302939-48-6
中文名稱
化合物KL201
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
化合物KL201 英文別名
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
所屬類別
醫(yī)藥中間體：雜環(huán)化合物常見問題列表
生物活性
KL201 是一種晝夜節(jié)律調(diào)制器，是一種同種型選擇性隱花色素 1 (CRY1) 穩(wěn)定劑。KL201 對 CRY2 沒有穩(wěn)定作用。KL201 延長了細(xì)胞和組織中的晝夜節(jié)律周期。體外研究
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.