2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs Deubiquitinase Apoptosis MDM-2/p53
  4. U7D-1

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells.

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

U7D-1 Chemical Structure

U7D-1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 2275 In-stock
Solution
10 mM * 1 mL in DMSO USD 2275 In-stock
Solid
1 mg USD 540 In-stock
5 mg USD 1350 In-stock
10 mg USD 2200 In-stock
25 mg USD 4400 In-stock
50 mg USD 7080 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

U7D-1 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP7 USP8 USP30 UCHL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells[1].

IC50 & Target[1]

USP7

 

In Vitro

U7D-1 (0-1 μM, 0-24 h) induced USP7 degradation in RS4;11 cell, reducing the USP7 protein level by 83.2% at 1 μM[1].
U7D-1 (0-20 μM, 3 days) shows anti-proliferative activity in p53 wild-type cell lines, and maintains potent cell growth inhibition in p53 mutant cancer cells[1].
U7D-1 (1 μM, 0-24 h) upregulates the level of p53 and p21 proteins in a time-dependent manner, and induces cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner[1].
U7D-1 (1 μM, 24 h) up-regulates the expression of apoptotic related genes and down-regulates the expression of E2F related genes in Jeko-1 cells[1].

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

U7D-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: RS4;11 cells
Concentration: 0, 5, 20, 50, 100, and 500 nM
Incubation Time: 24 h
Result: Induced USP7 degradation in RS4;11 cell in a dose dependent manner, with a DC50 (half-maximal degradation) value of 33 nM.

Cell Proliferation Assay[1]

Cell Line: p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines); p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM)
Concentration: 0-20 μM
Incubation Time: 3 days
Result: Showed antiproliferative activity in p53 wild-type cell lines (RS4;11, OCI-ly10, MV4;11, Reh and MOLT4 cell lines), and p53 mutant cell lines (Jeko-1 cells, Mino, RPMI-8226, Jurkat, SU-DHL-6, CCRF-CEM), with IC50 values for 3 days of 79.4, 227.0, 830.3, 1367.2, 4948.0, 1034.9, 1175.3, 1860.6, 6077.6, 9078.0, and 10675.0, respectively. Had an antiproliferative activity with an IC50 value of 53.5 nM in Jeko-1 cells for 7 days but exhibited a 13-fold loss in antiproliferative activity with an IC50 value of 727 nM in Jeko-1 CRBN KO cells.

Western Blot Analysis[1]

Cell Line: RS4;11 cells, Jeko-1 and Mino cell
Concentration: 1 μM
Incubation Time: 0, 2, 4, 6, 8, 10, 12, 20, 24, 36, 48, 60, and 72 h
Result: USP7 degradation in RS4;11 cells induced by U7D-1 started after 4 h of exposure and more effective degradation was observed after 8 h of exposure. Up-regulated the level of p53 and p21 proteins in RS4;11 cells in a time-dependent manner. Had no effect on the level of p53 protein in p53-mutant cell lines. Induced cleavage of caspase-3 in the Jeko-1 cell line in a time dependent manner.
Molecular Weight

940.14

Formula

C53H65N9O7
Appearance

Solid

Color

White to light yellow

SMILES

O=C1N(C(CC2)C(NC2=O)=O)C(C3=C1C=CC=C3NCCCCCCCCCCCNCC4=CC=C(C5=C(C6=NN5C)N=CN(CC7(O)CCN(C(C[C@H](C8=CC=CC=C8)C)=O)CC7)C6=O)C=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (106.37 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 1.0637 mL 5.3184 mL 10.6367 mL
5 mM 0.2127 mL 1.0637 mL 2.1273 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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. 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 1.0637 mL 5.3184 mL 10.6367 mL 26.5918 mL
5 mM 0.2127 mL 1.0637 mL 2.1273 mL 5.3184 mL
10 mM 0.1064 mL 0.5318 mL 1.0637 mL 2.6592 mL
15 mM 0.0709 mL 0.3546 mL 0.7091 mL 1.7728 mL
20 mM 0.0532 mL 0.2659 mL 0.5318 mL 1.3296 mL
25 mM 0.0425 mL 0.2127 mL 0.4255 mL 1.0637 mL
30 mM 0.0355 mL 0.1773 mL 0.3546 mL 0.8864 mL
40 mM 0.0266 mL 0.1330 mL 0.2659 mL 0.6648 mL
50 mM 0.0213 mL 0.1064 mL 0.2127 mL 0.5318 mL
60 mM 0.0177 mL 0.0886 mL 0.1773 mL 0.4432 mL
80 mM 0.0133 mL 0.0665 mL 0.1330 mL 0.3324 mL
100 mM 0.0106 mL 0.0532 mL 0.1064 mL 0.2659 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

U7D-1 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.

Keywords:

U7D-1PROTACsDeubiquitinaseApoptosisMDM-2/p53DUBsRS4;11OCI-ly10MV4;11RehMOLT4 cellJeko-1 cellsMinoRPMI-8226JurkatSU-DHL-6CCRF-CEMp53 mutant cancer cellsantiproliferativeJeko-1 CRBN KO cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
U7D-1
Cat. No.:
HY-148369
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.