MMP2-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

MMP2-IN-1 

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。

MMP2-IN-1

MMP2-IN-1 Chemical Structure

CAS No. : 2764598-01-6

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生物活性

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].

IC50 & Target[1]

MMP2

6.8 μM (IC50)

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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

319.33

Formula

C15H13NO5S

CAS 号

2764598-01-6

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.

参考文献
  • [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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