1. Cell Cycle/DNA Damage Apoptosis
  2. Deubiquitinase Apoptosis
  3. USP7-IN-9

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.

For research use only. We do not sell to patients.

USP7-IN-9 Chemical Structure

USP7-IN-9 Chemical Structure

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Based on 1 publication(s) in Google Scholar

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Description

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 & Target

IC50: 40.8 nM (USP7)[1]

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: LNCaP, RS4; 11, HCT 116, NB4, K562 and HuH-7 cells[1]
Concentration: 0-50 μM
Incubation Time: LNCaP, 6 days; RS4; 11, HCT 116, HuH-7, K562 and NB4, 3 days
Result: Exhibited high inhibitory activity against LNCaP and RS4; 11 cells, with IC50s of 29.6 nM and 41.6 nM, respectively, and weak inhibitory activity on HCT 116, NB4, K562 and HuH-7 cells.

Cell Cycle Analysis

Cell Line: RS4; 11 cells[1]
Concentration: 1 μM
Incubation Time: 0, 24, 48 and 72 hours
Result: Reduced the proportions of G2/M cells, while the proportions of G0/G1 and S cells were not apparently altered.

Western Blot Analysis

Cell Line: RS4; 11 cells[1]
Concentration: 0.1, 0.3 and 1 μM
Incubation Time: 24 hours
Result: Reduced the protein levels of MDM2 and DNMT1 in a dose-dependent manner, and increased the protein levels of p53 and p21.
Molecular Weight

779.08

Formula

C32H33ClF6N6O8

Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1(CN(C=NC2=C(C3=CC=C(C[NH3+])C=C3)N(C)N=C24)C4=O)CC[NH+](CC5=CC=C(C(OC)=O)C=C5Cl)CC1.O=C([O-])C(F)(F)F.O=C([O-])C(F)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (128.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2836 mL 6.4178 mL 12.8357 mL
5 mM 0.2567 mL 1.2836 mL 2.5671 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2836 mL 6.4178 mL 12.8357 mL 32.0891 mL
5 mM 0.2567 mL 1.2836 mL 2.5671 mL 6.4178 mL
10 mM 0.1284 mL 0.6418 mL 1.2836 mL 3.2089 mL
15 mM 0.0856 mL 0.4279 mL 0.8557 mL 2.1393 mL
20 mM 0.0642 mL 0.3209 mL 0.6418 mL 1.6045 mL
25 mM 0.0513 mL 0.2567 mL 0.5134 mL 1.2836 mL
30 mM 0.0428 mL 0.2139 mL 0.4279 mL 1.0696 mL
40 mM 0.0321 mL 0.1604 mL 0.3209 mL 0.8022 mL
50 mM 0.0257 mL 0.1284 mL 0.2567 mL 0.6418 mL
60 mM 0.0214 mL 0.1070 mL 0.2139 mL 0.5348 mL
80 mM 0.0160 mL 0.0802 mL 0.1604 mL 0.4011 mL
100 mM 0.0128 mL 0.0642 mL 0.1284 mL 0.3209 mL
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USP7-IN-9 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
USP7-IN-9
Cat. No.:
HY-146887
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