MF-438
SCD1 inhibitor / MF-438 is a potent inhibitor of stearoyl-CoA desaturase 1 (SCD1) - IC50 = 2.3 nM.1 MF-438 was potent in an in vivo mouse liver PD assay (ED50 between 1 and mg/kg).1 Cancer initiating cells (CSC-like) were shown to much more sensitive to MF-438 inhibition of SCD1 than progenitor and terminally differentiated cancer cells in a lung cancer model.2 MF-438 showed good oral bioavailability and metabolic stability making it an excellent tool for studying the effects of SCD1 in various disease models.
Biochemicals & reagents
921605-87-0
1) Leger et al., (2010), Synthesis and biological activity of a potent and orally bioavailable SCD inhibitor (MF-438); Bioorg.Med.Chem.Lett. 20 499 2) Noto et al. (2013), Stearoyl-CoA desaturase-1 is a key factor for lung cancer-initiating cells; Cell Death and Differ. 4 e947 3) Rodriguez-Perez et al. (2017) Altered fatty acid metabolism and reduced stearoyl coenzyme A desaturate activity in asthma; Allergy, 72 1744 [Citation]
-20°C
TARGET: ER/Golgi -- PATHWAY: Fatty acid metabolism; Lipid signaling -- RESEARCH AREA: Cancer stem cells; Neuroscience -- DISEASE AREA: Cancer; Neurodegeneration