(R)-TAPI-2 (Synonyms: (R)-TNF Protease Inhibitor 2)

目录号: HY-100211A: FAQs
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TAPI-2 是 TAPI-2 (HY-100211A) 的异构体。TAPI-2 (TNF Protease Inhibitor 2) 是基质金属蛋白酶 (MMP)，肿瘤坏死因子α 转换酶 (TACE) 和解联蛋白和金属蛋白酶 (ADAM) 的广谱抑制剂, 对 MMP 的IC₅₀ 值为 20 μM。TAPI-2 阻止传染性 SARS-CoV 进入。

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(R)-TAPI-2 Chemical Structure

CAS No. : 689284-12-6

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性	(R)-TAPI-2 is the isomer of TAPI-2 (HY-100211A). TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC₅₀ of 20 μM for MMP^[1]. TAPI-2 blocks the entry of infectious SARS-CoV^[2].
体外研究 (In Vitro)	基于 hydroxamate 的金属蛋白酶抑制剂 TAPI-2 与 hmeprin 结合，hmeprin β 亚基的抑制常数 IC₅₀ 为 20±10 μM，hmeprin α 为 1.5±0.27 nM 亚基。通常，hmeprin α 比 β 亚基受到更强烈的抑制^[1]。在不影响 ADAM17 表达的情况下，TAPI-2 会显着降低 HCP-1 和 HT29 细胞中 NICD 及其下游靶标 HES-1 的蛋白质水平。此外，在两种 CRC 细胞系中，用 TAPI-2 处理细胞可显著降低 50% 的 CSC 表型。TAPI-2 对 NICD 和 HES-1 的球形成和蛋白水平的剂量依赖性证实，所使用的浓度 (20 μM) 在 TAPI-2 的有效剂量范围 (5-40 μM) 内^[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. (R)-TAPI-2 相关抗体:
分子量	415.53
Formula	C₁₉H₃₇N₅O₅
CAS 号	689284-12-6
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.
纯度 & 产品资料	Data Sheet (529 KB) 产品使用指南 (1538 KB)
参考文献	[1]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [Content Brief] [2]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Content Brief] [3]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [Content Brief]

Cell Assay ^[3]	TAPI-2 is dissolved in DMSO and diluted with appropriate medium before use. All experiments are performed using 20 μM TAPI-2. Cells are cultured with or without TAPI-2 for 48 hours and then seeded at 3,000 cells per well in 96-well plates. After pretreatment, increasing doses of 5-fluorouracil (5-FU) that are relevant to the recommended clinical dose (up to 2 μg/mL) are added, with or without TAPI-2, for 72 hours. Cell viability is assessed by adding MTT substrate (0.25% in phosphate-buffered saline [PBS]) in growth medium (1:5 dilution) to cells for 1 hour at 37°C. The cells are ished with PBS, and 100 μL of dimethyl sulfoxideis added. Optical density is measured at 570 nM, and relative MTT is presented as a percentage of control^[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [Content Brief] [2]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Content Brief] [3]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [Content Brief]

Cell Assay
^[3]

TAPI-2 is dissolved in DMSO and diluted with appropriate medium before use. All experiments are performed using 20 μM TAPI-2. Cells are cultured with or without TAPI-2 for 48 hours and then seeded at 3,000 cells per well in 96-well plates. After pretreatment, increasing doses of 5-fluorouracil (5-FU) that are relevant to the recommended clinical dose (up to 2 μg/mL) are added, with or without TAPI-2, for 72 hours. Cell viability is assessed by adding MTT substrate (0.25% in phosphate-buffered saline [PBS]) in growth medium (1:5 dilution) to cells for 1 hour at 37°C. The cells are ished with PBS, and 100 μL of dimethyl sulfoxideis added. Optical density is measured at 570 nM, and relative MTT is presented as a percentage of control^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Wang R, et al. A Disintegrin and Metalloproteinase Domain 17 Regulates Colorectal Cancer Stem Cells and Chemosensitivity Via Notch1 Signaling. Stem Cells Transl Med. 2016 Mar;5(3):331-8. [Content Brief]

[2]. Kruse MN, et al. Human meprin alpha and beta homo-oligomers: cleavage of basement membrane proteins and sensitivity to metalloprotease inhibitors. Biochem J. 2004 Mar 1;378(Pt 2):383-9. [Content Brief]

[3]. Shiori Haga, et al. TACE Antagonists Blocking ACE2 Shedding Caused by the Spike Protein of SARS-CoV Are Candidate Antiviral Compounds. Antiviral Res. 2010 Mar;85(3):551-5. [Content Brief]

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(R)-TAPI-2689284-12-6(R)-TNF Protease Inhibitor 2OthersInhibitorinhibitorinhibit

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(R)-TAPI-2 (Synonyms: (R)-TNF Protease Inhibitor 2)

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(R)-TAPI-2 (Synonyms: (R)-TNF Protease Inhibitor 2)

Customer Review

Other Forms of (R)-TAPI-2:

(R)-TAPI-2 相关抗体

(R)-TAPI-2 相关产品

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

(R)-TAPI-2 相关抗体:

(R)-TAPI-2 相关分类

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