SB-3CT is a selective MMP-2 and MMP-9 inhibitor with Ki values of 13.9 and 600 nM, respectively, with much less potency to the other MMPs with Ki values of 206μM, 15μM and 96μM for MMP-1, 3 and 7, respectively[1]. SB-3CT also works as an inhibitor of gelatinase, a member of MMP family. Daily intraperitoneal administration of SB-3CT at dose of 50 mg/kg potently inhibited the liver metastasis and increased survival in an aggressive mouse model of T-cell lymphoma[2]. Treatment with 0.1 or 1μM SB-3CT inhibited capillary-like tubule formation by BMEC-1 cells and the ability of BMEC-1 cells to invade filters coated with Matrigel, but not the cell proliferation up to 10μM. Intraperitoneal injection with SB-3CT at dose of 50 mg/kg potently inhibited intraosseous tumor growth, bone degradation, and intratumoral angiogenesis of human PC3 cells within the marrow of human fetal femur fragments previously implanted in SCID mice[3]. SB-3CT is blood-brain barrier permeable as it can be rapidly absorbed and readily distributed to the brain, and also shows neuroprotective effect[4].
作用机制
SB-3CT directly binds the catalytic zinc ion of MMP-2.[5]
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