| 产品描述: | 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 |
| 靶点: |
NF-κB;Apoptosis; NF-κB |
| 体外研究: |
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 IC50s of 1.0–10 μM in CalcuSyn in MM cell lines. DCZ0415 exerts cytotoxic effects by inhibiting DNA 288 synthesis in MM cells. Cell Proliferation Assay Cell 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 Assay Cell 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 Analysis Cell 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 Analysis Cell Line: MM cells Concentration: 10 and 20 μM Incubation Time: 24 hours Result: Induced a significant accumulation in G0/G1 MM cells. Western Blot Analysis Cell Line: MM cells Concentration |
| 体内研究: |
DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly reduces the growth of MM cells-induced tumors in immune-deficient mice. 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. |
| 参考文献: |
1. Wang Y, et al. A Small Molecule Inhibitor Targeting TRIP13 suppresses multiple myeloma progression. Cancer Res. 2019 Nov 15. pii: canres.3987.2018. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.806 ml |
14.028 ml |
28.056 ml |
| 5 mM |
0.561 ml |
2.806 ml |
5.611 ml |
| 10 mM |
0.281 ml |
1.403 ml |
2.806 ml |
| 50 mM |
0.056 ml |
0.281 ml |
0.561 ml |
|
| 注意: |
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