- Batimastat (BB-94)
- CTS-1027
| DC_AC50Selective Atox1 and CCS inhibitor |

Sample solution is provided at 25 µL, 10mM.
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Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure


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| Cas No. | 497061-48-0 | SDF | Download SDF |
| Chemical Name | 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 | ||
| Formula | C17H12BrF2N3OS | M.Wt | 424.26 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For 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. | ||
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.
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现在有一个实验需要看一种药物与受体的结合情况,想咨询一下放射性配体受体结合实验,因为我们不具备这个实验条件,最好能外包那种
大多数药物在体内都是和特异性受体相互作用,改变细胞的生理生化功能而产生效应。目前已经确定的受体有30多种,根据受体存在的标准,受体可大致分为三类:
1.细胞膜受体:位于靶细胞膜上,如胆碱受体、肾上腺素受体、多巴胺受体、阿片受体等。
2.胞浆受体:位于靶细胞的胞浆内,如肾上腺皮质激素受体、性激素受体。
3.胞核受体:位于靶细胞的细胞核内,如甲状腺素受体。
另外也可根据受体的蛋白结构、信息转导过程、效应性质、受体位置等特点将受体分为四类:
1.含离子通道的受体(离子带受体):如N-型乙酰胆碱受体含钠离子通道。
2.G蛋白偶联受体:M-乙酰胆碱受体、肾上腺素受体等。
3.具有酪氨酸激酶活性的受体:如胰岛素受体。
4.调节基因表达的受体(核受体):如甾体激素受体、甲状腺激素受体等。
有些受体具有亚型,各种受体都有特定的分布部位核特定的功能,有些细胞也有多种受体。

