Name | tapi-2 |
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Description | (R)-TAPI-2 is the isomer of TAPI-2 (HY-100211A). TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP[1]. TAPI-2 blocks the entry of infectious SARS-CoV[2]. |
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Related Catalog | |
In Vitro | 基于 hydroxamate 的金属蛋白酶抑制剂 TAPI-2 与 hmeprin 结合,hmeprin β 亚基的抑制常数 IC50 为 20±10 μM,hmeprin α 为 1.5±0.27 nM 亚基。通常,hmeprin α 比 β 亚基 受到更强烈的抑制[1]。 在不影响 ADAM17 表达的情况下,TAPI-2 会显着降低 HCP-1 和 HT29 细胞中 NICD 及其下游靶标 HES-1 的蛋白质水平。此外,在两种 CRC 细胞系中,用 TAPI-2 处理细胞可显著降低 50% 的 CSC 表型。TAPI-2 对 NICD 和 HES-1 的球形成和蛋白水平的剂量依赖性证实,所使用的浓度 (20 μM) 在 TAPI-2 的有效剂量范围 (5-40 μM) 内[3]。 |
Cell Assay | TAPI-2 is dissolved in DMSO and diluted with appropriate medium before use. All experiments are performed using 20 μM TAPI-2. Cells are cultured with or without TAPI-2 for 48 hours and then seeded at 3,000 cells per well in 96-well plates. After pretreatment, increasing doses of 5-fluorouracil (5-FU) that are relevant to the recommended clinical dose (up to 2 μg/mL) are added, with or without TAPI-2, for 72 hours. Cell viability is assessed by adding MTT substrate (0.25% in phosphate-buffered saline [PBS]) in growth medium (1:5 dilution) to cells for 1 hour at 37°C. The cells are ished with PBS, and 100 μL of dimethyl sulfoxideis added. Optical density is measured at 570 nM, and relative MTT is presented as a percentage of control[3]. |
References |
Molecular Formula | C19H37N5O5 |
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Molecular Weight | 415.53 |
Exact Mass | 415.27900 |
PSA | 162.65000 |
LogP | 1.91860 |
RIDADR | NONH for all modes of transport |
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