2. Cell Cycle/DNA Damage
  3. Deubiquitinase
  4. IMP-2373

IMP-2373 is a low-toxicity activity-based probe targeting covalent pan-deubiquitinase (DUB), which modulates and monitors DUB activity via covalent binding to the catalytic cysteine and active site of DUB. IMP-2373 enables real-time tracking of dynamic intracellular DUB activity in physiologically relevant living cell systems, and quantitative analysis of activity changes induced by pharmacological inhibition or MYC dysregulation. IMP-2373 can be used for research on related diseases such as B-cell lymphoma.

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

IMP-2373

IMP-2373 Chemical Structure

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IMP-2373 Related Antibodies

Top Publications Citing Use of Products

View All Deubiquitinase Isoform Specific Products:

View All Isoforms
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15 USP28 USP25

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  • Purity & Documentation

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Description

IMP-2373 is a low-toxicity activity-based probe targeting covalent pan-deubiquitinase (DUB), which modulates and monitors DUB activity via covalent binding to the catalytic cysteine and active site of DUB. IMP-2373 enables real-time tracking of dynamic intracellular DUB activity in physiologically relevant living cell systems, and quantitative analysis of activity changes induced by pharmacological inhibition or MYC dysregulation. IMP-2373 can be used for research on related diseases such as B-cell lymphoma[1][2].

In Vitro

IMP-2373 (8 h; 24 h) shows no cytotoxicity against T47D, U2OS and U87-MG cells after 8 h of treatment, and exhibits only extremely low cytotoxicity after 24 h of treatment, with EC50 values all higher than 60 μM in these three cell lines[1].
IMP-2373 (10 μM; 1 h) is a competitive probe that selectively and efficiently detects the target engagement of intracellular active DUB inhibitors, including the UCHL1 inhibitor IMP-1711-S and the USP30 inhibitor FT385, in U87-MG and T47D cells[1].
IMP-2373 (25 μM; 1 h) captures the activity of 38 deubiquitinases in P493-6 B-cell lymphoma cells, and reveals that dysregulation of oncogenic MYC drives global downregulation of DUB activity, which is independent of DUB abundance. Meanwhile, the activities of UCHL3, USP7, USP47, USP10 and ATXN3 are selectively upregulated in low-MYC cells[1].
IMP-2373 exhibits extremely low off-target cytotoxicity: no reduction in cell viability is observed after treatment with >100 μM for 8 h in T47D and U2OS cells; no reduction in cell viability is detected either after treatment with 95.4 μM for 8 h in U87-MG cells; additionally, the 24 h EC50 values range from 8.9 μM (U87-MG) to 86.5 μM (T47D)[2].
IMP-2373 (10 μM; 1 h) acts as a competitive probe for the quantitative detection of intracellular target engagement corresponding to selective DUB inhibitors (UCHL1 and USP30 inhibitors) in U87-MG and T47D cells, respectively[2].
Analysis of DUB activity changes in P493-6 B cell lymphoma cells treated with IMP-2373 (25 μM; 1 h) shows that global DUB activity is lower in high MYC cells, while UCHL3, USP7, USP47, USP10 and ATXN3 exhibit significantly higher activity relative to their abundance in low MYC cells[2].

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

IMP-2373 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T cells overexpressing FLAG-tagged wild-type (UCHL1, USP30, USP7, OTUB1) and active site Cys-to-Ser mutant DUBs
Concentration: 0, 10, 25 μM
Incubation Time: 1 h
Result: Selectively engaged the catalytic cysteine of wild-type UCHL1, USP30, USP7, and OTUB1.
Showed no engagement with the corresponding active site Cys-to-Ser mutant DUBs.

Cell Cytotoxicity Assay[2]

Cell Line: T47D breast cancer cells, U2OS osteosarcoma cells, U87-MG glioblastoma cells
Concentration: >100 μM; 95.4 μM; 86.5 μM; 60.4 μM; 8.9 μM
Incubation Time: 8 h (T47D/U2OS/U87-MG); 24 h (T47D/U2OS/U87-MG)
Result: Did not affect cell viability after 8 h treatment at concentrations >100 μM in T47D and U2OS cells, and at 95.4 μM in U87-MG cells.
Showed minimal cytotoxicity after 24 h treatment, with EC50 values of 86.5 μM (T47D), 60.4 μM (U2OS), and 8.9 μM (U87-MG).
Molecular Weight

360.41

Formula

C21H20N4O2
Appearance

Solid

Color

White to off-white

SMILES

C#CC1=CC=C(CNC(C2=CC(C(C3CN(C#N)CC3)=O)=CN2C)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (277.46 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 2.7746 mL 13.8731 mL 27.7462 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 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 (protect from light). 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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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
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 (protect from light). 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 2.7746 mL 13.8731 mL 27.7462 mL 69.3654 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 mL 13.8731 mL
10 mM 0.2775 mL 1.3873 mL 2.7746 mL 6.9365 mL
15 mM 0.1850 mL 0.9249 mL 1.8497 mL 4.6244 mL
20 mM 0.1387 mL 0.6937 mL 1.3873 mL 3.4683 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7746 mL
30 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
40 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7341 mL
50 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
60 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
100 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
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IMP-2373 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:

IMP-2373IMP2373IMP 2373DeubiquitinaseDUBsdeubiquitinaseHEK293T cellsUSP30U87-MG cellsP493-6 B cell lymphoma cellsMYCT47D cellsUCHL1catalytic cysteineU2OS cellsInhibitorinhibitorinhibit

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