Uses
SB 3CT is a selective and potent gelatinase inhibitor which may be used for the treatment of brain metastasis.
Uses
SB3CT has been used as irreversible inhibitor of matrix metallopeptidase 9 (MMP9) in cell cultures to exclude reciprocal regulation.
Definition
ChEBI: 2-[(4-phenoxyphenyl)sulfonylmethyl]thiirane is an aromatic ether.
Biochem/physiol Actions
SB-3CT is a potent matrix metalloproteinase MMP-2 and MMP-9 inhibitor. Matrix metalloproteinases (MMPs) are involved in a number of activities including angiogenesis and embryogenesis. In particular, gelatinases A (MMP-2) and B (MMP-9), are thought to facilitate tumor metastasis. SB-3CT exhibits a covalent mechanism based behavior in inhibition of MMP-2 and MMP-9. This inhibitor appears to have similarity to TIMP-1 and TIMP-2 in the slow-binding component of inhibition. SB-3CT has been shown to directly bind to the zinc in the catalytic site of MMP-2. SB-3CT does not affect the activities of MMP-1 (Ki = 206 μM) MMP-3 (Ki = 15 μM), or MMP-7 (Ki = 96 μM).
in vivo
SB-3CT (i.p.; 50 mg/kg; every other day; five weeks) inhibits intraosseous growth of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice[3].
| Animal Model: | Five-week-old male C.B.-17.SCID mice[3] |
| Dosage: | 50 mg/kg |
| Administration: | IP; every other day; five weeks |
| Result: | Inhibited intraosseous growth of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice.
|
IC 50
MMP-2: 13.9 nM (Ki); MMP-9: 600 nM (Ki)
