KL001 is a novel and specific small molecule activator of cryptochrome (CRY) identified from an unbiased cell-based circadian screen (in human osteosarcoma U2OS cell line harboring a Bmal1-dLuc luciferase reporter). KL001 prevented ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. In addition, KL001-mediated CRY stabilization inhibited glucagon-induced gluconeogenesis in primary hepatocytes. Therefore, KL001 serves as a useful tool to study the regulation of CRY-dependent physiology and may help development of clock-based therapeutics for treating diabetes.

How to Use:

• In vitro:  KL001 was used at 10-50 µM in vitro and in cellular assays.
• In vivo: n/a

Reference:

• 1.  Hirota T, et al. Identification of Small Molecule Activators of Cryptochrome. (2012) Science 337(6098):1094-7.