Cryptocrome Activator, KL001

半岛bd体育手机客户端 说明

一般描述

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 ?M. 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 ofBmal1andPer2promoter-mediated transcription activity (IC₅₀of intensity reduction = 14 and 0.82 ?M, respectively, in U2OS reporter assay). KL001 is also reported to block glucagon-inducedPck1andG6pcmRNA upregulation as well as glucose production in primary murine hepatocyte cultures (IC₅₀<8 ?M). Longdaysin (Cat. No. 438075), in comparison, exerts its circadian perturbation activity via casein kinase inhibition.

包装

25 mg in Glass bottle
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
Cryptocrome protein
Reversible: yes

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Hirota, T., et al. 2012.Science337,1094.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式	C21H22N2O4S
分子量	398.48
MDL编号	MFCD02086647

半岛bd体育手机客户端 性质

质量水平	100
测定	≥98% (HPLC)
形式	solid
manufacturer/tradename	Calbiochem?
储存条件	OK to freeze protect from light
颜色	off-white
溶解性	DMSO: 50 mg/mL
运输	ambient
储存温度	2-8℃
SMILES string	OC(CN(CC1=CC=CO1)S(=O)(C)=O)CN2C3=C(C=CC=C3)C4=C2C=CC=C4

安全信息

象形图
警示用语：	Warning
危险声明	H302
预防措施声明	P264 - P270 - P301 + P312 - P501
危险分类	Acute Tox. 4 Oral
储存分类代码	11 - Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable