DCZ0415 是一种有效的 TRIP13 抑制剂，可损害非同源末端连接修复并抑制 NF-κB 活性。DCZ0415 在体外，体内以及在耐药性骨髓瘤患者衍生的原代细胞中诱导抗骨髓瘤活性。

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.

Solid

NF-κB

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 inMM 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 IC50s of 1.0–10 μM in CalcuSyn in MM cell lines.
DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells.
has not independently confirmed the accuracy of these methods. They are for reference only.

DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

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

In Vitro: DMSO : 62.5 mg/mL (175.35 mM; Need ultrasonic)配制储备液