巴马司他 T6011

Product Introduction
Bioactivity


英文名: Batimastat

描述: Batimastat (BB94) 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)。

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.

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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 47.8 mg/mL (100 mM)


关键字: Matrix metalloproteinases | Inhibitor | BB-94 | inhibit | BB 94 | MMP | Batimastat

相关产品: MMP3 inhibitor 1 | Excisanin A | Ilomastat | Leucodin | TNF Protease Inhibitor 2 | TAPI-1 trifluoroacetate (163847-77-6(free base)) | XL-784 | Chondroitin sulfate | Bacoside A | MMP-3 Inhibitor

相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Human Metabolite Library | Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Fibrosis Compound Library | Anti-Pancreatic Cancer Compound Library | Protease Inhibitor Library | Preclinical Compound Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途