302939-48-6
中文名称
化合物KL201
英文名称
2-bromo-N-(5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-yl)benzamide
CAS
302939-48-6
分子式
C17H14BrN3OS
分子量
388.28
MOL 文件
302939-48-6.mol
302939-48-6 结构式
基本信息
中文别名
化合物KL201 英文别名
KL2012-bromo-N-(5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d]pyrimidin-4-yl)benzamide
Benzamide, 2-bromo-N-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)-
KL201,CRY1,Inhibitor,Per2-dLuc,FBXL3,inhibit,clock,KL 201,circadian,cryptochrome,KL-201
所属类别
医药中间体：杂环化合物常见问题列表
生物活性
KL201 是一种昼夜节律调制器，是一种同种型选择性隐花色素 1 (CRY1) 稳定剂。KL201 对 CRY2 没有稳定作用。KL201 延长了细胞和组织中的昼夜节律周期。体外研究
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.
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.
KL201 lengthened circadian period and suppressed the intensity of
Per2::Luc
knockin reporter in mouse lung primary explants.