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/ MMP / Marimastat/马立马司他

Marimastat/马立马司他 {[allProObj[0].p_purity_real_show]}

货号：A573351 同义名： BB2516; TA2516

Marimastat是一种竞争性广谱基质金属蛋白酶（MMP）抑制剂，对MMP-9、MMP-1、MMP-2、MMP-14和MMP-7的IC50值分别为3、5、6、9和13 nM。

Marimastat/马立马司他 化学结构 CAS号：154039-60-8
Marimastat/马立马司他 化学结构
CAS号：154039-60-8
Marimastat/马立马司他 3D分子结构
CAS号：154039-60-8
Marimastat/马立马司他 化学结构 CAS号：154039-60-8
Marimastat/马立马司他 3D分子结构 CAS号：154039-60-8
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Marimastat/马立马司他 纯度/质量文件 产品仅供科研

货号：A573351 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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产品名称 MMP ↓ 其他靶点 纯度
Marimastat +++

MMP-14, IC50: 3 nM

MMP-7, IC50: 16 nM

 		98%
Ilomastat ++++

MMP-26, Ki: 0.36 nM

MMP-2, Ki: 0.1 nM

 		99%+
SB-3CT +

MMP-9, Ki: 600 nM

MMP-2, Ki: 13.9 nM

 		99%+
Doxycycline ✔ 95%
NSC 405020 ✔ 98%
Batimastat +++

MMP-1, IC50: 3 nM

MMP-7, IC50: 4 nM

 		99%+
Nobiletin ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Marimastat/马立马司他 生物活性

靶点

  • MMP

    MMP-14, IC50:3 nM

    MMP-7, IC50:16 nM
描述 Marimastat is a broad spectrum MMP inhibitor with IC50 values of 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 respectively[1]. Marimastat is the orally bioavailable analogue of hydroxamate peptidomimetic inhibitor batimastat[2]. Treatment with 10μM marimastat could inhibit elastin degradation and active MMP-2 production with aortic organ culture[3]. Marimastat at concentration of 50μg/ml could significantly reduce the invasion of osteosarcoma cells by 30-60%, including U2OS, OHS, and SaOS cells, but not KPDX cells[4]. Daily administration of marimastat at concentration of 27 mg/kg for 2 weeks by subcutaneously-inoculating mini-osmotic pumps could inhibit peritoneal dissemination of human gastric cancer cells through inhibition of tumor angiogenesis in SCID mice injected with human gastric cancer cells[5]. Marimastat also works as an inhibitor of TACE (tumor necrosis factor-α converting enzyme). An oral dose of 200mg/kg marimastat almost completely inhibited LPS-induced soluble TNF-α production, but only slightly delayed LPS lethality in mice[6].
作用机制 Marimastat is a hydroxamate peptidomimetic compound which can bind covalently to the zinc atom at the MMP-active site.[2]

Marimastat/马立马司他 细胞实验

Cell Line
Concentration Treated Time Description References
Polycystic kidney (PCK) rat cholangiocytes 200 µM 24 hours Inhibition of cystic expansion in polycystic kidney (PCK) cholangiocytes Gut. 2014 Oct;63(10):1658-67.
HaCaT cells 2.56 µM 24 hours To test the inhibitory effect of Marimastat on venom-induced cytotoxicity, results showed that Marimastat significantly reduced the cell-damaging potency of certain snake venoms. Nat Commun. 2023 Dec 14;14(1):7812.
4T1 cells 5 μg/mL 24 hours HPMC NPs significantly downregulated the expressions of MMP-2, MMP-3, MMP-7, and MMP-9 by 100-300%, and inhibited the activities of MMP-9 and MMP-7 by 50-100%. Theranostics. 2018 Apr 15;8(10):2830-2845.
786-O cells 1 µM, 2 µM, 3 µM 24 hours Marimastat could more efficiently reduce renal cell proliferation and invasive capacity, and increase the apoptosis rate of 786-O cells. J Exp Clin Cancer Res. 2013 May 9;32(1):26.
OS-RC-2 cells 1 µM, 2 µM, 3 µM 24 hours Marimastat could more efficiently reduce renal cell proliferation and invasive capacity. J Exp Clin Cancer Res. 2013 May 9;32(1):26.
ECFCs 10 µM 24 hours To evaluate the effect of Marimastat on cell viability and invasion ability of ECFCs. Results showed that Marimastat promoted ECFC invasion and tubular formation, inducing amoeboid characteristics. J Transl Med. 2023 Feb 9;21(1):102.
Crotalus atrox venom proteins 15 µM and 150 µM 30 minutes To assess the stabilizing effect of Marimastat on SVMP proteins in Crotalus atrox venom. Results showed that Marimastat significantly increased the stability of SVMP proteins in solution and reduced their content in the precipitate. Mol Cell Proteomics. 2024 Jun;23(6):100779.
Mouse cerebrovascular endothelial cells (mCEC) 5% v/v 4 hours To assess the inflammatory bioactivity of serum following MWCNT exposure, results showed that MWCNT exposure significantly upregulated endothelial Ccl2 and Vcam1 mRNA, while Marimastat pretreatment partially inhibited these effects. Part Fibre Toxicol. 2021 Sep 8;18(1):34.
4T1 cells 5 µg/mL 48 hours To evaluate the cytotoxicity of MATT-LTSLs on 4T1 cells, results showed that at 5 µg/mL, MATT-LTSLs did not significantly affect cell viability. Signal Transduct Target Ther. 2019 Aug 9;4:26.
MDA-MB-435 cells 10 µg/mL 48 hours To evaluate the cytotoxicity of MATT-LTSLs on MDA-MB-435 cells, results showed that at 10 µg/mL, MATT-LTSLs did not significantly affect cell viability. Signal Transduct Target Ther. 2019 Aug 9;4:26.
Zebrafish embryos 50 µM 48 hours Screening compounds that can reduce scleral tissue expansion, Marimastat significantly reduced the percentage of scleral tissue expansion EBioMedicine. 2021 Mar;65:103263.
HRECs 10 µM 48 hours To evaluate the effect of Marimastat on migration and tubular formation of HRECs. Results showed that Marimastat slightly inhibited the differentiation of HRECs in tubular structures and didn’t affect the migration ability without stimulating it. J Transl Med. 2023 Feb 9;21(1):102.
U87 200 nM 5 days To evaluate the effect of Marimastat on TMZ resistance, results showed Marimastat did not significantly enhance TMZ sensitivity Neuro Oncol. 2015 Nov;17(11):1474-85.
GBM29 200 nM 5 days To evaluate the effect of Marimastat on TMZ resistance, results showed Marimastat did not significantly enhance TMZ sensitivity Neuro Oncol. 2015 Nov;17(11):1474-85.
GBM42 200 nM 5 days To evaluate the effect of Marimastat on TMZ resistance, results showed Marimastat did not significantly enhance TMZ sensitivity Neuro Oncol. 2015 Nov;17(11):1474-85.
GBM98 200 nM 5 days To evaluate the effect of Marimastat on TMZ resistance, results showed Marimastat did not significantly enhance TMZ sensitivity Neuro Oncol. 2015 Nov;17(11):1474-85.
Normal human cholangiocytes 200 µM Inhibition of matrix metalloprotease (MMP) activity Gut. 2014 Oct;63(10):1658-67.
Polycystic human cholangiocytes 200 µM Inhibition of matrix metalloprotease (MMP) activity Gut. 2014 Oct;63(10):1658-67.

Marimastat/马立马司他 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Polycystic kidney (PCK) rats Polycystic kidney (PCK) rat model Oral 0.2856 mg/kg/day Twice daily for 8 weeks Inhibition of hepatic cystogenesis and fibrosis Gut. 2014 Oct;63(10):1658-67.
A/J mice AOM-induced colon cancer model Alzet pump implantation 1.1 μmoles/day/mouse Daily administration for 2 weeks To assess the effect of Marimastat on EGFR signaling in the colonic mucosa of mice fed a Western diet (WD), results showed that Marimastat significantly inhibited EGFR signals in the colonic mucosa, with greater than 50% reductions in phospho-active EGFR (pEGFR), pErbB2 and pERK. Clin Cancer Res. 2017 Jan 15;23(2):549-561
C57BL/6 mice MWCNT-induced pulmonary inflammation model Oropharyngeal aspiration 10 mg/kg Single dose, 24 hours duration To investigate the effect of Marimastat on MWCNT-induced pulmonary inflammation and serum peptide generation, results showed that Marimastat significantly inhibited MWCNT-induced serum peptide generation but had minimal effect on pulmonary inflammation. Part Fibre Toxicol. 2021 Sep 8;18(1):34.
C57BL6 mice Colorectal cancer model Intraperitoneal injection 15 mg/kg Daily for 15 days Marimastat treatment reduced tumor size, with enhanced effects when combined with miR-126 overexpression. Cell Death Dis. 2024 Oct 17;15(10):753
Mice 4T1 tumor model Tail vein injection 5 mg/kg Every 3 days for 18 days To evaluate the antitumor efficacy of MATT-LTSLs in 4T1 tumor-bearing mice, results showed that MATT-LTSLs significantly inhibited tumor growth and reduced the number of metastatic lung nodules and microvessels inside the tumor. Signal Transduct Target Ther. 2019 Aug 9;4:26.
Balb/C mice 4T1 breast cancer model Intravenous injection 5 mg/kg Every 3 days for 15 days HPMC NPs significantly inhibited tumor growth, reducing tumor volume by 5.5-fold, and significantly downregulated the expressions and activities of MMP-2 and MMP-9 by >150% and >50%, respectively. Theranostics. 2018 Apr 15;8(10):2830-2845.
C57BL/6 mice Form-deprivation myopia model Eye drops 50 µM Twice daily for 28 days Validate the efficacy of Marimastat in form-deprivation myopia models, results showed Marimastat significantly mitigated myopic shift and axial elongation EBioMedicine. 2021 Mar;65:103263.
SCID beige mice Matrigel plug assay Subcutaneous injection 50 µM Single injection, lasting 5 days To evaluate the effect of Marimastat on angiogenesis in mice. Results showed that Marimastat stimulated angiogenesis. J Transl Med. 2023 Feb 9;21(1):102.
Mice Dermonecrosis model Intradermal injection 60 µg Single injection, lasting 72 hours To test the inhibitory effect of Marimastat on venom-induced dermonecrosis, results showed that Marimastat significantly reduced the area of skin lesions. Nat Commun. 2023 Dec 14;14(1):7812.
Mice Snake envenoming model Intravenous injection 60 µg/mouse Single dose, monitored for 6 hours Marimastat significantly prolonged the survival time of envenomed mice, with only one mouse succumbing at the end of the 6-hour experimental period, while the remaining four survived. Nat Commun. 2020 Dec 15;11(1):6094

Marimastat/马立马司他 动物研究

Dose Mice: 8.7 mg/kg[7] (subcutaneous osmotic pump), 18 mg/kg[8] (s.c.); 100 mg/kg[9] (p.o.)
Administration OMP (s.c.), p.o.

Marimastat/马立马司他 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00261391 Vascular Anomalies Phase 1 Completed - United States, Massachusetts ... 展开 >> Childrens Hospital Boston, Massachusetts, United States, 02115 收起 <<
NCT00002911 Lung Cancer Phase 3 Completed - -
NCT00003010 Breast Cancer Phase 3 Completed - United States, Arizona ... 展开 >> CCOP - Scottsdale Oncology Program Scottsdale, Arizona, United States, 85259-5404 United States, Illinois Robert H. Lurie Comprehensive Cancer Center, Northwestern University Chicago, Illinois, United States, 60611 CCOP - Carle Cancer Center Urbana, Illinois, United States, 61801 United States, Iowa CCOP - Cedar Rapids Oncology Project Cedar Rapids, Iowa, United States, 52403-1206 CCOP - Iowa Oncology Research Association Des Moines, Iowa, United States, 50309-1016 Siouxland Hematology-Oncology Sioux City, Iowa, United States, 51101-1733 United States, Kansas CCOP - Wichita Wichita, Kansas, United States, 67214-3882 United States, Minnesota CCOP - Duluth Duluth, Minnesota, United States, 55805 Mayo Clinic Cancer Center Rochester, Minnesota, United States, 55905 CentraCare Clinic Saint Cloud, Minnesota, United States, 56303 United States, Nebraska CCOP - Missouri Valley Cancer Consortium Omaha, Nebraska, United States, 68131 United States, New Jersey Trinitas Hospital - Jersey Street Campus Elizabeth, New Jersey, United States, 07201 Hunterdon Regional Cancer Center Flemington, New Jersey, United States, 08822 Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 Morristown Memorial Hospital Morristown, New Jersey, United States, 07962-1956 Riverview Medical Center Red Bank, New Jersey, United States, 07701 St. Francis Medical Center Trenton, New Jersey, United States, 08629 United States, New York Albert Einstein Comprehensive Cancer Center Bronx, New York, United States, 10461 United States, North Dakota Medcenter One Health System Bismarck, North Dakota, United States, 58501 Altru Health Systems Grand Forks, North Dakota, United States, 58201 United States, Ohio CCOP - Columbus Columbus, Ohio, United States, 43206 CCOP - Toledo Community Hospital Oncology Program Toledo, Ohio, United States, 43623-3456 United States, Pennsylvania Hahnemann University Hospital Philadelphia, Pennsylvania, United States, 19102-1192 United States, South Dakota Rapid City Regional Hospital Rapid City, South Dakota, United States, 57709 CCOP - Sioux Community Cancer Consortium Sioux Falls, South Dakota, United States, 57105-1080 收起 <<

Marimastat/马立马司他 参考文献

[1]Rasmussen HS, McCann PP, et al. Matrix metalloproteinase inhibition as a novel anticancer strategy: a review with special focus on batimastat and marimastat. Pharmacol Ther. 1997;75(1):69-75.

[2]Hidalgo M, Eckhardt SG, et al. Development of matrix metalloproteinase inhibitors in cancer therapy. J Natl Cancer Inst. 2001 Feb 7;93(3):178-93.

[3]Treharne GD, Boyle JR, et al. Marimastat inhibits elastin degradation and matrix metalloproteinase 2 activity in a model of aneurysm disease. Br J Surg. 1999 Aug;86(8):1053-8.

[4]Bjørnland K, Flatmark K, et al. Matrix metalloproteinases participate in osteosarcoma invasion. J Surg Res. 2005 Aug;127(2):151-6. Epub 2005 Apr 14.

[5]Wada N, Otani Y, et al. Reduced angiogenesis in peritoneal dissemination of gastric cancer through gelatinase inhibition. Clin Exp Metastasis. 2003;20(5):431-5.

[6]Tsuji F, Oki K, et al. Differential effects between marimastat, a TNF-alpha converting enzyme inhibitor, and anti-TNF-alpha antibody on murine models for sepsis and arthritis. Cytokine. 2002 Mar 21;17(6):294-300.

Marimastat/马立马司他 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.02mL

0.60mL

0.30mL

15.09mL

3.02mL

1.51mL

30.17mL

6.03mL

3.02mL

Marimastat/马立马司他 技术信息

CAS号154039-60-8
分子式C15H29N3O5
分子量 331.41
SMILES Code O=C(N[C@@H](C(C)(C)C)C(NC)=O)[C@H](CC(C)C)[C@H](O)C(NO)=O
MDL No. MFCD00866242
别名 BB2516; TA2516; KB-R8898
运输蓝冰
InChI Key OCSMOTCMPXTDND-OUAUKWLOSA-N
Pubchem ID 119031
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(316.83 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Marimastat | 154039-60-8 | BB2516 | TA2516 | BB 2516 | BB-2516 | TA2516 | TA 2516 | TA-2516 | MMP Inhibitor | Metabolic Enzyme/Protease | MMP | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Marimastat/马立马司他 纯度/质量文件 | Marimastat/马立马司他 亚型比较 | Marimastat/马立马司他 生物活性 | Marimastat/马立马司他 动物研究 | Marimastat/马立马司他 临床数据 | Marimastat/马立马司他 参考文献 | Marimastat/马立马司他 实验方案 | Marimastat/马立马司他 技术信息

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