DCZ0415-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDCZ0415Cat. No.: HY-130603CAS No.: 2242470-43-3分式: CHNO分量: 356.42作靶点: NF-B; Apoptosis作通路: NF-B; Apoptosis储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 DCZ0415种有效的 TRIP13 抑制剂，可损害同

2、末端连接修复并抑制 NF-B 活性。DCZ0415 在体外，体内以及在耐药性髓瘤患者衍的原代细胞中诱导抗髓瘤活性。IC50 & Target NF-B体外研究DCZ0415 (10, 20 M; 72 hours) shows a significant decrease in colony formation, indicating it inhibits cellproliferation 1.DCZ0415 (1.25-40 M; 72 hours) induces a significant dose-dependent decrease in viabilityMM cells 1.

3、DCZ0415 (10, 20 M; 24-72 hours) shows a dose-dependent relationship between DCZ0415 treatment andapoptotic cell death 1.DCZ0415 (10 and 20 M; 24 hours) induces a significant accumulation in G0/G1 MM cells 1.DCZ0415 (10 M; 48 hours) decreases the protein levels of phosphorylated (p)-iB and phosphoryl

4、ated (p)-NF-B in MM cells 1.DCZ0415 has IC50s of 1.010 M in CalcuSyn in MM cell lines 1.DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells 1.Cell Proliferation Assay 1Cell Line: Multiple myeloma (MM) cellsConcentration: 10, 20 MIncubation Time: 72 hours1/3 Master of Small M

5、olecules 您边的抑制剂师www.MedChemEResult: Showed a significant decrease in colony formation, indicating it inhibits cell proliferation.Cell Viability Assay 1Cell Line: MM cellsConcentration: 1.25, 2.5, 5, 10, 20, 40 MIncubation Time: 72 hoursResult: Induced a significant dose-dependent decrease in viabili

6、ty.Apoptosis Analysis 1Cell Line: MM cellsConcentration: 10, 20 MIncubation Time: 24, 48, 72 hoursResult: Showed a dose-dependent relationship between DCZ0415 treatment and apoptotic celldeath.Cell Cycle Analysis 1Cell Line: MM cellsConcentration: 10 and 20 MIncubation Time: 24 hoursResult: Induced

7、a significant accumulation in G0/G1 MM cells.Western Blot Analysis 1Cell Line: MM cellsConcentration: 10 MIncubation Time: 48 hoursResult: Decreased the protein levels of phosphorylated (p)-iB and phosphorylated (p)-NF-B inMM cells.体内研究DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the

8、 growth of MM cells-induced tumors inimmune-deficient mice 1.Animal Model: Nude mice (6-weeks-old) with H929 775 cells 12/3 Master of Small Molecules 您边的抑制剂师www.MedChemEDosage: 50 mg/kgAdministration: Intraperitoneal injection; every day for 14 daysResult: Significantly reduced the growth of MM cells-induced tumors.REFERENCES1. Wang Y, et al. A Small Molecule Inhibitor Targeting TRIP13 suppresses multiple myeloma progression. Cancer Res. 2019 Nov 15. pii:canres.3987.2018.McePdfHeightCaution: Product has not been fully validated for medical app