Dacinostat (LAQ824)

Catalog No.S1095 Synonyms: NVP-LAQ824

Dacinostat (LAQ824) Chemical Structure

Molecular Weight(MW): 379.459

Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.

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In DMSO USD 420 In stock
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Cited by 8 Publications

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  • Class I selective HDACi have the highest INS-1 rescue potential . INS-1 cells were monitored using the real-time xCELLigence system h and the impedance (cell adhesion) was measured as a surrogate of cell viability (cell index) as described in the Methods. (a ) The impedance of duplicates of control (green line), cytokine-exposed (red line) and cytokine+ITF-J-exposed INS-1 cells (blue line) was followed from the start of exposure (indicated by the arrow). Heat maps of 13 different ITF HDAC inhibitor compounds ( b )orsix different commercial HDAC inhibitor compounds (c) were made based on their IC50 values towards selected HDACs . The HDACi inhibitors are ranked after rescue potential according to ESM Tables 1, 2 .( c) Values are corrected for differences in potency since they varied from 33.3 (CI-994) to 0.041 (LAQ824). (d ) Colour code for both heat maps: low IC50 values coloured red, intermediate IC50 values coloured black and high IC50 values coloured blue; grey indicates undetermined IC50.

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

    Analyses of efficacy, potency and IC50 of HDAC inhibitors point toward HDACs 1–3 as relevant candidates for beta cell protection. Ranking and raw data on ITF drugs (Table 3) and commercial HDAC inhibitors (Table 4) underlying the heat maps of Fig. 1 (A and B). The HDAC inhibitor compounds were tested using a HDAC activity kit and recombinant proteins to determine IC50 values on each individual HDAC (right part of the table). Each drug was further tested using Real-Time Cell Analysis (RTCA) to score their maximal effective concentration (ECmax) as well as the corresponding rescue percentage of cytokine treated INS-1 cells. The drugs were ranked according to % rescue. * DMSO alone controls were included in each experiment, but not shown here. The results indicate that the highest concentrations of DMSO used here (1:1,000) were slightly potentiating the proliferation of the cells. The effects observed in this group of compounds were ascribed to the DMSO.?

    Diabetologia 2012 55(9), 2421-2431. Dacinostat (LAQ824) purchased from Selleck.

  • Mice received intrathecally injected vehicle or  LAQ824 at indicated dose 30 min before unilateral injection of CFA. Paw withdrawal latency was measured before injections as baseline, and after CFA injections as hyperalgesia response.

     

     

    Mol Pain 2010 6, 51. Dacinostat (LAQ824) purchased from Selleck.

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

     

     

    2010 Dr. Zhang of Tianjin Medical University. Dacinostat (LAQ824) purchased from Selleck.

  • Levels of H3K9, H4K12, and 5-mC in blastocyst stage embryos. (A) Immunofluorescence staining at the blastocyst stage of H3K9, H4K12, and 5-mC (green) in the control group and after 100 nM LAQ824 treatment for 24 h post-activation. Each sample was counterstained with propidium iodide (PI) to visualize DNA (red). Merged images of H3K9, H4K12, and 5-mC and DNA staining are shown. The merged images of H3K9 and DNA are yellow. Scale bar indicates 50 μm. (B) Quantifications of H3K9, H4K12, and 5-mC are represented by signal intensities per group. Fluorescence intensity was measured using Image J software 1.46r. Bars and error bars show mean values and SEM, respectively.

    Cell Physiol Biochem, 2017, 41(3):1255-1266. Dacinostat (LAQ824) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
Targets
HDAC [1]
(Cell-free assay)
32 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1299 NE\TfWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmnXTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN NXHNS41sOTR3MkG0NlI>
HCT116 M33VNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTGNVOTF4IHj1cYFvKGOxbH;uJINmdGxiZ4Lve5RpNCCLQ{WwQVAvODFizszN NGG4ZoQyPDV{MUSyNi=>
HCT116 NEnPXmREgXSxdH;4bYNqfHliYYPzZZk> NVzVblRGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= MXexO|k1OTZ{NR?=
human mammary epithelial cells NVjjNmlZS3m2b4TvfIlkcXS7IHHzd4F6 MlWxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NIrafnUyPzl2MU[yOS=>
HEK293 cells NYTkfJFmTnWwY4Tpc44h[XO|YYm= NHq1fXlKdmirYnn0bY9vKG:oIFjERWMyKGmwIFjFT|I6OyClZXzsd{whUUN3ME2wMlAxOjZizszN NH;QUXQyQDNyOEW2Ny=>
HeLa cells NV7CNoFNTnWwY4Tpc44h[XO|YYm= MX6wMlMh|ryP MUGxOkBp NUDjO49oUW6qaXLpeIlwdiCxZjDISGFEPC2vZXTpZZRm\CC{ZYDy[ZN{cW:wIH;mJG1GTjJvZHXw[Y5l\W62IITyZY5{[3KrcITpc44hcW5iSHXMZUBk\WyuczDheEAxNjNidV2gZYZ1\XJiMU[gbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NXvObFBFOTd7NU[5PFg>
HCT116 cells NYrob2hDWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4xOTNizszN NXL2S5ZTOjB{MEWzPVQ>
H1299 cells MlTrVJJwdGmoZYLheIlwdiCjc4PhfS=> NETYSGdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjF4MTFOwG0> MVeyNFIxPTN7NB?=
H460 cells NW\RdmZpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TIdVQ5KGh? NVTie2FCT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUDR4MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODdizszN NGrmPIQzOTB5M{G2NC=>
HCT116 cells NWPYbppGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3XncVQ5KGh? NXnTOIxCT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO M4To[|IyODd|MU[w
CCRF-CEM cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 Mk[0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQ2LGMWNGVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NUGg{txO M17iXlIyPjJzOEiz
K562 cells NHfaTYZRem:uaX\ldoF1cW:wIHHzd4F6 MoPiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU2KM7:TR?= NV;OOJAyOjF4MkG4PFM>
MOLT4 cells NHHnWpFRem:uaX\ldoF1cW:wIHHzd4F6 M{C1WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MWFQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzFzIN88US=> M{jzbVIyPjJzOEiz
SR cells MU\Qdo9tcW[ncnH0bY9vKGG|c3H5 NF3iSXpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= MmO0NlE3OjF6OEO=
A549 cells M{n2cHBzd2yrZnXyZZRqd25iYYPzZZk> M3nXZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= M2LJd|IyPjJzOEiz
EKVX cells M4Gzd3Bzd2yrZnXyZZRqd25iYYPzZZk> MnHqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHS2\YJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlc2KM7:TR?= NYC2VFhkOjF4MkG4PFM>
HOP62 cells NUHjbYdKWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXnYVGNESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MEKg{txO NGjOS44zOTZ{MUi4Ny=>
HOP92 cells M4rtXnBzd2yrZnXyZZRqd25iYYPzZZk> M{HlOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QPVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTl7IN88US=> MkDHNlE3OjF6OEO=
NCI-H226 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> MV[yNVYzOTh6Mx?=
NCI-H23 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 MoruRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN NYnsWpJQOjF4MkG4PFM>
NCI-H322M cells NEjiO2pRem:uaX\ldoF1cW:wIHHzd4F6 MkTORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO MVuyNVYzOTh6Mx?=
NCI-H460 cells M{KzSHBzd2yrZnXyZZRqd25iYYPzZZk> NHvTdJBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkeg{txO MV6yNVYzOTh6Mx?=
COLO205 cells MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 MlHoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> M1zOfVIyPjJzOEiz
HCT116 cells M2\GUnBzd2yrZnXyZZRqd25iYYPzZZk> NYr5U2d7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{S3JO69VQ>? NEOzN3YzOTZ{MUi4Ny=>
HCT15 cells NYroS3BpWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEDsO5VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> MmTZNlE3OjF6OEO=
HT-29 cells NUPQN4s5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUDTW2RRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO MkW0NlE3OjF6OEO=
KM12 cells Mlz0VJJwdGmoZYLheIlwdiCjc4PhfS=> MlXvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= NWT1Z5U2OjF4MkG4PFM>
SW620 cells NYHOPHl{WHKxbHnm[ZJifGmxbjDhd5NigQ>? M4nJ[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDd6IN88US=> MlT5NlE3OjF6OEO=
SF268 cells NGq1dHhRem:uaX\ldoF1cW:wIHHzd4F6 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= MnT3NlE3OjF6OEO=
SF295 cells NVfqSHEyWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= MnzlNlE3OjF6OEO=
SF539 cells NFHIV2FRem:uaX\ldoF1cW:wIHHzd4F6 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOINUO5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk3PSEQvF2= MUOyNVYzOTh6Mx?=
SNB19 cells M2LrTHBzd2yrZnXyZZRqd25iYYPzZZk> MlvLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= MYOyNVYzOTh6Mx?=
SNB75 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= MoPvNlE3OjF6OEO=
U251 cells NH3rUo9Rem:uaX\ldoF1cW:wIHHzd4F6 MnTxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NHLzSo0zOTZ{MUi4Ny=>
LOXIMVI cells NWe5WGY2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIC1PWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO MW[yNVYzOTh6Mx?=
MALME-3M cells NUD2[WtZWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> NVzUVVE1OjF4MkG4PFM>
M14 cells M4XEPHBzd2yrZnXyZZRqd25iYYPzZZk> MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1zNDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD64OFkh|ryP M{jQWFIyPjJzOEiz
MDA-MB-435 cells NYO2OZVKWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIrkNmRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVM4KM7:TR?= NULlVJdPOjF4MkG4PFM>
SK-MEL-28 cells NXvMUmNUWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE0zQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57OUOg{txO NX3jeZVUOjF4MkG4PFM>
SK-MEL-5 cells M1u1N3Bzd2yrZnXyZZRqd25iYYPzZZk> M1;ac2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkexJO69VQ>? MXGyNVYzOTh6Mx?=
UACC257 cells NH7qenBRem:uaX\ldoF1cW:wIHHzd4F6 M4HSZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO NGf4dFMzOTZ{MUi4Ny=>
UACC62 cells Mnq5VJJwdGmoZYLheIlwdiCjc4PhfS=> MnfvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> MYSyNVYzOTh6Mx?=
IGROV1 cells MoXoVJJwdGmoZYLheIlwdiCjc4PhfS=> NIjPSJdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFnHVm9XOSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5zOEeg{txO M2nuOVIyPjJzOEiz
OVCAR3 cells M{nRT3Bzd2yrZnXyZZRqd25iYYPzZZk> NVrRSFV3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMUGg{txO MXmyNVYzOTh6Mx?=
OVCAR4 cells MnT6VJJwdGmoZYLheIlwdiCjc4PhfS=> NFXLRYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> M3K4blIyPjJzOEiz
OVCAR5 cells Mn7HVJJwdGmoZYLheIlwdiCjc4PhfS=> MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4zPiEQvF2= NXrJeYg3OjF4MkG4PFM>
OVCAR8 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NXHMWpJJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO NGnLcY8zOTZ{MUi4Ny=>
NCI/ADR-RES cells M33n[nBzd2yrZnXyZZRqd25iYYPzZZk> NVHqPJgzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= M4e5OVIyPjJzOEiz
SKOV3 cells M2HySXBzd2yrZnXyZZRqd25iYYPzZZk> MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUzPCEQvF2= M{Hre|IyPjJzOEiz
786-0 cells M1HkT3Bzd2yrZnXyZZRqd25iYYPzZZk> M{H3XGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN MV6yNVYzOTh6Mx?=
A498 cells M2q0fXBzd2yrZnXyZZRqd25iYYPzZZk> NVL4V|lNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> MWiyNVYzOTh6Mx?=
ACHN cells M4XmbXBzd2yrZnXyZZRqd25iYYPzZZk> M2rWZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= NXHpOJppOjF4MkG4PFM>
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TK10 cells NHK5XpBRem:uaX\ldoF1cW:wIHHzd4F6 MlO4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWS{GwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ1PCEQvF2= Mkm1NlE3OjF6OEO=
UO31 cells Mn\2VJJwdGmoZYLheIlwdiCjc4PhfS=> NEXzfFVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXPN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDV{IN88US=> NHiyO48zOTZ{MUi4Ny=>
PC3 cells M3Hu[nBzd2yrZnXyZZRqd25iYYPzZZk> NUn0SW5iSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= MXeyNVYzOTh6Mx?=
DU145 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yPU46KM7:TR?= NYX4XlZUOjF4MkG4PFM>
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MDA-MB-231 cells M1vzfHBzd2yrZnXyZZRqd25iYYPzZZk> M33GRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{GuO{DPxE1? M3P1dVIyPjJzOEiz
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BT549 cells NF;zR4ZRem:uaX\ldoF1cW:wIHHzd4F6 MkDERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= MlvsNlE3OjF6OEO=
T47D cells NHrpXnpRem:uaX\ldoF1cW:wIHHzd4F6 M4\JOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlgvQCEQvF2= NHzKbFQzOTZ{MUi4Ny=>
MDA-MB-468 cells MoPIVJJwdGmoZYLheIlwdiCjc4PhfS=> MnH5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDZ6IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13Lki4JO69VQ>? MYCyNVYzOTh6Mx?=
NCI-H226 cells M1PW[GN6fG:2b4jpZ4l1gSCjc4PhfS=> M{\ieGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KMkK2JINmdGy|LDDMR|UxRTJyIN88US=> NWroTJBmOjF4MkG4PFM>
KM12 cells MVPDfZRwfG:6aXPpeJkh[XO|YYm= NXG3UZhTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU01zMjDj[YxteyxiTFO1NF0zQS57IN88US=> MVuyNVYzOTh6Mx?=
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LOXIMVI cells MXLDfZRwfG:6aXPpeJkh[XO|YYm= NHz3O5dEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNV1iLTW\JJINmdGy|LDDMR|UxRTZwMESg{txO NGnmV|MzOTZ{MUi4Ny=>
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SK-MEL-5 cells NE\ufWVEgXSxdH;4bYNqfHliYYPzZZk> NIDm[pJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? NHfXdIMzOTZ{MUi4Ny=>
UACC257 cells NHnYZXZEgXSxdH;4bYNqfHliYYPzZZk> MYrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{NCCOQ{WwQVQ1NjhizszN M2HL[lIyPjJzOEiz
UACC62 cells M4\QO2N6fG:2b4jpZ4l1gSCjc4PhfS=> M4nrSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> Mn[xNlE3OjF6OEO=
IGROV1 cells NVj5WW1QS3m2b4TvfIlkcXS7IHHzd4F6 M2DCSmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGlIWk:YMTDj[YxteyxiTFO1NF01QC57IN88US=> Mlj2NlE3OjF6OEO=
OVCAR5 cells Mn3RR5l1d3SxeHnjbZR6KGG|c3H5 M{G5b2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUNTDj[YxteyxiTFO1NF0{QC57IN88US=> NYLZdXpoOjF4MkG4PFM>
SKOV3 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= MlLGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMtKEyFNUC9NlgvPSEQvF2= MY[yNVYzOTh6Mx?=
A498 cells Mm\zR5l1d3SxeHnjbZR6KGG|c3H5 NXjINmRFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyxiTFO1NF02Njh6IN88US=> MlLiNlE3OjF6OEO=
Caki1 cells NV;SV|kyS3m2b4TvfIlkcXS7IHHzd4F6 MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{whVEN3ME21Mlc6KM7:TR?= MmXjNlE3OjF6OEO=
HCT116 cells NXW1eIo6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2rjWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= NUToN|NkOjF5NEK0PVY>
HCT116 cells Mm\XVJJwdGmoZYLheIlwdiCjc4PhfS=> M1v6T2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> MVSyNVY2ODJ{MR?=
H1299 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NYLOSYdiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{whUUN3ME2wMlEh|ryP M17aWVIyPjVyMkKx
HCT116 cells NV7KfY46WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIjOVWhKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDIR3QyOTZiY3XscJMheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCxJO69VQ>? M4S4RlE1PjF|M{Gy
RPMI8226 cells MnnSVJJwdGmoZYLheIlwdiCjc4PhfS=> M3K0dmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? NFHmTokzOTZ{MUi4Ny=>
CHO cells NUW0enpoTnWwY4Tpc44h[XO|YYm= NXLaU5dIUW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDheZRwdWG2ZXSgdIF1[2hiY3zhcZAh\WynY4Tyc5BpgXOrb3zv[5kh[XO|YYmsJGlEPTB;MUKuNkDPxE1? NGqzOGQzODJyNUO5OC=>
HL-60(TB) cells NX\ydoFLWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHXsS3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMMVYxMFSEKTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOFkh|ryP NV\GeIFDOjF4MkG4PFM>
RXF393 cells NIXuV2tRem:uaX\ldoF1cW:wIHHzd4F6 Mn7kRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN MVWyNVYzOTh6Mx?=
RXF393 cells NEflPWxEgXSxdH;4bYNqfHliYYPzZZk> M{XKZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJZTjN7MzDj[YxteyxiTFO1NF0yPS5|IN88US=> NWrTT|I6OjF4MkG4PFM>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:[1]
+ Expand

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 Research:[1]
+ Expand
  • 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)/T0*100; 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.28 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 379.459
Formula

C22H25N3O3

CAS No. 404951-53-7
Storage powder
in solvent
Synonyms NVP-LAQ824

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Tech Support

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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID