Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer.
Description | TMI-1 (WAY-171318), a novel orally active inhibitor of ADAM17 (TACE) and MMP, induces tumor apoptosis in a breast cancer. |
Targets&IC50 | ADAM8:21 nM(ki), MMP9:12 nM, MMP2:4.7 nM, TNF-α secretion (Raw cells):40 nM, MMP14:26 nM, ADAMTS-4:100 nM, MMP7:26 nM, ADAM12:1.8 nM(ki), ADAM17/TACE:0.079 nM(ki), TNF-α secretion (THP-1 cells):200 nM, MMP1:6.6 nM, MMP13:3 nM, ADAM10:16 nM(ki), ADAM17/TACE:8.4 nM (IC50) |
In vitro |
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).[1] 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.[3] |
In vivo | 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.[3] |
Synonyms | WAY-171318 |
Molecular Weight | 398.5 |
Formula | C17H22N2O5S2 |
CAS No. | 287403-39-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.9 mg/mL (410.4 mM)
You can also refer to dose conversion for different animals. More
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TMI-1 287403-39-8 Apoptosis Proteases/Proteasome MMP WAY171318 TMI1 WAY-171318 TMI 1 WAY 171318 inhibitor inhibit