921605-87-0

MF-438 (921605-87-0) 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 3 mg/kg).1?Cancer initiating cells (CSC-like) were shown to be 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.

MF-438 is a potent and orally bioavailable stearoyl-CoA desaturase 1 (SCD1) inhibitor with an IC50 of 2.3 nM for rSCD1[1].

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 desaturase activity in asthma; Allergy,?72?1744 [Citation]