NCH-51
NCH-51 性质
| 熔点 | 127-128 °C(Solv: hexane (110-54-3); ethyl acetate (141-78-6)) |
|---|---|
| 密度 | 1.181±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 在DMSO中的溶解度为26mg/mL |
| 形态 | 白色粉末 |
| 酸度系数(pKa) | 9.52±0.50(Predicted) |
| 颜色 | 白色至米白色 |
NCH-51 用途与合成方法
|
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 . |
