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Biological Activity 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.
Sold for research purposes under agreement from Pfizer Inc
Compound Libraries for TMI 1
Technical Data for TMI 1
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for TMI 1
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for TMI 1
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
References for TMI 1
References are publications that support the biological activity of the product.
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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2 Citations for TMI 1
Citations are publications that use Tocris products. Selected citations for TMI 1 include:
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
Do you know of a great paper that uses TMI 1 from Tocris? Please let us know.
Reviews for TMI 1
Average Rating: 5 (Based on 1 Review.)
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Literature in this Area
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