TMI-1
Based on 2 publication(s) in Google Scholar
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.
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- Pureté: 99.57%
- CAS No.: 287403-39-8
- Formule: C17H22N2O5S2
- Masse moléculaire:398.50
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) TMI-1
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MoreVoir tous les produits spécifiques à Isoform Caspase
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Activité biologique
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IL-6 |
IL-1β |
MMP-1 6.6 nM (IC50) |
MMP-2 4.7 nM (IC50) |
MMP-7 26 nM (IC50) |
MMP-14 26 nM (IC50) |
MMP-9 12 nM (IC50) |
MMP-13 3 nM (IC50) |
TACE 8.8 nM (IC50) |
ADAM17 |
ADAM-TS-4 100 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
8 nM
Compound: 6
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Inhibition of human TACE expressed in CHO cells by FRET assay
Inhibition of human TACE expressed in CHO cells by FRET assay
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[PMID: 17606376] |
TMI-1 inhibits TNF-α secretion in mouse monocyte Raw cells with an IC50 of 40 nM, in human monocyte THP-1 cells with an IC50 of 200 nM, in primary human monocyte lines with an IC50 of 190 nM, and in human whole blood with an IC50 of 300 nM[1].
TMI-1 inhibits the shedding of TNFR II in human whole blood, with an IC50 of 0.72μM[1].
TMI-1 (0-20 μM, 5 days) shows a dose-dependent inhibition of proliferation in breast cancer cell lines BT-20, SUM149, MDA-MB-231, SK-BR-3, L226, SUM190, T147D and Cama-1, with ED50 of 1.3, 1.5, 8.1, 1.6, 2.0, 2.0, 2.5, and 2.5 μM respectively, and induces the activity of Caspase-3 and Caspase-7 without affecting the vitality of normal cells[2].
TMI-1 (0-20 μM, 48 h) inhibits the cell cycle of breast cancer cells SUM149, promotes apoptosis, activates Caspase-3, Caspase-7, Caspase-8, Caspase-9, and increases ROS production[2].
TMI-1 (4 ng/mL, 24 h) improves the degenerative changes in the axons of 50B11 cells induced by paclitaxel (HY-B0015) and enhances the growth of neurites induced by forskolin (HY-15371), and this effect is dose-dependent[3].
TMI-1 (0.04-4 ng/mL, 24 h) reduces the expression of TRPV1 protein in 50B11 cells in a dose-dependent manner, along with a decrease in the expressions of PKC, PI3K, NF-κB, TNF-α, IL-1β, and IL-6 mRNA, as well as calcium influx[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SUM149, TgNeu 27
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Concentration:0, 5, 10, 15, 20 μM
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Incubation Time:5 days
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Result:Inhibited breast cancer cell proliferation by dosage-dependent.
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Cell Line:SUM149
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Concentration:0, 2.5, 5, 10, 15, 20 μM
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Incubation Time:48 h
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Result:Made G0/G1 phase cell cycle arrest.
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Cell Line:SUM149, TgNeu 27
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Concentration:0, 1.25, 5, 10, 20 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis and activated Caspase-3, Caspase-7, Caspase-8, and Caspase-9 in a dose-dependent manner, while also increasing the generation of ROS.
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Cell Line:50B11 (induced by forskolin and paclitaxel)
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Concentration:4 ng/mL; 0.04, 0.4, 4 ng/mL
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Incubation Time:24 h
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Result:Promoted the repair of axonal damage, improved the growth of neural projections, and had a dose-dependent effect.
Reduced intracellular calcium concentration.
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Cell Line:50B11 (induced by forskolin and paclitaxel)
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Concentration:0.04, 0.4, 4 ng/mL
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Incubation Time:24 h
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Result:Reduced the levels of the TRPV1 protein in a dose-dependent manner.
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Cell Line:50B11 (induced by forskolin and paclitaxel)
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Concentration:0.04, 0.4, 4 ng/mL
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Incubation Time:24 h
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Result:Decreased the levels of PKC, PI3K, NF-κB, TNF-α、IL-1β and IL-6.
TMI-1 (100 mg/kg, daily, 30 days, oral) slows down breast cancer tumor growth and prevents tumor occurrence in a breast cancer mouse model[2].
TMI-1 (100 mg/kg, daily, 4 weeks, oral) alters the lipoprotein profile that promotes atherosclerosis but does not affect the progression of early atherosclerotic lesions[4].
Analysis of pharmacokinetics in Balb/CJ mice after a single oral dose of 50 mg/kg[1]
| Route | Dose (mg/kg) | AUC (ng•h/mL) | bioavailability (%) | t1/2 (h) | Cmax (μM) |
| oral | 50 | 1484 | 39 | 1.68 | 3 |