tcsc3456 Marimastat

Marimastat is a broad spectrum inhibitor of MMPs with IC₅₀ values of 3, 5, 6, 9 and 13 nM for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7, respectively.

IC50 & Target: IC50: 3 nM (MMP-9), 5 nM (MMP-1), 6 nM (MMP-2), 9 nM (MMP-14), 13 nM (MMP-7)

In Vitro: Cyclam-marimastat conjugate and its metal complexes exhibit slightly reduced potency against MMP-1, but essentially identical inhibitory activity against MMP-3^[1]. Marimastat (1 μM) shows inhibition of vascular outgrowth, and selectively affects angiogenesis^[2].

In Vivo: Animals receiving chemoradiation + marimastat (8.7 mg/kg) have statistically significant delayed growth, compared to animals receiving chemoradiation alone. Marimastat may work in combination with chemotherapy and radiation to inhibit tumor growth^[3].