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TMI-1

CAT: 0804-HY-101448-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-101448-01Size:5 mg
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Description
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].
CAS Number
287403-39-8
Product Name Alternative
WAY-171318
UNSPSC
12352005
Target
Apoptosis; Caspase; Interleukin Related; MMP; TNF Receptor
Type
Reference compound
Related Pathways
Apoptosis; Immunology/Inflammation; Metabolic Enzyme/Protease
Applications
COVID-19-immunoregulation
Field of Research
Cancer; Infection; Inflammation/Immunology; Neurological Disease
Assay Protocol
https://www.medchemexpress.com/tmi-1.html
Purity
99.57
Solubility
DMSO : ≥ 100 mg/mL
Smiles
O=C([C@@H]1N(S(=O)(C2=CC=C(OCC#CC)C=C2)=O)CCSC1(C)C)NO
Molecular Formula
C17H22N2O5S2
Molecular Weight
398.50
References & Citations
[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.|[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.|[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.|[4]Wynand Melenhorst, et al. ADAM17 INHIBITION IN APOE DEFICIENT MICE RESULTS IN A PROATHEROGENIC LIPOPROTEIN PROFILE WITHOUT AFFECTING ATHEROSCLEROSIS. University of Groningen.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
IL-1; IL-6; MMP-1; MMP-14; MMP-2; MMP-7; MMP-9