MMP2 Inhibitor Screening Assay Kit (Colorimetric) (ab139446)
Key features and details
- Assay type: Enzyme activity
- Detection method: Colorimetric
- Platform: Microplate reader
- Sample type: Inhibitor compounds
製品の概要
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製品名
MMP2 Inhibitor Screening Assay Kit (Colorimetric)
MMP2 キット 製品一覧 -
検出方法
Colorimetric -
サンプルの種類
Inhibitor compounds -
アッセイタイプ
Enzyme activity -
製品の概要
MMP2 Inhibitor Screening Assay Kit (Colorimetric) (ab139446) is a complete assay system designed to screen MMP2 inhibitors using a thiopeptide as a chromogenic substrate (Ac-PLG-[2-mercapto-4-methyl-pentanoyl]-LG-OC2H5). The MMP cleavage site peptide bond is replaced by a thioester bond in the thiopeptide. Hydrolysis of this bond by an MMP produces a sulfhydryl group, which reacts with DTNB [5,5’-dithiobis(2-nitrobenzoic acid), Ellman’s reagent] to form 2-nitro-5-thiobenzoic acid, which can be detected by its absorbance at 412 nm (ε=13,600 M-1cm-1 at pH 6.0 and above). The assays are performed in a convenient 96-well microplate format.
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特記事項
This kit is useful to screen inhibitors of MMP2, a potential therapeutic target. The MMP inhibitor NNGH is also included as a prototypic control inhibitor.
Thiol inhibitors should not be used with this kit, as they may interfere with the colorimetric assay.
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試験プラットフォーム
Microplate reader
製品の特性
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保存方法
Please refer to protocols. -
内容 1 x 96 tests 96-well Clear Microplate (1/2 Volume) 1 unit Colorimetric Assay Buffer 1 x 20ml MMP Inhibitor 1 x 50µl MMP Substrate 1 x 50µl MMP2 Enzyme (Human, Recombinant) 1 x 45.7µl -
研究分野
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機能
Ubiquitinous metalloproteinase that is involved in diverse functions such as remodeling of the vasculature, angiogenesis, tissue repair, tumor invasion, inflammation, and atherosclerotic plaque rupture. As well as degrading extracellular matrix proteins, can also act on several nonmatrix proteins such as big endothelial 1 and beta-type CGRP promoting vasoconstriction. Also cleaves KISS at a Gly-
-Leu bond. Appears to have a role in myocardial cell death pathways. Contributes to myocardial oxidative stress by regulating the activity of GSK3beta. Cleaves GSK3beta in vitro.
PEX, the C-terminal non-catalytic fragment of MMP2, posseses anti-angiogenic and anti-tumor properties and inhibits cell migration and cell adhesion to FGF2 and vitronectin. Ligand for integrinv/beta3 on the surface of blood vessels. -
組織特異性
Produced by normal skin fibroblasts. PEX is expressed in a number of tumors including gliomas, breast and prostate. -
関連疾患
Defects in MMP2 are the cause of Torg-Winchester syndrome (TWS) [MIM:259600]; also known as multicentric osteolysis nodulosis and arthropathy (MONA). TWS is an autosomal recessive osteolysis syndrome. It is severe with generalized osteolysis and osteopenia. Subcutaneous nodules are usually absent. Torg-Winchester syndrome has been associated with a number of additional features including coarse face, corneal opacities, patches of thickened, hyperpigmented skin, hypertrichosis and gum hypertrophy. However, these features are not always present and have occasionally been observed in other osteolysis syndromes. -
配列類似性
Belongs to the peptidase M10A family.
Contains 3 fibronectin type-II domains.
Contains 4 hemopexin-like domains. -
ドメイン
The conserved cysteine present in the cysteine-switch motif binds the catalytic zinc ion, thus inhibiting the enzyme. The dissociation of the cysteine from the zinc ion upon the activation-peptide release activates the enzyme. -
翻訳後修飾
Phosphorylation on multiple sites modulates enzymatic activity. Phosphorylated by PKC in vitro.
The propeptide is processed by MMP14 (MT-MMP1) and MMP16 (MT-MMP3). Autocatalytic cleavage in the C-terminal produces the anti-angiogenic peptide, PEX. This processing appears to be facilitated by binding integrinv/beta3. -
細胞内局在
Secreted > extracellular space > extracellular matrix. Membrane. Nucleus. Colocalizes with integrin alphaV/beta3 at the membrane surface in angiogenic blood vessels and melanomas. Found in mitochondria, along microfibrils, and in nuclei of cardiomyocytes. - Information by UniProt
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別名
- 72 kDa gelatinase
- 72kD type IV collagenase
- CLG 4
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画像
データシートおよび資料
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SDS download
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Datasheet download
参考文献 (0)
ab139446 は論文での使用が確認できていません。