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|233624-25MG||Glass bottle||25 mg||
|Overview||A cell-permeable carbazole compound that competes against FAD (flavin adenine dinucleotide) for cryptocrome (CRY) 1 & 2 binding, displaying little affinity toward other clock proteins (PER1/2, CLOCK, or BMAL1) or inhibitory activity against casein kinase (CKIα, CKIδ, and CK2) activity even at concentrations as high as 100 µM. Shown to selectively stabilize cellular CRY1/2 protein, but not mRNA, by preventing FBXL3-mediated CRY1/2 ubiquitination and proteasomal degradation, effectively lengthening the period and reducing the amplitude of the circadian transcription rhythms of Bmal1 and Per2 promoter-mediated transcription activity (IC50 of intensity reduction = 14 and 0.82 µM, respectively, in U2OS reporter assay). KL001 is also reported to block glucagon-induced Pck1 and G6pc mRNA upregulation as well as glucose production in primary murine hepatocyte cultures (IC50 <8 µM). Longdaysin (Cat. No. 438075), in comparison, exerts its circadian perturbation activity via casein kinase inhibition.|
|Synonyms||CRY Activator, KL001, N-(3-(9H-Carbazol-9-yl)-2-hydroxypropyl)-N-(furan-2-ylmethyl)methanesulfonamide|
|References||Hirota, T., et al. 2012. Science 337, 1094.|
|Structure formula Image|
|Primary Target||Cryptocrome protein|
|Purity||≥98% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
|Hirota, T., et al. 2012. Science 337, 1094.|
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