1. Cell Cycle/DNA Damage Apoptosis
  2. Deubiquitinase Apoptosis
  3. 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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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.

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: 

DMSO : 25 mg/mL (47.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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 / DMSO 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
DMSO 20 mM 0.0951 mL 0.4757 mL 0.9514 mL 2.3784 mL
25 mM 0.0761 mL 0.3805 mL 0.7611 mL 1.9027 mL
30 mM 0.0634 mL 0.3171 mL 0.6342 mL 1.5856 mL
40 mM 0.0476 mL 0.2378 mL 0.4757 mL 1.1892 mL
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  • 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:
DC-U4106
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HY-150505
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