Batimastat (BB94) (BB-94) is an effective, broad-spectrum matrix metalloprotease (MMP) inhibitor. Batimastat induces extracellular matrix degradation and inhibits angiogenesis, tumor growth and invasion, and metastasis.

MMP3:20 nM, MMP9:4 nM, MMP1:3 nM, MMP2:4 nM, MMP7:6 nM

Batimastat (BB-94) 是一种强效的、广谱的基质金属蛋白酶(MMP)抑制剂，针对MMP-1, MMP-2, MMP-9, MMP-7和MMP-3，其IC50分别为3 nM, 4 nM, 4 nM, 6 nM和20 nM。Batimastat展现出意外的结合几何形态，其中噻吩环深入主要特异性位点。

Batimastat能抑制B16-BL6小鼠黑色素瘤的转移扩散和生长。[1] 在小鼠的原位结肠肿瘤模型中，timastat的治疗能够抑制主要肿瘤生长(50%)、局部/区域性扩散(从67%降至35%)及远处转移(从30%降至10%)。[3]Batimastat通过阻断变异细胞招募内皮细胞或干扰血管结构中的细胞组织，最有可能减缓实验性血管瘤的体内生长。[4]

For luciferase assay, FG-9307 cells are transfected with the firefly NF-κB-specific luciferase reporter vector pNFκB-Met-Luc2. Transfection efficiency is monitored by co-transfection with the pSEAP2 control vector, which constitutively expresses the human secreted enhanced alkaline phosphatase (SEAP). Then the cells are treated with Resiquimod (R848, 1?μg/mL), CQ (10?μM), CQ plus R848 or PBS and incubated at 22°C for 24?h. The culture medium of the transfectants is then analyzed for luciferase activity and SEAP activity using Luciferase Assay Kit and the Great EscAPe? SEAP Chemiluminescence Detection Kit, respectively. The assay is performed three times.