Description
BRD7389 is an inhibitor of ribosomal S6 kinases (RSKs; IC50s = 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.
Uses
BRD7389 is a specific RSK family kinase inhibitor with IC50s of 1.5 μM, 2.4 μM, and 1.2 μM for RSK1, RSK2, and RSK3, respectively. BRD7389 is a small-molecule inducer of insulin expression in pancreatic α-cells[1].
Definition
ChEBI: LSM-4550 is a member of anthracenes.
IC 50
RSK1: 1.5 μM (IC50); RSK2: 2.4 μM (IC50); RSK3: 1.2 μM (IC50); CDK5/p35: 6.5 μM (IC50); DRAK1: 2.8 μM (IC50); FLT3: 3.5 μM (IC50); PIM1: 3.7 μM (IC50); PKG1α: 6.5 μM (IC50); SGK: 13.8 μM (IC50)
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
