| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
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info@bocsci.com |
| Products Intro: |
Product Name:TMI 1
CAS:287403-39-8
Purity:98% by HPLC Remarks:TMI 1 is a dual inhibitor of Adam 17 (TACE) and MMP inhibitor (IC50 = 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). TMI 1 suppresses TNF
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| Product Name: | TMI 1 | | Synonyms: | TMI 1;(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)-;TMI-1 >=98% (HPLC);TMI 1,TMI1 | | CAS: | 287403-39-8 | | MF: | C17H22N2O5S2 | | MW: | 398.5 | | EINECS: | | | Product Categories: | | | Mol File: | 287403-39-8.mol |  |
| | TMI 1 Chemical Properties |
| 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 |
| | TMI 1 Usage And Synthesis |
| 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 |
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