Adam 17 (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
|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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 398.49. Batch specific molecular weights may vary from batch to batch due to solvent 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 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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Citations for TMI 1
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.