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DCZ0415

Catalog No. T10981   CAS 2242470-43-3

DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.

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DCZ0415 Chemical Structure
DCZ0415, CAS 2242470-43-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 48.00
2 mg In stock $ 71.00
5 mg In stock $ 118.00
10 mg In stock $ 198.00
25 mg In stock $ 437.00
50 mg In stock $ 646.00
100 mg In stock $ 919.00
1 mL * 10 mM (in DMSO) In stock $ 128.00
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Purity: 99.1%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.
In vitro DCZ0415 (10, 20 μM; 72 hours) showed a marked reduction in colony formation, indicating that it inhibited cell proliferation. DCZ0415 (1.25-40 μM; 72 hours) caused a significant dose-dependent reduction in MM cell viability. DCZ0415 (10, 20 μM; 24-72 hours) showed a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death. DCZ0415 (10, 20 μM; 24 hours) induced massive accumulation in G0 / G1 MM cells. DCZ0415 (10 μM; 48 hours) can reduce the protein levels of phosphorylated (p) -iκBα and phosphorylated (p) -NF-κB in MM cells. The IC50 of DCZ0415 in CalcuSyn in MM cell line is 1.0–10 μM. DCZ0415 exerts a cytotoxic effect by inhibiting the synthesis of DNA 288 in MM cells.
In vivo DCZ0415, was confirmed to bind TRIP13 using pull-down, nuclear magnetic resonance spectroscopy, and surface plasmon resonance-binding assays.?DCZ0415 induced antimyeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant patients with myeloma.?The inhibitor impaired nonhomologous end joining repair and inhibited NF-κB activity.?Moreover, combining DCZ0415 with the multiple myeloma chemotherapeutic melphalan or the HDAC inhibitor panobinostat induced synergistic antimyeloma activity.?Therefore, targeting TRIP13 may be an effective therapeutic strategy for multiple myeloma, particularly refractory or relapsed multiple myeloma.
Molecular Weight 356.42
Formula C23H20N2O2
CAS No. 2242470-43-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (175.35 mM), sonification is recommended.

TargetMolReferences and Literature

1. Wang Y, et al. A Small Molecule Inhibitor Targeting TRIP13 suppresses multiple myeloma progression. Cancer Res. 2019 Nov 15. pii: canres.3987.2018.

TargetMolCitations

1. Chen Y, Chen D, Qin Y, et al. TRIP13, identified as a hub gene of tumor progression, is the target of microRNA-4693-5p and a potential therapeutic target for colorectal cancer. Cell Death Discovery. 2022, 8(1): 1-10.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Compound Library Transcription Factor-Targeted Compound Library Anti-Pancreatic Cancer Compound Library Anti-Ovarian Cancer Compound Library NO PAINS Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library Anti-Prostate Cancer Compound Library Bioactive Compounds Library Max Anti-Liver Cancer Compound Library

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Keywords

DCZ0415 2242470-43-3 Apoptosis NF-Κb Others NF-κB inhibit nonhomologous Nuclear factor-κB TRIP13 Inhibitor joining end drug-resistant DCZ-0415 myeloma repair anti-myeloma DCZ 0415 Nuclear factor-kappaB inhibitor

 

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