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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-Dacinostat
Dacinostat

Chemical Structure : Dacinostat

CAS No.: 404951-53-7

Dacinostat (LAQ824, NVP-LAQ824)

货号: PC-49004Not For Human Use, Lab Use Only.

Dacinostat (NVP-LAQ824) is a potent histone deacetylase (HDAC) inhibitor with IC50 of 32 nM, transcriptionally activates the p21 promoter in reporter gene assays with AC50 of 0.3 uM.

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10 mg ¥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Dacinostat (NVP-LAQ824) is a potent histone deacetylase (HDAC) inhibitor with IC50 of 32 nM, transcriptionally activates the p21 promoter in reporter gene assays with AC50 of 0.3 uM.
LAQ824 (30 nM) resulted in a delayed (2 h) increase in reactive oxygen species (ROS), induction of p21(WAF1/CIP1), pRb dephosphorylation, growth arrest of cells in G(0)/G(1) phase, and differentiation in in human leukemia cells (U937 and Jurkat).
NVP-LAQ824 selectively inhibited growth of cancer cell lines at submicromolar levels after 48-72 h of exposure.
NVP-LAQ824 increased histone H3 and H4 acetylation level in cancer cell lines.
NVP-LAQ824 exhibited antitumor effects in a xenograft animal model.

物理化学性质&存储条件

分子量 379.5
分子式 C22H25N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2E)-N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-2-propenamide

参考文献

1. Jin JX, et al. Cell Physiol Biochem. 2017;41(3):1255-1266.

2. Roberto R Rosato, et al. Mol Pharmacol. 2006 Jan;69(1):216-25.

3. Atadja P, et al. Cancer Res. 2004 Jan 15;64(2):689-95.

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