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LAQ824 (NVP-LAQ824, Dacinostat)

LAQ824 (NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM.

Catalog No.S1095

4 Reviews 3 Product Citations

: Tel: +1-832-582-8158[email protected]

LAQ824 (NVP-LAQ824, Dacinostat) Chemical Structure
Molecular Weight: 379.459

Validation & Quality Control

Product Citations(3)

Nat Biotechnol, 2011, 29(3), 255-265

Diabetologia, 2012, 55(9):2421-31

Mol Pain, 2010, 6, 51

Customer Reviews(4) in vivo invitation

Western blot analysis of Acetyl-H3 and H3. 0-10μM LAQ824 was added.

Dr. Zhang of Tianjin Medical University. LAQ824 (NVP-LAQ824, Dacinostat) purchased from Selleck

Related Compound Libraries

LAQ824 (NVP-LAQ824, Dacinostat) is available in the following compound libraries:

Chemical Library (96-well) Epigenetics Compound Library (96-well) Inhibitor Library (96-well)

Product Information

Compare HDAC Inhibitors

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S1053	Entinostat (MS-275, SNDX-275)	<1 mg/mL	75 mg/mL	<1 mg/mL
S1047	Vorinostat (SAHA)	<1 mg/mL	53 mg/mL	3 mg/mL
S1030	Panobinostat (LBH589)	<1 mg/mL	70 mg/mL	<1 mg/mL
S3020	Romidepsin (FK228 ,depsipeptide)	<1 mg/mL	10 mg/mL	<1 mg/mL
S1045	Trichostatin A (TSA)	<1 mg/mL	23 mg/mL	<1 mg/mL
S1122	Mocetinostat (MGCD0103)	<1 mg/mL	13 mg/mL	<1 mg/mL
S2627	Tubastatin A HCl	<1 mg/mL	74 mg/mL	<1 mg/mL
S1085	Belinostat (PXD101)	<1 mg/mL	64 mg/mL	<1 mg/mL
S2170	ITF2357 (Givinostat)	<1 mg/mL	95 mg/mL	3 mg/mL
S1095	LAQ824 (NVP-LAQ824, Dacinostat)	<1 mg/mL	76 mg/mL	<1 mg/mL
S1194	CUDC-101	<1 mg/mL	20 mg/mL	<1 mg/mL
S1515	SB939 (Pracinostat)	<1 mg/mL	72 mg/mL	27 mg/mL
S2012	PCI-34051	<1 mg/mL	59 mg/mL	<1 mg/mL
S1422	Droxinostat	<1 mg/mL	49 mg/mL	49 mg/mL
S1484	MC1568	<1 mg/mL	13 mg/mL	<1 mg/mL
S1090	PCI-24781	<1 mg/mL	80 mg/mL	<1 mg/mL
S1096	JNJ-26481585	<1 mg/mL	79 mg/mL	<1 mg/mL
S1168	Valproic acid sodium salt (Sodium valproate)	33 mg/mL	33 mg/mL	33 mg/mL
S2818	CI994 (Tacedinaline)	<1 mg/mL	≥54 mg/mL	<1 mg/mL
S2244	AR-42 (HDAC-42)	<1 mg/mL	63 mg/mL	63 mg/mL
S2779	M344	<1 mg/mL	62 mg/mL	4 mg/mL
S2759	PI3K/HDAC InhibitorⅠ	<1 mg/mL	102 mg/mL	<1 mg/mL
S8001	Rocilinostat (ACY-1215)	<1 mg/mL	87 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	LAQ824 (NVP-LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM.
Targets	HDAC
IC50	32 nM ^[1]
In vitro	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. ^[1] 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. ^[2]
In vivo	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. ^[1]
Clinical Trials
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

In Vitro Histone Deacetylase Assay	HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl₂, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO₄, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-³²P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.

In Vitro Histone Deacetylase Assay

HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl₂, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO₄, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-³²P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.

Cell Assay: ^[1]

Cell lines	H1299, HCT116, DU145, PC3 and MDA435 cells
Concentrations	0-10 μM
Incubation Time	48 hours
Method	Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If X0, %Growth=(X-T₀)/T₀100; If X>T₀, %Growth=(X-T₀)/(GC-T₀)100. where T₀ is the average value of T₀ − background, GC is the average value of untreated cells (in triplicate) − background, and X is the average value of compound-treated cells (in triplicate)-background. The “% Growth” is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.

Animal Study: ^[1]

Animal Models	HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
Formulation	LAQ824 is dissolved in DMSO.
Dosages	≤100 mg/kg
Administration	Administered via i.v.

References

Chemical Information

Download LAQ824 (NVP-LAQ824, Dacinostat) SDF

Molecular Weight (MW)	379.459
Formula	C₂₂H₂₅N₃O₃
CAS No.	404951-53-7, 927176-79-2 (TFA)
Synonyms	N/A

Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name	(E)-3-(4-(((2-(1H-indol-3-yl)ethyl)(2-hydroxyethyl)amino)methyl)phenyl)-N-hydroxyacrylamide

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Research Area

Customer Reviews (4)

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Rating

Source

Molecular Pain , 2010, 6, 51. LAQ824 (NVP-LAQ824, Dacinostat) purchased from Selleck

Method

Paw withdrawal latency analysis

Cell Lines

C57BL/6NTac mice

Concentrations

8-200 ng

Incubation Time

30 min

Results

CFA-induced thermal hyperalgesia was significantly attenuated by all HDACIs, except for MS-275, in comparison to vehicle. Of these tested HDACIs, LAQ824 showed similar inhibitory effects between 40 and 200 ng suggesting saturation above 40 ng dosage.

Click to enlarge

Rating

Source

Diabetologia, 2012, 55(9), 2421-31.. LAQ824 (NVP-LAQ824, Dacinostat) purchased from Selleck

Method

Cell viability assay

Cell Lines

INS-1 cells

Concentrations

16-80 h

Incubation Time

Results

CI-994, PCI24781 and LAQ824 all protected against cytokine-induced beta cell death, whereas the HDAC8-selective inhibitor PCI34051 showed no protection.

Click to enlarge

Rating

Source

Diabetologia, 2012, 55, 2421–2431. LAQ824 (NVP-LAQ824, Dacinostat) purchased from Selleck

Method

Analyses of efficacy, potency and IC50

Cell Lines

INS-1 cells

Concentrations

Incubation Time

Results

HC toxin, CI-994, PCI24781 and LAQ824 all protected against cytokine-induced beta cell death, whereas the HDAC8-selective inhibitor PCI34051 showed no protection.

Click to enlarge

Rating

Source

Dr. Zhang of Tianjin Medical University. LAQ824 (NVP-LAQ824, Dacinostat) purchased from Selleck

Method

Western blot

Cell Lines

Concentrations

0.01-20 µM

Incubation Time

Results

LAQ824 treatment resulted in a reduction of Histone H3 acetylation.

Product Citations (3)

Chemoproteomics profiling of HDAC inhibitors reveals selective targeting of HDAC complexes. [Bantscheff M, et al. Nat Biotechnol 2011;29(3), 255-265]
PubMed: 21258344
Histone deacetylases 1 and 3 but not 2 mediate cytokine-induced beta cell apoptosis in INS-1 cells and dispersed primary islets from rats and are differentially regulated in the islets of type 1 diabetic children. [Lundh M, et al. Diabetologia 2012;55(9):2421-31]
PubMed: 22772764
Inhibition of class II histone deacetylases in the spinal cord attenuates inflammatory hyperalgesia. [Bai G,et al. Mol Pain 2010;6, 51]
PubMed: 20822541

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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LAQ824 (NVP-LAQ824, Dacinostat)