287403-39-8
Chemical Structure
TMI-1
Synonym(s): WAY-171318
- CAS. Nr.: 287403-39-8
- Formula:C17H22N2O5S2
- Molecular Weight:398.50
IUPAC Name: (S)-4-((4-(but-2-yn-1-yloxy)phenyl)sulfonyl)-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide
InChIKey: CVZIHNYAZLXRRS-HNNXBMFYSA-N
SMILES: O=C([C@@H]1N(S(=O)(C2=CC=C(OCC#CC)C=C2)=O)CCSC1(C)C)NO
Biological Activity: TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions[1][2][3][4].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
TMI-1 | 99.57% | TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
TMI-1 (Standard) | ≥98% | TMI-1 (Standard) is the analytical standard of TMI-1 (HY-101448). This product is intended for research and analytical applications. TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Zhang Y, et al. 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-alpha-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J Pharmacol Exp Ther. 2004 Apr;309(1):348-55. [Content Brief]
- [2]. Mezil L, et al. Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer. PLoS One. 2012;7(9):e43409. [Content Brief]
- [3]. Yesul Kim, et al. TMI-1, TNF-α-Converting Enzyme Inhibitor, Protects Against Paclitaxel-Induced Neurotoxicity in the DRG Neuronal Cells In Vitro. Front Pharmacol. 2022 Feb 16:13:842779. [Content Brief]
- [4]. Wynand Melenhorst, et al. ADAM17 INHIBITION IN APOE DEFICIENT MICE RESULTS IN A PROATHEROGENIC LIPOPROTEIN PROFILE WITHOUT AFFECTING ATHEROSCLEROSIS. University of Groningen.
