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DC_AC50

Catalog No.
B5981
Selective Atox1 and CCS inhibitor
Grouped product items
SizePriceStock Qty
5mg
$231.00
In stock
25mg
$924.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

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.

Chemical Properties

StorageStore at 2-8°C
M.Wt424.26
Cas No.497061-48-0
FormulaC17H12BrF2N3OS
SolubilitySoluble in DMSO
Chemical Name3-amino-N-(2-bromo-4,6-difluorophenyl)-6,7-dihydro-5H-cyclopenta[b]thieno[3,2-e]pyridine-2-carboxamide
SDFDownload SDF
Canonical SMILESNC1=C(C(NC2=C(C=C(F)C=C2Br)F)=O)SC3=NC4=C(CCC4)C=C31
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

DC_AC50