产品描述:
DCLK1-IN-1 is an inhibitor of doublecortin-like kinase 1 (DCLK1; IC50 = 17 nM).{69699} It is selective for DCLK1 over leucine-rich repeat kinase 2 (LRRK2), bromodomain-containing protein 4 (BRD4), and ERK5 (IC50s = 7,000, >10,000, and 3,350 nM, respectively). DCLK1-IN-1 (1 µM) reduces the number of cells in primary patient-derived pancreatic cancer organoids. In vivo, DCLK1-IN-1 (10 mg/kg every other day) reduces plaque area and collagen levels in the aortic arches and serum levels of Tnf-α and Il-6 an ApoE-/- mouse model of atherosclerosis induced by a high-fat diet.{69700}