USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects^[1].

IC50: 1.4 μM (USP7)

USP7 or HAUSP (herpesvirus-associated USP) is a ubiquitin specific protease or a deubiquitylating enzyme that cleaves ubiquitin from its substrates. USP7 is a eubiquitinase (DUB) that controls cell proliferation by altering the stability of Mdm2, p53, PTEN and FOXO4^[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.

347.41

C₂₁H₂₁N₃O₂

2009273-60-1

Room temperature in continental US; may vary elsewhere.

DMSO : 83.33 mg/mL (239.86 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。

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    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.99 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.99 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.99 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.99 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Robert Blake, et al. Usp7 inhibitor compounds and methods of use. US20160272588A1.

USP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21^[1].

IC₅₀: 40.8 nM (USP7)^[1]

USP7-IN-9 (compound L55) (0-50 μM; 3 or 6 days) exhibits inhibitory activity against cancer cells^[1].
USP7-IN-9 (1 μM; 0-72 hours) reduces the proportions of G2/M cells, and does not change the proportions of G0/G1 and S cells^[1].
USP7-IN-9 (0.1-1 μM; 24 hours) reduces the protein levels of MDM2 and DNMT1 in a dose-dependent manner, and increases the protein levels of p53 and p21^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

779.08

C₃₂H₃₃ClF₆N₆O₈

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Li M, Liu S, Chen H, et al. N-benzylpiperidinol derivatives as novel USP7 inhibitors: Structure-activity relationships and X-ray crystallographic studies. Eur J Med Chem. 2020;199:112279.