1. NF-κB Apoptosis
  2. NF-κB Apoptosis
  3. DCZ0415

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients.

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DCZ0415

DCZ0415 Chemical Structure

CAS No. : 2242470-43-3

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Based on 5 publication(s) in Google Scholar

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Description

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-κB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients[1].

IC50 & Target[1]

NF-κB

 

Cellular Effect
Cell Line Type Value Description References
NCI-H929 IC50
6.88 μM
Compound: DCZ0415
Anti-proliferative activity against human NCI-H929 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
Anti-proliferative activity against human NCI-H929 cells assessed as cell growth inhibition incubated for 72 hrs by CCK-8 assay
[PMID: 39083980]
In Vitro

DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation[1].
DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells[1].
DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death[1].
DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells[1].
DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells[1].
DCZ0415 has IC50s of 1.0–10 μM in CalcuSyn in MM cell lines[1].
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells[1].

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

Cell Proliferation Assay[1]

Cell Line: Multiple myeloma (MM) cells
Concentration: 10, 20 μM
Incubation Time: 72 hours
Result: Showed a significant decrease in colony formation, indicating it inhibits cell proliferation.

Cell Viability Assay[1]

Cell Line: MM cells
Concentration: 1.25, 2.5, 5, 10, 20, 40 μM
Incubation Time: 72 hours
Result: Induced a significant dose-dependent decrease of viability.

Apoptosis Analysis[1]

Cell Line: MM cells
Concentration: 10, 20 μM
Incubation Time: 24, 48, 72 hours
Result: Showed a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death.

Cell Cycle Analysis[1]

Cell Line: MM cells
Concentration: 10 and 20 μM
Incubation Time: 24 hours
Result: Induced a significant accumulation in G0/G1 MM cells.

Western Blot Analysis[1]

Cell Line: MM cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Decreased the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells.
In Vivo

DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice[1].

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

Animal Model: Nude mice (6-weeks-old) with H929 775 cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; every day for 14 days
Result: Significantly reduced the growth of MM cells-induced tumors.
Molecular Weight

356.42

Formula

C23H20N2O2

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C1N(C2=CC=C(CC3=CC=NC=C3)C=C2)C(C4C5C(C6)C6C(C=C5)C14)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (175.35 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 2.8057 mL 14.0284 mL 28.0568 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.81%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8057 mL 14.0284 mL 28.0568 mL 70.1420 mL
5 mM 0.5611 mL 2.8057 mL 5.6114 mL 14.0284 mL
10 mM 0.2806 mL 1.4028 mL 2.8057 mL 7.0142 mL
15 mM 0.1870 mL 0.9352 mL 1.8705 mL 4.6761 mL
20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5071 mL
25 mM 0.1122 mL 0.5611 mL 1.1223 mL 2.8057 mL
30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3381 mL
40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 mL
80 mM 0.0351 mL 0.1754 mL 0.3507 mL 0.8768 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7014 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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DCZ0415
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