HDAC-IN-51 是一种有效的组蛋白脱乙酰酶 (HDAC) 抑制剂，对 HDAC10、HDAC1、HDAC2、 HDAC3 和 HDAC11 的IC50值分别为 0.32、0.353、0.431、0.515 和 85.4 μM。HDAC-IN-51 诱导细胞周期停滞和细胞凋亡，调节细胞周期/细胞凋亡相关的 miRNA 表达。HDAC-IN-51 可用于癌症研究。
| 生物活性 | HDAC-IN-51 is a potenthistone deacetylase (HDAC)inhibitor withIC50values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM forHDAC10,HDAC1,HDAC2,HDAC3andHDAC11, respectively. HDAC-IN-51 induces cell cycle arrest andapoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research ofcancer[1]. |
| IC50& Target[1] | HDAC10 0.32 μM (IC50) | HDAC1 0.353 μM (IC50) | HDAC2 0.431 μM (IC50) | HDAC3 0.515 μM (IC50) | HDAC11 85.4 μM (IC50) |
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体外研究
(In Vitro) | HDAC-IN-51 (compound 8d; 1 nM-10 μM; 48 h) 具有抗增殖活性，对 K562、HCT116 和 A549 细胞的 IC50值分别为 0.54、0.56 和 1.35 μM[1].
HDAC-IN-51 (1 and 5 μM; 24 and 48 h; U937 白血病细胞) 使细胞周期停滞在 G1 期[1]。
HDAC-IN-51 (1 and 5 μM; 48 h; U937 细胞) 诱导细胞凋亡并下调具有抗细胞凋亡活性的 miRNA（miR-17-5p、miR-18-5p、miR-19b-3p、miR-20a- 5p 和 miR-21-5p)[1]。
HDAC-IN-51 (1 and 5 μM; 48 h; U937 细胞) 增加 p21、BAX 和 BAK 的 mRNA 表达，下调细胞周期蛋白 D1 和 BCL-2[1]。
Cell Viability Assay[1] | Cell Line: | K562, HCT116, and A549 cells | | Concentration: | 1 nM-10 μM | | Incubation Time: | 48 hours | | Result: | Inhibited cell growth in cancer cells. |
Cell Cycle Analysis[1] | Cell Line: | U937 leukaemia cells | | Concentration: | 1 and 5 μM | | Incubation Time: | 24 and 48 hours | | Result: | Blocked the cell cycle at the G1 phase in U937 leukaemia cells. |
Western Blot Analysis[1] | Cell Line: | U937 cells | | Concentration: | 1 and 5 μM | | Incubation Time: | 48 hours | | Result: | Down-regulates miRNAs with antiapoptotic activity including miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p. |
Western Blot Analysis[1] | Cell Line: | U937 cells | | Concentration: | 1 and 5 μM | | Incubation Time: | 48 hours | | Result: | Increased mRNA expression of p21, BAX and BAK and down-regulated cyclin D1 and BCL-2 in a dose-dependent manner. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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