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 In Vitro DCZ0415 (10, 20 μM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation. DCZ0415 (1.25-40 μM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells. DCZ0415 (10, 20 μM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death. DCZ0415 (10, 20 μM; 24 hours) induces a significant accumulation in G0/G1 MM cells. DCZ0415 (10 μM; 48 hours) decreases the protein levels of phosphorylated (p)-iκBα and phosphorylated (p)-NF-κB in MM cells. DCZ0415 has IC 50 s of 1.0–10 μM in CalcuSyn in MM cell lines. DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AssayCell 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 AnalysisCell 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 AnalysisCell Line: MM cells Concentration: 10 and 20 μM Incubation Time: 24 hours Result: Induced a significant accumulation in G0/G1 MM cells. Western Blot AnalysisCell 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 . 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 Dosage: 50 mg/kg Administration: Intraperitoneal injection; every day for 14 days Result: Significantly reduced the growth of MM cells-induced tumors. IC50& Target:NF-κB

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