化合物TMI-1 T28985

Product Introduction
Bioactivity


英文名: TMI-1

描述: TMI-1 (WAY-171318) 是一种有效的抑制剂，用于抑制去整合素金属酶17 (ADAM17) 和其他基质金属蛋白酶MMPs。TMI-1 能够有效地抑制LPS 诱导的人原代单核细胞和人全血中TNF-α的分泌。TMI-1 在三阴性 (TN) 和过度表达ERBB2的乳腺肿瘤细胞系中选择性地诱导Caspase 依赖的细胞凋亡。

体外活性: TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC50s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC50s = 190 and 300 nM, respectively).[1] It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC50 values of less than 100 nM without inhibiting TNF-α expression in vitro.[3]

体内活性: TMI 1 inhibits LPS-induced TNF-α production in mice (ED50 = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED50s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.[3]

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

溶解度: DMSO : 35.9 mg/mL (410.4 mM)


关键字: WAY171318 | TMI1 | TMI-1 | TMI 1 | WAY 171318

相关产品: L-Cystathionine | ZNL 02-096 | Tanespimycin | NSC348884 | BML-277 | AFMK | BMS-202 | Hypericin | Solamargine | Ro-3306

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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