-permeable naphthoquinolinedione compound that is reported to preferentially inhibit 23 kinases (IC50 <=10 µ,M) from a panel of 219, notably IRR (h), CLK2(h), Rsk1(h), Flt3(h), Rsk1(r), Rsk2(h), Haspin(h), Rsk4(h), Melk(h), Drak1(h), Rsk3(h), and CK13(h) (% inhibition by 10 µ,M BRD7389 = 91, 87, 86, 79, 78, 76, 74, 73, 73, 72, 71, and 71, respectively). Shown to induce beta-cell-like morphology in cultured murine pancreatic alpha-cell alphaTC1 and stimulate the expression of insulin mRNA (by ~50-fold, 0.85 µ,M for 5 d) and protein (by 1.5-fold, 3.4 µ,M for 5 d), as well as other beta-cell mRNAs, including Iapp, Npy, Pdx1, and Pax4, in alphaTC1 cultures. In human primary islets cultures, BRD7389 treatments result in a decrease of overall cell counts over time due to apoptosis induction, while insulin-positive population, and in some cases also glucagon-positive cell population, remains more or less unaffected.