产品说明
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 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.
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 |
产品性质
| 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 |
