biological activity | Marimastat (BB-2516, TA2516) is a broad-spectrum matrix metalloprotease (MMP) inhibitor with IC50 of 3 nM,5 nM,6 nM,9 nM and 13 nM for MMP-9,MMP-1,MMP-2,MMP-14 and MMP-7, respectively. Phase 3. |
target | TargetValue MMP-9 3 nM MMP-1 5 nM MMP-2 6 nM MMP-14 9 nM MMP-7 16 nM |
|
| | | | | Target | Value |
MMP-9
(cell-free assay)
| 3 nM |
MMP-1
(cell-free assay)
| 5 nM |
MMP-2
(cell-free assay)
| 6 nM |
MMP-14
(cell-free assay)
| 9 nM |
MMP-7
(cell-free assay)
| 16 nM |
in vitro study | in U251, U87, GBM39 and GBM43 tumor cells, Marimastat(100 nM) can significantly inhibit the expression of MMP14. Marimastat can specifically inhibit the growth of glioma cells and has no effect on normal human astrocytes (NHA). Early Marimastat can down-regulate the expression of Notch target genes, such as Hes1 and HES5. |
in vivo study | in situ squamous cell carcinoma transplantation model, marimastat(150 mg/kg/day, oral administration) can significantly inhibit cervical lymph node metastasis and MMP-2 activation by osmotic pump administration, and the survival time is significantly prolonged compared with the control group. Marimastat can reduce polycystic MMP hyperactivity in human and rat bile ducts and block cystic dilatation of PCK bile ducts. marimastat chronic treatment inhibited hepatic cyst formation and fibrosis in eight-week-old PCK rats. |