TMI 1
- Product Name
- TMI 1
- CAS No.
- 287403-39-8
- Chemical Name
- TMI 1
- Synonyms
- TMI 1;TMI 1,TMI1;TMI-1 >=98% (HPLC);(S)-4-((4-(But-2-yn-1-yloxy)phenyl)sulfonyl)-N-hydroxy-2,2-dimethylthiomorpholine-3-carboxamide;(3S)-4-[[4-(2-Butyn-1-yloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-3-thiomorpholinecarboxamide;3-Thiomorpholinecarboxamide, 4-[[4-(2-butyn-1-yloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-, (3S)-
- CBNumber
- CB84727413
- Molecular Formula
- C17H22N2O5S2
- Formula Weight
- 398.5
- MOL File
- 287403-39-8.mol
TMI 1 Property
- Density
- 1.325±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- solubility
- DMSO: 25 mg/ml
- form
- powder
- pka
- 9.25±0.23(Predicted)
- color
- white to beige
N-Bromosuccinimide Price
- Product number
- PZ0336
- Product name
- TMI-1
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $108
- Updated
- 2024/03/01
- Product number
- PZ0336
- Product name
- TMI-1
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $174
- Updated
- 2024/03/01
- Product number
- 29713
- Product name
- TMI 1
- Packaging
- 5mg
- Price
- $153
- Updated
- 2024/03/01
- Product number
- 29713
- Product name
- TMI 1
- Packaging
- 10mg
- Price
- $275
- Updated
- 2024/03/01
- Product number
- 5960
- Product name
- TMI1
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $265
- Updated
- 2021/12/16
TMI 1 Chemical Properties,Usage,Production
Description
TMI 1 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17 (ADAM17/TACE; IC50 = 8.4 nM in a cell-free enzyme assay). It inhibits matrix metalloproteinase-1 (MMP-1), -2, -7, -9, -13, and -14, as well as ADAM-TS-4 in vitro (IC50s = 6.6, 4.7, 26, 12, 3, 26, and 100 nM, respectively). It also inhibits ADAM8, -10, -12, and -17/TACE in cell-free enzyme assays with Ki values of 21, 16, 1.8, and 0.079 nM, respectively, with slow-binding inhibition of ADAM17/TACE but not the other ADAM enzymes. TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC50s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC50s = 190 and 300 nM, respectively). It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC50 values of less than 100 nM without inhibiting TNF-α expression in vitro. TMI 1 inhibits LPS-induced TNF-α production in mice (ED50 = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED50s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.
Uses
TMI 1 is a dual TACE/MMP inhibitor, which represents a unique class of orally bioavailable small molecule TNF inhibitors that may be effective and beneficial for treating rhuematoid arthritis.
storage
Store at -20°C
TMI 1 Preparation Products And Raw materials
Raw materials
Preparation Products
TMI 1 Suppliers
- Tel
- --
- Fax
- --
- reag-info@gms.kanto.co.jp
- Country
- Japan
- ProdList
- 6756
- Advantage
- 74