DCZ0415

SKU: orb1309781

Description

DCZ0415 is a potent and selective TRIP13 inhibitor that demonstrates antimyeloma activity in vitro and in vivo, including in primary cells from drug-resistant patients. It functions by impairing non-homologous end joining repair and suppressing NF-κB signaling, making it a valuable tool for cancer research, particularly in studying myeloma pathogenesis and therapy resistance mechanisms.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 2242470-43-3
• MW: 356.42
• Purity: 99.95% (May vary between batches)
• Formula: C₂₃H₂₀N₂O₂
• SMILES: O=C1C2C(C3C=CC2C2CC32)C(=O)N1c1ccc(Cc2ccncc2)cc1
• Target: Apoptosis,NF-κB
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.61 mM);DMSO:62.5 mg/mL (175.35 mM)

Bioactivity

• 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.
• In Vitro:
  DCZ0415 demonstrated significant anti-proliferative effects: it reduced colony formation at 10-20 μM (72 hours), decreased MM cell viability in a dose-dependent manner at 1.25-40 μM (72 hours), increased apoptotic cell death at 10-20 μM (24-72 hours), induced G0/G1 cell cycle arrest at 10-20 μM (24 hours), and reduced protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB at 10 μM (48 hours). The IC50 in MM cell lines was 1.0–10 μM, and DCZ0415 exerted cytotoxicity by inhibiting DNA synthesis in MM cells.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

repair, TRIP13, end, DCZ 0415, DCZ0415, DCZ-0415, Inhibitor, myeloma, inhibit, joining, nonhomologous, NFkB, NF-kB, NFκB, NF-κB, Nuclear factor-κB, Nuclear factor-kappaB, drug-resistant, Apoptosis, anti-myeloma

Compound Identifiers

PubChem CID

145925662