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Competitive, mechanism-based inhibitor of matrix metalloproteinases 2 and 9 (MMP-2 and MMP-9). It possesses Ki values in the nanomolar range against the gelatinases (14nM for MMP-2; 600nM for MMP-9), but in the micromolar range against other metalloproteinases (206μM for MMP-1, 15μM for MMP-3, 96μM for MMP-7, and 4μM for ADAM17/TACE). This inhibitor has also been used in vitro, in vivo, and in tissue culture. In vivo, it is metabolized to an even more potent gelatinase inhibitor. | [Enzyme inhibitor]
This thiirane (FW = 306.41 g/mol), also known as matrix
metalloproteinase-2/matrix metalloproteinase-9 inhibitor IV (MMP-
2/MMP-9 inhibitor IV) and SB-3CT, is a mechanism-based inhibitor of
gelatinase A, or matrux metalloproteinase 2, Ki = 0.014 μM, gelatinase
B, or matrix metalloproteinase 9, Ki = 0.6 μM, membrane-type matrix
metalloproteinase 1, matrix metalloproteinase 14, matrilysin, Ki = 96
μM, stromelysin 1, or matrix metalloproteinase 3, Ki = 15 μM. |
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