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TMI 1

Cat. No. 5960 2 篇引用文献 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Adam 17 (TACE) and MMP inhibitor; orally bioavailable
化学名： (3S)-4-[[4-(2-Butyn-1-yloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-3-thiomorpholinecarboxamide
纯度： ≥98% (HPLC)
说明书
引用文献 (2)
评论 (1)
文献 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for TMI 1

TMI 1 is an ADAM17 (TACE) and MMP inhibitor (IC50 values are 3, 4.7, 6.6, 8.4, 12, 26 and 26 nM for MMP-13, MMP-2, MMP-1, ADAM 17, MMP-9, MMP-7 and MMP-14, respectively). Suppresses TNF-α production in an acute LPS-mouse model. Reduces severity score in an in vivo model of rheumatoid arthritis. Displays selective cytotoxicity to tumor cells and cancer stem cells in vitro. Induces tumor apoptosis in a breast cancer in vivo model. Orally bioavailable.

许可信息

Sold for research purposes under agreement from Pfizer Inc

化合物库 for TMI 1

TMI 1 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for TMI 1

分子量 398.49
公式 C17H22N2O5S2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 287403-39-8
PubChem ID 5288615
InChI Key CVZIHNYAZLXRRS-HNNXBMFYSA-N
Smiles CC1(C)SCCN(S(C2=CC=C(OCC#CC)C=C2)(=O)=O)[C@H]1C(NO)=O

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for TMI 1

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 39.85 100
ethanol 7.97 20

制备储备液 for TMI 1

以下数据基于产品分子量 398.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.51 mL 12.55 mL 25.09 mL
5 mM 0.5 mL 2.51 mL 5.02 mL
10 mM 0.25 mL 1.25 mL 2.51 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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参考文献 for TMI 1

参考文献是支持产品生物活性的出版物。

Mezil et al (2012) Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer PLoS One 7 e43409 PMID: 23028451

Levin (2006) Heterocyclic inhibitors of tumor necrosis factor-α converting enzyme (TACE) Heterocycles 70 691

Zhang et al (2004) Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-α-converting enzyme/matrix meta J.Pharmacol.Exp.Ther. 309 348 PMID: 14718605

If you know of a relevant reference for TMI 1, please let us know.

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关键词: TMI 1, TMI 1 supplier, TMI1, Adam, 17, TACE, MMP, inhibitors, inhibits, tumor, necrosis, factor-α, TNF-α, converting, enzyme, rheumatoid, arthritis, cancer, stem, cells, anticancer, cytotoxic, orally, bioavailable, matrixins, matrix, metalloproteinases, proteinases, proteases, disintegrin, meta, Matrix, Metalloprotease, Cancer, Stem, Cells, ADAMs, 5960, Tocris Bioscience

2 篇 TMI 1 的引用文献

引用文献是使用了 Tocris 产品的出版物。 TMI 1 的部分引用包括：

Bent et al (2017) The LIM-Only Protein Four and a Half LIM Domain Protein 2 Attenuates Development of Psoriatic Arthritis by Blocking Adam17-Mediated Tumor Necrosis Factor Release. Am J Pathol 187 2388-2398 PMID: 28823868

J Philip et al (2020) Dendritic Cell-Restricted Progenitors Contribute to Obesity-Associated Airway Inflammation via Adam17-p38 MAPK-Dependent Pathway. Front Immunol 11 363 PMID: 32184787

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TMI 1 的评论

平均评分: 5 (Based on 1 Review.)

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Selective effect of TMI-1 was observed for caspase-dependent apoptosis.
By Anonymous on 10/12/2019
种属： Human

Selective effect of TMI-1 was observed for caspase-dependent apoptosis. TMI-1 was observed for efficient in 34/40 tumor cell lines of various origins.

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