Description
BRD7389 is an inhibitor of ribosomal S6 kinases (RSKs; IC
50s = 1.5, 2.4, and 1.2 μM for RSK1, RSK2, and RSK3, respectively). Through this action, BRD7389 causes mouse αTC1 pancreatic α cells to adopt several morphological and gene expression features of β cells, including increased insulin expression. BRD7389 also enhances glucose-stimulated insulin and glucagon secretion by pancreatic islet cells isolated from human donors with a low body mass index.
References
1) Fomina-Yadlin et al. (2010), Small molecule inducers of insulin expression in pancreatic alpha-cells; Proc. Natl. Acad. Sci. USA, 107 15099
2) Choudhary et al. (2014), Quantitative-proteomic comparison of alpha and Beta cells to uncover novel targets for lineage reprogramming; PLoS One, 9(4) e95194
3) Park and Cho (2012), EGFR and PKC are involved in the activation of ERK1/2 and p90 RSK and the subsequent proliferation of SNU-470 colon cancer cells by muscarinic acetylcholine receptors; Mol. Cell. Biochem., 370 191