MMP2-IN-1 是一种中度有效的MMP2抑制剂，IC50为 6.8 μM。MMP2-IN-1 通过阻滞细胞周期和诱导细胞凋亡 (apoptosis)，在某些癌细胞中表现出显著的抗增殖活性。
| 生物活性 | MMP2-IN-1 is a moderate potenetMMP2inhibitor withIC50of 6.8 μM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certaincancercells by arresting the cell cycle and inducingapoptosis[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | MMP2-IN-1 (compound 4a) (0-10 μM; 74 hours) exhibits IC50values of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, and over 10 μM in Hep 5G cells[1].
MMP2-IN-1 (10 μM; 24 hours) induces cell cycle arrest in the S phase[1].
MMP2-IN-1 (0.01 μM, 0.1 μM, 1 μM and 10 μM; 24 hours) induces a dose-dependent increment in early-and late-stage apoptosis of MDA-MB-231 cells, and increased the early-stage apoptosis percentage from 4.66% to 10.9% at 10 μM[1].
Cell Proliferation Assay | Cell Line: | MDA-MB-231, A549, HeLa and Hep 5G cells[1] | | Concentration: | 0-10 μM | | Incubation Time: | 74 hours | | Result: | Exhibited IC50values of 0.07 μM, 0.11 μM, and 0.18 μM against MDA-MB-231, A549, and HeLa cancer cells, respectively, and over 10 μM in Hep 5G cells. |
Cell Cycle Analysis | Cell Line: | MDA-MB-231[1] | | Concentration: | 10 μM | | Incubation Time: | 24 hours | | Result: | Induced cell cycle arrest in the S phase. |
Apoptosis Analysis | Cell Line: | MDA-MB-231[1] | | Concentration: | 0.01 μM, 0.1 μM, 1 μM and 10 μM | | Incubation Time: | 24 hours | | Result: | Induced a dose-dependent increment in early-and late-stage apoptosis of MDA-MB-231 cells, and increased the early-stage apoptosis percentage from 4.66% to 10.9% at 10 μM. |
|
体内研究
(In Vivo) | MMP2-IN-1 (100 mg/kg, 150 mg/kg, 200 mg/kg, 250 mg/kg; IP, single) causes 0%, 30%, 50% and 60% mortality rate at dosing 100 mg/kg, 150 mg/kg, 200 mg/kg and 250 mg/kg respectively[1].
MMP2-IN-1 (10 mg/kg; IP, daily, for 14 days) significantly inhibits tumor growth in metastatic 4T1 murine breast cancer model[1].
| Animal Model: | Kunming mice (n = 10, half male and half female)[1] | | Dosage: | 100 mg/kg, 150 mg/kg, 200 mg/kg, 250 mg/kg | | Administration: | IP, single | | Result: | No mortality occurred after administration of 100 mg/kg, and the mortality rate was 30%, 50% and 60% at dosing 150 mg/kg, 200 mg/kg, 250 mg/kg respectively. |
| Animal Model: | Orthotopic 4T1 tumor-bearing mice[1] | | Dosage: | 10 mg/kg | | Administration: | IP, daily, for 14 days | | Result: | Significantly inhibited tumor growth in metastatic 4T1 murine breast cancer model. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
