Longdaysin

Longdaysin is an inhibitor of casein kinase 1δ (CK1δ) and CK1α (IC₅₀ = 12 µM for both).¹ It also inhibits cyclin-dependent kinase 2 (Cdk2), Cdk7, MAPK, and MAP3K (IC50s = 13, 32, 59, and 92 µM, respectively). Longdaysin increases the circadian period of U2OS cells by one and five hours when used at concentrations of 0.39 and 3.4 µM, respectively.² It inhibits Wnt-signaling induced by Wnt3A-containing conditioned medium in HEK293 cells and reduces levels of active β-catenin in HEK293 cells expressing CK1δ or CK1ε. Longdaysin (10 and 25 µM) reduces colony formation, as well as cell migration and invasion, by Hs 578T and MDA-MB-231 breast cancer cells. In vivo, longdaysin (5 mg/kg) reduces tumor volume in an MDA-MB-231 mouse xenograft model.

WARNING This product is not for human or veterinary use.

1. Lee, J.W., Hirota, T., Ono, D., et al. Chemical control of mammalian circadian behavior through dual inhibition of casein kinase Iα and δ. J. Med. Chem. 62(4), 1989-1998 (2019).

2. Bedair, M., and El Rassi, Z. Affinity chromatography with monolithic capillary columns I. Polymethacrylate monoliths with immobilized mannan for the separation of mannose-binding proteins by capillary electrochromatography and nano-scale liquid chromatography. J. Chromatogr. A 1044(1-2), 177-186 (2004).