2. Cell Cycle/DNA Damage Apoptosis
  3. Deubiquitinase Apoptosis
  4. DC-U4106

DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer.

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

DC-U4106 Chemical Structure

DC-U4106 Chemical Structure

CAS No. : 2410534-62-0

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Based on 1 publication(s) in Google Scholar

DC-U4106 Related Antibodies

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Description

DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer[1].

IC50 & Target

Kd: 4.7 μM (USP8), IC50: 1.2 μM (USP8)[1].
In Vitro

DC-U4106 (1.2-45.2 μM) inhibits USP8 and USP2 with the IC50 values of 1.2 μM and 58.4 μM, respectively, and no activity in USP7[1].
DC-U4106 (0-7 μM, 24 hours) reduces mRNA levels of ERα and PR[1].
DC-U4106 (0-5 μM, 24 hours) can regulate the RTK pathway related proteins and the expression of ERα and PR proteins[1].
DC-U4106 (0-5 μM, 12 hours) can induce apoptosis and inhibit cell proliferation[1].

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

DC-U4106 Related Antibodies

Western Blot Analysis[1]

Cell Line: USP8-positive cell line MCF-7
Concentration: 0-5 μM
Incubation Time: 24 hours
Result: Reduced the expression of EGFR, ErbB2, and ErbB3 proteins with increasing concentrations and caused degradation of ERα and PR proteins.

RT-PCR[1]

Cell Line: USP8-positive cell line MCF-7
Concentration: 0-7 μM
Incubation Time: 24 hours
Result: Reduced mRNA levels of ERα and PR.

Cell Proliferation Assay[1]

Cell Line: USP8-positive cell line MCF-7
Concentration: 0-5 μM
Incubation Time:
Result: Inhibited cell growth in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: USP8-positive cell line MCF-7
Concentration: 0-5 μM
Incubation Time: 12 hours
Result: Resulted in increasing in the proportion of apoptotic cells with increasing concentrations.
In Vivo

DC-U4106 (intraperitoneal injection, 5 mg/kg or 20 mg/kg, every 2 days, 14 days) inhibits the proliferation of tumors and no significantly effects on body weight, organ morphology and structure in BALB/c nude mice[1].

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

Animal Model: BALB/c nude mice[1]
Dosage: 5 mg/kg , 20 mg/kg
Administration: Intraperitoneal injection, Every 2 days, 14 days
Result: Inhibited tumor growth significantly at a concentration of 20 mg/kg.
Molecular Weight

525.56

Formula

C29H27N5O5
CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

O=C1C=C(C2=CC=C(N3CCN(C4=NC=CC=C4)CC3)C=C2)OC5=C1C(O)=CC(O)=C5OC6=C(C)NN=C6C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility
In Vitro: 

THF : 10 mg/mL (19.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9027 mL 9.5137 mL 19.0273 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 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 and 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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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 and 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
THF 1 mM 1.9027 mL 9.5137 mL 19.0273 mL 47.5683 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 mL 9.5137 mL
10 mM 0.1903 mL 0.9514 mL 1.9027 mL 4.7568 mL
15 mM 0.1268 mL 0.6342 mL 1.2685 mL 3.1712 mL
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DC-U4106 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:

DC-U41062410534-62-0DeubiquitinaseApoptosisDUBsUSP8-targeting inhibitorubiquitin pathwayErαbreast cancerInhibitorinhibitorinhibit

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