KL-001
Cryptochrome (CRY) activator / A novel tool that specifically interacts with cryptochrome (CRY) preventing its ubiquitin-dependent degradation resulting in lengthening of the circadian period. KL-001-mediated CRY stabilization inhibits glucagon-induced gluconeogenesis in primary hepatocytes1. Binds to the FAD-binding pocket of CRY2 as determined by co-crystal structure2. Induces an increase in period along with simultaneous reduction in amplitude of circadian reporter expression3 in mammalian cells.
Biochemicals & reagents
309928-48-1
1) Hirota et al. (2012), Identification of small molecule activators of cryptochrome; Science, 337 1094 2) Nangle et al. (2013), Crystal structure of mammalian cryptochrome in complex with a small molecule competitor of its ubiquitin ligase; Cell Res., 23 1417 3) St. John et al. (2014), Spatiotemporal separation of PER and CRY posttranslational regulation in the mammalian circadian clock; Proc. Natl. Acad. Sci. USA, 11 2040
RT
PATHWAY: Degradation -- RESEARCH AREA: Circadian clock; Ubiquitin/Proteasome