DCZ0415

2242470-43-3

356.42

DMSO : 62.5 mg/mL (175.35 mM; Need ultrasonic)

Apoptosis; NF-kappaB

DCZ0415, a potent TRIP13 inhibitor, impairs nonhomologous end joining repair and inhibits NF-kappaB activity. DCZ0415 induces anti-myeloma activity in vitro, in vivo, and in primary cells derived from drug-resistant myeloma patients^[1]. IC50 & Target: TRIP13; NF-kappaB^[1] In Vitro: DCZ0415 (10, 20 uM; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cell proliferation^[1].
DCZ0415 (1.25-40 uM; 72 hours) induces a significant dose-dependent decrease of viability in MM cells^[1].
DCZ0415 (10, 20 uM; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment and apoptotic cell death^[1].
DCZ0415 (10, 20 uM; 24 hours) induces a significant accumulation in G0/G1 MM cells^[1].
DCZ0415 (10 uM; 48 hours) decreases the protein levels of phosphorylated (p)-ikappaBalpha and phosphorylated (p)-NF-kappaB in MM cells^[1].
DCZ0415 has IC₅₀s of 1.0-10 uM in CalcuSyn in MM cell lines^[1].
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells^[1].
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].