| Description |
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis[1].
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| Related Catalog |
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| Target |
MMP2:6.8 μM (IC50)
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| In Vitro |
MMP2-IN-1 (compound 4a) (0-10 μM; 74 hours) exhibits IC50 values 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 IC50 values 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.
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| 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.
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| References |
[1]. Chen C, Luo Y, Yin H, et al. Design, synthesis, and antitumor activity evaluation of novel acyl sulfonamide spirodienones. Bioorg Med Chem. 2022;60:116626.
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