1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. USP28-IN-4

USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331).

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

USP28-IN-4 Chemical Structure

USP28-IN-4 Chemical Structure

CAS No. : 2931509-15-6

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Description

USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331)[1].

IC50 & Target[1]

USP28

0.04 μM (IC50)

In Vitro

USP28-IN-4 (compound 9p) (12.5 μM, 15 μM; 3 d) inhibits colony formation of human colorectal cancer cells HCT116 (15 μM) and Ls174T (12.5 μM)[1].
USP28-IN-4 (20-80 μM; 24 h) down-regulates the level of c-Myc by enhancing its degradation via ubiquitin-proteasome system (UPS)[1].

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

Western Blot Analysis[1]

Cell Line: Human colorectal cancer cells HCT116 and Ls174T
Concentration: 20 μM, 30 μM, 50 μM, and 60 μM, for Ls174T; 30 μM, 50 μM, 60 μM and 80 μM for HCT116
Incubation Time: 24 h
Result: Dose-dependently down-regulated the cellular level of c-Myc.
Molecular Weight

461.36

Formula

C22H18Cl2N2O3S

CAS No.
Appearance

Solid

Color

White to light brown

SMILES

CS(=O)(C1=CC=C(C(Cl)=C1)C(NC2=CC=C(C(C3=CC4=C(CNC4)C=C3)=C2)Cl)=O)=O

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 : 10 mg/mL (21.68 mM; ultrasonic and warming and adjust pH to 2 with 1 M HCL and heat to 60°C; 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 2.1675 mL 10.8375 mL 21.6750 mL
5 mM 0.4335 mL 2.1675 mL 4.3350 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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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.35%

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 2.1675 mL 10.8375 mL 21.6750 mL 54.1876 mL
5 mM 0.4335 mL 2.1675 mL 4.3350 mL 10.8375 mL
10 mM 0.2168 mL 1.0838 mL 2.1675 mL 5.4188 mL
15 mM 0.1445 mL 0.7225 mL 1.4450 mL 3.6125 mL
20 mM 0.1084 mL 0.5419 mL 1.0838 mL 2.7094 mL
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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:
USP28-IN-4
Cat. No.:
HY-149230
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