Matrix metalloproteinases (MMPs) play important roles in tumor invasion, metastasis, and angiogenesis. Batimastat is a synthetic, low molecular weight, hydroxamate-based inhibitor of MMPs. It inhibited MMP-1, 2, 3, 9, 13, and 14 with IC50 values of 0.99, 0.73, 0.56, 0.60, 5.0, and 4.6 nM, respectively. It also blocked the activity of TNF-α converting enzyme with an IC50 value of 14.9 nM[3]. Batimastat showed less inhibitory effect on the processing of CD23, a low affinity IgE receptor, with an IC50 value of 100 nM[4]. In athymic mice inoculated with MDA435/LCC6 human breast cancer cells, daily injection of 50 mg/kg batimastat for 28 days significantly reduced tumor volumes relative to vehicle-treated controls[5].
作用机制
Batimastat inhibits the activity of MMPs via binding the zinc ion in the catalytic site of MMPs.
Batimastat/巴马司他 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Zebrafish embryos
5 mM
48 hours
Batimastat effectively reduced the expansion of scleral diameter in zebrafish embryos with an inhibition rate of 1.7%.
EBioMedicine. 2021 Mar;65:103263.
HL-60 cells
1-10 µM
72 hours
BB-94 decreases cell viability and density in a dose-, time-, administration-scheme-, and cell-line-dependent manner.
Int J Mol Sci. 2024 Apr 22;25(8):4554.
NB-4 cells
1-10 µM
72 hours
BB-94 decreases cell viability and density in a dose-, time-, administration-scheme-, and cell-line-dependent manner.
Int J Mol Sci. 2024 Apr 22;25(8):4554.
F36-P cells
1-10 µM
72 hours
BB-94 decreases cell viability and density in a dose-, time-, administration-scheme-, and cell-line-dependent manner.
Int J Mol Sci. 2024 Apr 22;25(8):4554.
H929 cells
1-10 µM
72 hours
BB-94 decreases cell viability and density in a dose-, time-, administration-scheme-, and cell-line-dependent manner.
Int J Mol Sci. 2024 Apr 22;25(8):4554.
IMC cells
1-10 µM
72 hours
BB-94 did not show an impact on cell viability and only induced a small reduction in cell density.
Int J Mol Sci. 2024 Apr 22;25(8):4554.
CHO (7W cells)
2.6 µM
Overnight
To evaluate the capability to inhibit α-secretase activity and confirm selectivity for ADAMs, with results showing indistinguishable inhibition and no significant toxicity to cells.
ACS Chem Neurosci. 2016 Jan 20;7(1):40-5.
Batimastat/巴马司他 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Form-deprivation myopia model
Eye drops
5 mM
Twice daily for 28 days
Batimastat significantly mitigated myopic shift and axial elongation in the form-deprivation myopia model and reduced scleral thinning and changes in collagen fibril diameter.
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