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

DCZ0415 

Cat. No.: HY-130603
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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.

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

DCZ0415 Chemical Structure

DCZ0415 Chemical Structure

CAS No. : 2242470-43-3

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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

 

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].

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].

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.

2242470-43-3

SMILES

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

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DCZ0415DCZ 0415DCZ-0415NF-κBApoptosisNuclear factor-κBNuclear factor-kappaBTRIP13nonhomologousendjoiningrepairanti-myelomadrug-resistantmyelomaInhibitorinhibitorinhibit

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