产品属性：
产品名称 | 规格 | CAS号 | 型号 |
DC_AC50 | 1mg 5mg 10mg 25mg | 497061-48-0 | EY-Y0164667 |
Cas No.497061-48-0
别名 N/A
化学名 3-amino-N-(2-bromo-4,6-difluorophenyl)-6,7-dihydro-5H-cyclopenta[b]thieno[3,2-e]pyridine-2-carboxamide
分子式 C17H12BrF2N3OS
分子量 424.26
溶解度 DMSO: 10 mg/ml
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
DC_AC50 is a selective inhibitor of human copper-trafficking proteins Atox1 and CCS with Kd values of ～6.8 μM and ～8.2 μM [1].
Human copper-trafficking proteins Atox1 and CCS are cytosolic copper chaperones that transfer
copper to specific cellular destinations [1].
DC_AC50 is a selective inhibitor of human copper-trafficking proteins Atox1 and CCS. DC_AC50 is a self-fluorescing compound with excitations at 290 nm and 355 nm, and emission at 494 nm. In FRET assay, DC_AC50 bound to Atox1 and full-length CCS with Kd values of ～6.8 μM and 8.2 μM. In fluorescence anisotropy (FA) assay, DC_AC50 bound to Atox1, full-length CCS and CCS domain I with Kd values of 6.4 μM, 7.9 μM and 12.2 μM. In human lung cancer H1299 cells, leukaemia cancer K562 cells, breast cancer MDA-MB-231 cells and head and neck cancer 212LN cells, DC_AC50 dose-dependently inhibited cancer cell proliferation by targeting Atox1 and CCS. DC_AC50 also induced reactive oxygen species (ROS) accumulation, reduced cellular ATP production and decreases lipid biosynthesis via AMP-activated protein kinase (AMPK) activation [1].
In nude mice bearing lung cancer H1299 cells or leukaemia cancer K562 cells, DC_AC50 (100 mg/kg per day for 21 days) significantly decreased tumour size compared with vehicle control. In K562 mice model, DC_AC50 (10, 20 and 50 mg/kg per day) also induced a similar tumor-inhibition effects without any obvious toxicity or a change in body weight [1].
Reference:
[1]. Wang J, Luo C, Shan CL, et al. Inhibition of human copper trafficking by a small molecule significantly attenuates cancer cell proliferation. Nature Chemistry, 2015, published online 09 November 2015.
