Batimastat 是广谱MMP抑制剂,能够抑制MMP-1 (IC50:3 nM),MMP-2 (IC50:4 nM),MMP-9 (IC50:4 nM),MMP-7 (IC50:6 nM) 和 MMP-3 (IC50:20 nM)。
产品描述
Batimastat (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.
体外活性
Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively. [1]Batimastat exhibits an unexpected binding geometry, with the thiophene ring deeply inserted into the primary specificity site. [2]
体内活性
Batimastat can inhibit metastatic spread and growth of B16-BL6 murine melanoma. [1] In an orthotopic colon tumor model in mice, timastat treatment results in inhibition of primary tumor growth (by 50%), local/regional spread(from 67% to 35%), and distant metastasis(from 30% to 10%).[3]Batimastat reduces in vivo growth of experimental hemangiomas, most probably by blocking endothelial cell recruitment by the transformed cells or by interfering with cell organization in vascular structures. [4]
激酶实验
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.
Cas No.
130370-60-4
分子式
C23H31N3O4S2
分子量
477.64
别名
巴马司他;BB94
储存和溶解度
DMSO:47.8 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years