生物活性 | |||
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描述 | Histone deacetylases (HDAC) are enzymes that catalyze the removal of acetyl functional groups from the lysine residues of histones and non-histone proteins. HDAC inhibitors are a new class of anti-cancer agents that induce apoptosis and cell cycle arrest in cancer cells. CXD-101 is a class I-selective HDAC inhibitor that inhibits HDAC1, HDAC2, and HDAC3 with IC50 values of 63, 570, and 550nM, respectively, and had no activity against class II HDAC[1]. The IC50 values of CXD-101 in colon, lung, non-Hodgkin lymphoma, and myeloma cell lines ranged from 0.2 to 15μM. In murine lung (A549a) and colon (HT29) models, CXD-101 reduced tumor size at a dose of 50mg/kg, which was found to be associated with decreased HDAC enzyme activity and increased histone acetylation[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.48mL 0.50mL 0.25mL |
12.39mL 2.48mL 1.24mL |
24.78mL 4.96mL 2.48mL |
参考文献 |
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