FT827
目录号 : GC32917
FT827是选择性和共价的泛素特异性蛋白酶7(USP7)抑制剂，IC50值为52nM。
Cas No.:1959537-86-0
Sample solution is provided at 25 µL, 10mM.
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FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 52 nM.
FT827 features a vinylsulfonamide moiety that covalently modifies the catalytic Cys223 of USP7 and inhibits the enzyme with Ki and Kd of 7.8 and 4.2 μM, respectively. FT827 exclusively inhibit USP7 in a panel of 38 deubiquitinases (DUBs) from diverse families. FT827 inhibits USP7 probe reactivity with IC50s of 0.1-2 µM, confirming 10 to 100-fold higher potency as compared to P22077 in crude cell extracts or with intact MCF7 breast cancer cells, followed by incubation with the ubiquitin active site suicide probe haemagglutinin (HA)-tagged ubiquitin bromoethyl (HA-UbC2Br)[1].
[1]. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486.
Kinase experiment: | To determine compound IC50s, FT827 is diluted in 100% DMSO in three-fold 12- point dilution series from 100 µM. 100 nL of 100-fold concentrated solutions are dispensed into black 384-well plate. 25 nM ubiquitin-rhodamine 110, along with recombinant USP7CD (3 nM), or USP7C-term (30-125 pM, depending on batch activity) are added and the plates incubated at room temperature for 1 h. The reaction is terminated by adding 2.5 µL citric acid to a final concentration of 10 mM prior to measuring fluorescence intensity on a Pherastar with a 485 nm excitation/520 nm emission optic module[1]. |
References: [1]. Turnbull AP, et al. Molecular basis of USP7 inhibition by selective small-molecule inhibitors. Nature. 2017 Oct 26;550(7677):481-486. | |
| Cas No. | 1959537-86-0 | SDF | |
| Canonical SMILES | C=CS(=O)(NC1=CC=CC=C1C2=CC=C(C(N3CCC(O)(CN(C=NC4=C5C=NN4C)C5=O)CC3)=O)C=C2)=O | ||
| 分子式 | C27H28N6O5S | 分子量 | 548.61 |
| 溶解度 | DMSO : 125 mg/mL (227.85 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8228 mL | 9.1139 mL | 18.2279 mL |
| 5 mM | 0.3646 mL | 1.8228 mL | 3.6456 mL |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8228 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet