| Bioactivity | KL001 is a first-in-class cryptochrome (CRY, a flavoproteins that are sensitive to blue light, and is involved in the circadian rhythms of plants and animals) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis[1][2][3]. |
| Invitro | KL001 (0.03-71 μM) causes circadian period lengthening and amplitude reduction in a dose-dependent manner in stable U2OS reporter cell lines harboring Bmal1-dLuc or Per2-dLuc[1].KL001 (2-8 μM; 18 h) represses glucagon-dependent induction of Pck1 and G6pc genes in a dose-dependent manner without affecting their basal expression in mouse primary hepatocytes[1]. |
| Name | KL001 |
| CAS | 309928-48-1 |
| Formula | C21H22N2O4S |
| Molar Mass | 398.48 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Hirota T, et, al. Identification of small molecule activators of cryptochrome. Science. 2012 Aug 31;337(6098):1094-7. [2]. Kelleher FC, et, al. Circadian molecular clocks and cancer. Cancer Lett. 2014 Jan 1;342(1):9-18. [3]. Nangle S, et, al. Crystal structure of mammalian cryptochrome in complex with a small molecule competitor of its ubiquitin ligase. Cell Res. 2013 Dec;23(12):1417-9. |