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编 号:F762903
分子式:C27H24N4O2
分子量:436.51
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生物活性:
HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10, HDAC1, HDAC2, HDAC3 and HDAC11, respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis, modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer.

体外研究:
HDAC-IN-51 (compound 8d; 1 nM-10 μM; 48 h) has antiproliferative activity with IC50 values of 0.54, 0.56, and 1.35 μM for K562, HCT116, and A549 cells, respectively.HDAC-IN-51 (1 and 5 μM; 24 and 48 h; U937 leukaemia cells) arrests cell cycle at the G1 phase.HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) induces apoptosis and down-regulates miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p).HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) increases mRNA expression of p21, BAX and BAK, down-regulates cyclin D1 and BCL-2.
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