产品信息
抗原名称
HDAC
商品描述
Dacinostat (NVP-LAQ824, LAQ824) is a highly potent HDAC inhibitor with IC50 of 32 nM.
分子量
379.46
纯度
>98%
可溶性
DMSO 76 mg/mL (200.28 mM)
外观
Powder
In vitro(体外研究)
LAQ824 activates the expression of the gene encoding the p21 cell cycle inhibitor by activating the p21 promoter with 50% of the maximal promoter activation (AC50) of 0.30 μM. LAQ824 inhibits the cell growth of both H1299, a non-small cell lung carcinoma line, and HCT116, a colon cancer cell line with IC50 of 0.15 μM and 0.01 μM, respectively, and the antiproliferative effect of LAQ824 is selective toward the tumor cell lines while inducing only growth arrest in normal fibroblasts. Furthermore, LAQ824 induces a dose-dependent increase of p21 protein in A549 cells and an increase in the hypophosphorylated state of the Rb tumor suppressor. A recent study shows that LAQ824 induces chromatin changes at the level of the IL-10 gene promoter that lead to enhanced recruitment of the transcriptional repressors HDAC11 and PU.1 and inhibits IL-10 production in BALB/c murine macrophages.
In vivo(体内研究)
In HCT116 and human colon tumor xenografts in nude mice, LAQ824 treatment at 100 mg/kg produces the inhibitory effects on tumor growth in a dose-dependent mode without general cytotoxicity.
背景
别名
NVP-LAQ824; LAQ824; LAQ 824; LAQ-824
分子式
C22H25N3O3
CAS号
404951-53-7
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
本文来自投稿，不代表本人立场，如若转载，请注明出处：http://www.iamyjet.com/article/13856.html