NCH-51
| 中文名称 | NCH-51 |
|---|---|
| 中文同义词 | 化合物PTACH;S-[7-氧代-7-[(4-苯基-1,3-噻唑-2-基)氨基]庚基]-2-甲基丙硫酸酯;NCH 51,新型HDAC抑制剂 |
| 英文名称 | PTACH |
| 英文同义词 | Cpd 51, S-[6-(4-Phenyl-2-thiazolylcarbamoyl)hexyl] thioisobutyrate;2-MethylpropanethioicacidS-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl]ester;S-(7-Oxo-7-((4-phenylthiazol-2-yl)amino)-heptyl) 2-methylpropanethioate;PTACH (NCH-51);HDAC Inhibitor XXII, NCH51;Propanethioic acid,2-methyl-, S-[7-oxo-7-[(4-phenyl-2-thiazolyl)amino]heptyl] ester;NCH51, >98%;PTACH?, >98% |
| CAS号 | 848354-66-5 |
| 分子式 | C20H26N2O2S2 |
| 分子量 | 390.56 |
| EINECS号 | |
| 相关类别 | 标准品 |
| Mol文件 | 848354-66-5.mol |
| 结构式 |  |
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) |
|
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 . |