1. Cell Cycle/DNA Damage
    Epigenetics
    Autophagy
  2. HDAC
    Autophagy
  3. Dacinostat

Dacinostat (Synonyms: NVP-LAQ824; LAQ824)

Cat. No.: HY-13606 Purity: >98.0%
Handling Instructions

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

For research use only. We do not sell to patients.

Dacinostat Chemical Structure

Dacinostat Chemical Structure

CAS No. : 404951-53-7

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Based on 1 publication(s) in Google Scholar

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Description

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

IC50 & Target[1][2]

HDAC1

9 nM (IC50)

HDAC

32 nM (IC50)

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[1]. Dacinostat inhibits HDAC1 with an IC50 of 9 nM[2]. 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[3].

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[1].

Molecular Weight

379.45

Formula

C₂₂H₂₅N₃O₃

CAS No.

404951-53-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 43 mg/mL (113.32 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[2]

The HDAC enzymatic assay measures compound activity in inhibiting purified HDAC isoforms. HDACs 1, 3, and 6 are immunopurified from 293 cells stably expressing the FLAG-tagged HDAC isoform, whereas HDACs 2, 4, 5, 7, 8, 9, 10, and 11 are purified from the baculovirus expression system. HDAC activity is measured in a fluorescent assay in which deacetylation of the substrate, bis-Boc-(Ac)Lys-rhodamine 110, generates a fluorophore that can be detected on a fluorometric plate reader[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cells are plated at 5000−10000 cells per well in 96-well plates and treated with eight serial compound dilutions. Cell viability following 72 h of compound treatment is measured using the CellTiter-Glo or MTS assay. XLfit 4 is used for plotting of the growth curves and calculation of IC50 values[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

The studies are performed on-site, using outbred athymic (nu/nu) female mice. Mice are anesthetized with Metofane, and a cell suspension (100 μL) containing 1×106 HCT116 cells is injected s.c. into the right axillary (lateral) region of each animal. Tumors are allowed to reach the volume of approximately 100-400 mm3. At this point, mice bearing tumors with acceptable morphology (non-necrotic) and of similar size range are selected and distributed into groups of six for the studies. NVP-LAQ824 is dissolved in DMSO to create a stock solution, which is further diluted just before dosing with D5W to a final DMSO concentration of 10%. Tumor-bearing mice are treated with the compound by i.v. injection into the tail vein. NVP-LAQ824 is dosed once daily, 5 days/week, for a total of 15 doses. 5-Fluorouracil is administered at 100 mg/kg in 0.9% saline 1 day/week for a total of three doses. The control groups are treated with the vehicle. Tumors are collected from the animals at the indicated time points[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: >98.0%

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Dacinostat
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