KL201 causes dose-dependent lengthening of circadian period in Bmal1-dLuc reporter cells, and in cells with another circadian reporter Per2-dLuc. KL201 suppresses the intensity of Per2-dLuc reporter much more than that of Bmal1-dLuc, without affecting cellular viability[1]. KL201 binds to CRY1 in overlap with FBXL3, a subunit of ubiquitin ligase complex, and the effect of KL201 is blunted by knockdown of FBXL3[1]. KL201 lengthened circadian period and suppressed the intensity of Per2::Luc knockin reporter in mouse lung primary explants[1].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Simon Miller, et al. An Isoform-Selective Modulator of Cryptochrome 1 Regulates Circadian Rhythms in Mammals. Cell Chem Biol. 2020 Sep 17;27(9):1192-1198.e5.
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