Biological Activity:
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.
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Reference:
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