LAQ824

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LAQ824 (Dacinostat) 是一种新型 HDAC 抑制剂，IC50 为 32 nM，已知可激活 p21 启动子。

LAQ824 (Dacinostat) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.(In Vitro):Dacinostat (NVP-LAQ824) activates p21 promoter, with AC50 of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC50s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC50s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4. Dacinostat inhibits HDAC1 with an IC50 of 9 nM. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC.(In Vivo):NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil.

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Dacinostat

Cell Cycle/DNA Damage

HDAC

HDAC

Cancer

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404951-53-7

379.46

C22H25N3O3

>98% (HPLC)

DMSO: 76 mg/mL (200.28 mM)

O=C(NO)/C=C/C1=CC=C(CN(CCO)CCC2=CNC3=C2C=CC=C3)C=C1

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

(-20℃)

With Ice Pack

≥ 2 years