Insulin Expression Inducer, BRD7389

A cell-permeable naphthoquinolinedione compound that is reported to preferentially inhibit 23 kinases (IC₅₀ ≤10 µM) 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 µM BRD7389 = 91, 87, 86, 79, 78, 76, 74, 73, 73, 72, 71, and 71, respectively). Shown to induce β-cell-like morphology in cultured murine pancreatic α-cell αTC1 and stimulate the expression of insulin mRNA (by ~50-fold; 0.85 µM for 5 d) and protein (by 1.5-fold; 3.4 µM for 5 d), as well as other β-cell mRNAs, including Iapp, Npy, Pdx1, and Pax4, in αTC1 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.

Packaged under inert gas

Following recontitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Fomina-Yadlin, D., et al. 2010. Proc. Natl. Acad. Sci. USA107, 15099.

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Toxicity: Regulatory Review (Z)