USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC₅₀s of 0.42 μM and 1.0 μM, respectively.

EC50: 0.42 μM (USP7), 1.0 μM (USP47)^[1]

USP7/USP47 inhibitor (compound 14) is a selective inhibitor of USP7/USP47 with EC₅₀s of 0.42 μM and 1 μM, respectively. USP7/USP47 inhibitor does not inhibit caspase 3, calpain 1, 20S proteasome, and a panel of representative USPs (USP2, USP5, USP8, USP21, and USP28; EC₅₀ > 31.6 μM). USP7/USP47 inhibitor inhibits the growth of HCT-116 cells with an EC₅₀ of 7.6 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.

484.40

C₁₈H₁₁Cl₂N₃O₃S₃

1247825-37-1

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (103.22 mM; Need ultrasonic)

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Weinstock J, et al. Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47. ACS Med Chem Lett. 2012 Sep 11;3(10):789-92.

The cloning, expression and purification of USP21 from BL21 (DE3) bacteria are performed using standard molecular biology techniques. USP2, USP5, USP7, USP8, USP28, USP47, Ub-PLA2 (Ub-CHOP) and Ub-EKL (Ub-CHOP2) are generated. Caspase 3 and the caspase 3 substrate DEVD-Rh110 are used. Deubiquitylating enzyme, cathepsin B and 20S proteasome chymotrypsin like protease activities are measured. Caspase 3 activity is determined using a similar protocol. Briefly, dose ranges of compound (including USP7/USP47 inhibitor) are incubated with caspase 3 for 30 minutes before the addition of DEVD-Rh110 and reading on a fluorometric plate reader using excitation and emission maxima of 485 nm and 531 nm respectively. The final concentrations of caspase 3 and DEVD-Rh110 are 2 nM and 100 nM respectively^[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.

• [1]. Weinstock J, et al. Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47. ACS Med Chem Lett. 2012 Sep 11;3(10):789-92.