USP7-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

USP7-IN-1  纯度: 98.92%

USP7-IN-1 是一种选择性的,可逆的泛素蛋白特异性蛋白酶 (USP7) 抑制剂,IC50 值为 77 μM,可用于癌症研究。

USP7-IN-1

USP7-IN-1 Chemical Structure

CAS No. : 1381291-36-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3280 In-stock
2 mg ¥2333 In-stock
5 mg ¥3500 In-stock
10 mg ¥5000 In-stock
50 mg ¥15000 In-stock
100 mg ¥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

USP7-IN-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Ubiquitination Compound Library

生物活性

USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.

IC50 & Target

IC50: 77 μM (USP7)[1]

体外研究
(In Vitro)

USP7-IN-1 (Example 2) is a selective and reversible inhibitor of USP7, with an IC50 of 77 μM, and shows no inhibition of USP8, USP5, Uch-L1, Uch-L3 or caspase 3. USP7-IN-1 inhibits the proliferation of HCT116 cells, with a GI50 of 67 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

425.91

Formula

C23H24ClN3O3

CAS 号

1381291-36-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 40 mg/mL (93.92 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3479 mL 11.7396 mL 23.4791 mL
5 mM 0.4696 mL 2.3479 mL 4.6958 mL
10 mM 0.2348 mL 1.1740 mL 2.3479 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. SELECTIVE AND REVERSIBLE INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 7. WO 2013030218 A1

Kinase Assay
[1]

USP7 is diluted in USP buffer (50 mM Tris HCl; 0.5 mM EDTA (Ethylenediaminetetraacetic acid); 5 mM DTT; 0.01 % Triton X-100; Bovine Serum Albumin 0.05 mg/mL pH7.6). Compounds stocks (10 mM) are stored at -20°C in DMSO. Compounds (including USP7-IN-1) are tested at different concentrations: from 200 μM to 91 nM. Reactions are performed as duplicates in Black 384 well plates (10 μL final reaction volume). The substrate concentration for USP7 is 300 nM Ub-AMC. The concentrations of the enzyme (USP7) in specificity assays is 100 pM. The concentrations are determined in order to perform specificity assays under initial velocities at fixed substrate concentration. Compounds are pre-incubated with enzymes for 30 minutes at 25°C. Reactions are initiated by addition of substrate to the plates containing the enzymes (+/- compounds) diluted in assay buffer. Reactions are incubated for 60 minutes at 37°C. Reactions are stopped by adding acetic acid (100 mM final). Readings are performed on a Pherastar Fluorescent Reader. λ Emission 380 nm; λ Excitation = 460 nm. Data (mean values +/- standard deviation) are analyzed as % of control (no compound) and plotted as percentage versus the Log of the compound concentration using GraphPad. Data are fitted to a sigmoidal model (variable slope)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

HCT116 colon cancer cells are maintained in Mc Coy’s 5A medium containing 10% FBS, 3 mM glutamine and 1 % penicillin/streptomycin. Cells are incubated at 37°C in a humidified atmosphere containing 5% CO2. Cell viability is assayed using the MTS technique in 96-well culture plates. MTS (3-(4,5-dimethyl-thiazol-2-yl)-5-(3-carboxy- methoxyphenyl)-2-(4-sulfophenyl)-2H-tetra-zolium) is a MTT-derived tetrazolium that is reduced in metabolically active cells into a soluble, cell-permeant formazan. The amount of formazan, detected by its absorbance at 492 nm is proportional to the number of living, metabolically active cells. 103 HCT116 cells are seeded per well. 24 hours later, the medium is changed and the cells treated in triplicate with the concentrations of each compound from 100 μM to 50 nM. The compounds (including USP7-IN-1) are diluted in 100% DMSO, whose final concentration on cells is kept at 0.5%. Cells are incubated with the compounds for 72 hours, and their viability then assayed by the addition of MTS for 2 hours. Absorbance at 492 nm is measured directly from the 96-well culture plates. GI50 (Growth Inhibition 50) concentrations for each compound are calculated using a sigmoidal variable slope fit. Values represent mean of three independent experiments[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. SELECTIVE AND REVERSIBLE INHIBITORS OF UBIQUITIN SPECIFIC PROTEASE 7. WO 2013030218 A1

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