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DC_AC50 Sale

目录号 : GC15206

An inhibitor of Atox1 and CCS

DC_AC50 Chemical Structure

Cas No.:497061-48-0

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1mg
¥150.00
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5mg
¥765.00
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10mg
¥1,170.00
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25mg
¥2,250.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

Cas No. 497061-48-0 SDF
化学名 3-amino-N-(2-bromo-4,6-difluorophenyl)-6,7-dihydro-5H-cyclopenta[b]thieno[3,2-e]pyridine-2-carboxamide
Canonical SMILES NC1=C(C(NC2=C(C=C(F)C=C2Br)F)=O)SC3=NC4=C(CCC4)C=C31
分子式 C17H12BrF2N3OS 分子量 424.26
溶解度 DMSO: 10 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.357 mL 11.7852 mL 23.5705 mL
5 mM 0.4714 mL 2.357 mL 4.7141 mL
10 mM 0.2357 mL 1.1785 mL 2.357 mL
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