HDAC1 48 nM (IC 50 ) HDAC4 32 nM (IC 50 ) HDAC6 41 nM (IC 50 ) HIV-1

PTACH (compound 51) treatment elevates the levels of acetylated histone H4 and p21 WAF1/CIP1 in a dose-dependent manner. In cancer cell growth inhibition assay, PTACH (compound 51) shows strong activity. PTACH inhibits various cancer cells with EC50 values of 2.3 μM, 9.1 μM, 3.0 μM, 2.6 μM, 1.1 μM, 4.5 μM, 2.4 μM, 5.0 μM, and 4.5 μM for MDA-MB-231, SNB-78, HCT116, NCI-H226, LOX-IMVI, SK-OV-3, RXF-631L, St-4, and DU-145 cells, respectively. PTACH (NCH-51) augments the HIV-1 production in latently infected OM10.1 cells and such reactivation is associated with a loss of HDAC1 occupancy and subsequent hyperacetylation of histones in nuc-1 at the HIV-1 promoter. Western Blot Analysis Cell Line: HCT 116 cells Concentration: 1 μM, 5 μM, 25 μM Incubation Time: 8 hours Result: Gave rise to elevated and dose-dependent levels of acetylated histone H4 and p21 WAF1/CIP1 .

PTACH (NCH-51) 是一种有效的 HDAC 抑制剂，对 HDAC1，HDAC4 和 HDAC6 的 IC50 分别为 48 nM，32 nM 和 41 nM。PTACH 对多种癌细胞具有强大的生长抑制作用 (EC50 为 1.1-9.1 µM)。