GlpBio

FT827

目录号: GC32917纯度: >98.50%
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。
FT827
Cas No.: 1959537-86-0
规格价格库存数量操作
5mg¥6,694.00现货
1
10mg¥10,710.00现货
1
25mg¥21,420.00现货
1
50mg¥34,808.00现货
1
100mg¥52,658.00现货
1
10mM (in 1mL DMSO)¥8,079.00现货
1
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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
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    641, 529–536 (2025)
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    610, 366–372 (2022)
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
1959537-86-0
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 g/mol
溶解性
DMSO : 125 mg/mL (227.85 mM)
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol