Dacinostat (LAQ824)

For research use only.

Catalog No.S1095 Synonyms: NVP-LAQ824

18 publications

Dacinostat (LAQ824) Chemical Structure

CAS No. 404951-53-7

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

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Selleck's Dacinostat (LAQ824) has been cited by 18 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.

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Choose Selective HDAC Inhibitors

Biological Activity

Description Dacinostat (LAQ824, NVP-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 NFPrcVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoLqTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN M2XrVlE1PTJzNEKy
HCT116 NYG2WWNKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVn1UHM4UW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiFVEGxOkBpfW2jbjDjc4xwdiClZXzsJIdzd3e2aDygTWM2OD1yLkCxJO69VQ>? M{LvflE1PTJzNEKy
HCT116 MXPDfZRwfG:6aXPpeJkh[XO|YYm= NXrCSHFvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= MV:xO|k1OTZ{NR?=
human mammary epithelial cells NGnaT5FEgXSxdH;4bYNqfHliYYPzZZk> MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDtZY1u[XK7IHXwbZRp\WyrYXygZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUGg{txO MYWxO|k1OTZ{NR?=
HEK293 cells MUTGeY5kfGmxbjDhd5NigQ>? MmDmTY5pcWKrdHnvckBw\iCKRFHDNUBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6wNFI3KM7:TR?= NV73cVhoOTh|MEi1OlM>
HeLa cells MmrpSpVv[3Srb36gZZN{[Xl? MmDJNE4{KM7:TR?= NWDaSIlFOTZiaB?= MXfJcohq[mm2aX;uJI9nKEiGQVO0MY1m\GmjdHXkJJJmeHKnc4Ppc44hd2ZiTVXGNk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbjDpckBJ\UyjIHPlcIx{KGG2IECuN{B2VSCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 Mn\4NVc6PTZ7OEi=
HCT116 cells M1XuUnBzd2yrZnXyZZRqd25iYYPzZZk> NIG5fGFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO M4j2bFIxOjB3M{m0
H1299 cells NIjxZnRRem:uaX\ldoF1cW:wIHHzd4F6 MnHvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN MmP4NlAzODV|OUS=
H460 cells NECyNXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{\QdlQ5KGh? MXHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wO{DPxE1? MWWyNVA4OzF4MB?=
HCT116 cells MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHWOFghcA>? NWXEfYx5T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO NEDOVlEzOTB5M{G2NC=>
CCRF-CEM cells NWjDXodOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGPjTYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? MnLINlE3OjF6OEO=
K562 cells NXLQTHNpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkXHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU2KM7:TR?= MlnuNlE3OjF6OEO=
MOLT4 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 NWjwfWRlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MlHVNlE3OjF6OEO=
SR cells M{XqZnBzd2yrZnXyZZRqd25iYYPzZZk> NEDjRW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= MnS3NlE3OjF6OEO=
A549 cells NVjKVoh4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNFkh|ryP MYGyNVYzOTh6Mx?=
EKVX cells NFLQdGFRem:uaX\ldoF1cW:wIHHzd4F6 M33GWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= NEe5eY8zOTZ{MUi4Ny=>
HOP62 cells MmftVJJwdGmoZYLheIlwdiCjc4PhfS=> M{DHdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTB{IN88US=> M1;YdFIyPjJzOEiz
HOP92 cells NYr4ZppYWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUEmyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE6QSEQvF2= NYPYdJNIOjF4MkG4PFM>
NCI-H226 cells MmL3VJJwdGmoZYLheIlwdiCjc4PhfS=> NYexSW5xSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MT60NUDPxE1? MlrmNlE3OjF6OEO=
NCI-H23 cells NWj4RZpxWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVz2S|FbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO MUWyNVYzOTh6Mx?=
NCI-H322M cells MoDrVJJwdGmoZYLheIlwdiCjc4PhfS=> MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|IzVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5{NjFOwG0> MXqyNVYzOTh6Mx?=
NCI-H460 cells MlG4VJJwdGmoZYLheIlwdiCjc4PhfS=> MkD5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> M4nHclIyPjJzOEiz
COLO205 cells NULTUnJ5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHvEV|JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO Ml3CNlE3OjF6OEO=
HCT116 cells NXHyNVFoWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnPGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzR5IN88US=> M{LXT|IyPjJzOEiz
HCT15 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NFLKbVNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> NUHi[HJyOjF4MkG4PFM>
HT-29 cells NUXTXIpmWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVXyZXVwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO M4G0U|IyPjJzOEiz
KM12 cells NYXMTWpVWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWj5VnF[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> NYDBWpZ5OjF4MkG4PFM>
SW620 cells NHHv[ZFRem:uaX\ldoF1cW:wIHHzd4F6 NVH5PIlVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO MVOyNVYzOTh6Mx?=
SF268 cells NF35TYpRem:uaX\ldoF1cW:wIHHzd4F6 M4TFNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN MWWyNVYzOTh6Mx?=
SF295 cells NHPoPW1Rem:uaX\ldoF1cW:wIHHzd4F6 MlSzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK5OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE44PDNizszN MW[yNVYzOTh6Mx?=
SF539 cells NGfEXoxRem:uaX\ldoF1cW:wIHHzd4F6 M{niTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> NV3nbnJMOjF4MkG4PFM>
SNB19 cells NVLEToFJWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlvsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= NYXNbZVzOjF4MkG4PFM>
SNB75 cells MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 NVHyO5FNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmI4PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUig{txO M1n5VlIyPjJzOEiz
U251 cells MlvmVJJwdGmoZYLheIlwdiCjc4PhfS=> MlzyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NI[y[JczOTZ{MUi4Ny=>
LOXIMVI cells M3SwbXBzd2yrZnXyZZRqd25iYYPzZZk> NHjWfVVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO NYC1cZZSOjF4MkG4PFM>
MALME-3M cells NVrXc241WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2rCcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? NXzXO3plOjF4MkG4PFM>
M14 cells NU\He4VqWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIj5OnpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2xOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE45PDlizszN NYq3TmMxOjF4MkG4PFM>
MDA-MB-435 cells NYnXbJBzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2LNRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP M2P4V|IyPjJzOEiz
SK-MEL-28 cells M1u1eXBzd2yrZnXyZZRqd25iYYPzZZk> NXjVSHBnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= NHryb3UzOTZ{MUi4Ny=>
SK-MEL-5 cells MmfEVJJwdGmoZYLheIlwdiCjc4PhfS=> MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ5MTFOwG0> NWDJOYdnOjF4MkG4PFM>
UACC257 cells MnG5VJJwdGmoZYLheIlwdiCjc4PhfS=> M3PPR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO NIHVUmgzOTZ{MUi4Ny=>
UACC62 cells NFPGT3NRem:uaX\ldoF1cW:wIHHzd4F6 MnvqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> MkLrNlE3OjF6OEO=
IGROV1 cells NYTYSlhnWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN M{HZUFIyPjJzOEiz
OVCAR3 cells NWnReJRqWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2fFSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> M2ezW|IyPjJzOEiz
OVCAR4 cells NFSybo5Rem:uaX\ldoF1cW:wIHHzd4F6 NHq4O|VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> MonINlE3OjF6OEO=
OVCAR5 cells NF\ROGhRem:uaX\ldoF1cW:wIHHzd4F6 MmjRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOjZizszN MVOyNVYzOTh6Mx?=
OVCAR8 cells MorUVJJwdGmoZYLheIlwdiCjc4PhfS=> NYrafYhwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO MnXpNlE3OjF6OEO=
NCI/ADR-RES cells NVrLU4pWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF;NbopCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU9CTFJvUlXTJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE5KM7:TR?= NE\2bZczOTZ{MUi4Ny=>
SKOV3 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M1jNb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> M33sOlIyPjJzOEiz
786-0 cells M2jiUXBzd2yrZnXyZZRqd25iYYPzZZk> MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= NUjwc4Z1OjF4MkG4PFM>
A498 cells M2rxdnBzd2yrZnXyZZRqd25iYYPzZZk> M3P6[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NEjzR3ozOTZ{MUi4Ny=>
ACHN cells NFLGXJJRem:uaX\ldoF1cW:wIHHzd4F6 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? MXOyNVYzOTh6Mx?=
Caki1 cells M3fKW3Bzd2yrZnXyZZRqd25iYYPzZZk> NWPYTJl5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC54MUmg{txO NXzhXpNCOjF4MkG4PFM>
SN12C cells M2HDXXBzd2yrZnXyZZRqd25iYYPzZZk> NIXvWZZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPONVJEKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{Njl{IN88US=> MX[yNVYzOTh6Mx?=
TK10 cells MYTQdo9tcW[ncnH0bY9vKGG|c3H5 M2\lN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFuxNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PDRizszN M4HCb|IyPjJzOEiz
UO31 cells NFPEWZRRem:uaX\ldoF1cW:wIHHzd4F6 NY\Xd5MzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> NXO3XIJSOjF4MkG4PFM>
PC3 cells NVuyOZYzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWWzSHNDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= NWj3[3d5OjF4MkG4PFM>
DU145 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 M4nydGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI6NjlizszN MojnNlE3OjF6OEO=
MCF7 cells M{eyTnBzd2yrZnXyZZRqd25iYYPzZZk> NGDRWVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvQTFizszN MnHoNlE3OjF6OEO=
MDA-MB-231 cells MlvtVJJwdGmoZYLheIlwdiCjc4PhfS=> NH;YfZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUOxMlch|ryP NHXF[W8zOTZ{MUi4Ny=>
Hs 578T cells NFvSRXVRem:uaX\ldoF1cW:wIHHzd4F6 NGDM[odCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjzJFU4QFRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEKg{txO NHr4eFkzOTZ{MUi4Ny=>
BT549 cells NX;zcYlSWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1HVfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvODRizszN MnHvNlE3OjF6OEO=
T47D cells MlO1VJJwdGmoZYLheIlwdiCjc4PhfS=> NYrLdIlqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQC56IN88US=> MnSyNlE3OjF6OEO=
MDA-MB-468 cells MnnnVJJwdGmoZYLheIlwdiCjc4PhfS=> MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEig{txO NGfFTZAzOTZ{MUi4Ny=>
NCI-H226 cells MkixR5l1d3SxeHnjbZR6KGG|c3H5 MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyxiTFO1NF0zOCEQvF2= NF7CcmwzOTZ{MUi4Ny=>
KM12 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzMEBNSzVyPUK5Mlkh|ryP M3S5TVIyPjJzOEiz
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SNB19 cells MmL5R5l1d3SxeHnjbZR6KGG|c3H5 NVK3SGFHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06EMUmgZ4VtdHNuIFzDOVA:OzFwNzFOwG0> NFzwb2szOTZ{MUi4Ny=>
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LOXIMVI cells MkTqR5l1d3SxeHnjbZR6KGG|c3H5 M{j4SGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxQYEmPVlmgZ4VtdHNuIFzDOVA:Pi5yNDFOwG0> M1XpPVIyPjJzOEiz
MDA-MB-435 cells M2rqNmN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3KR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygUGM2OD1{OD64JO69VQ>? NEXBfmczOTZ{MUi4Ny=>
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SK-MEL-5 cells M3rHNGN6fG:2b4jpZ4l1gSCjc4PhfS=> NHPUS|lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? NFnPUnYzOTZ{MUi4Ny=>
UACC257 cells M1foWWN6fG:2b4jpZ4l1gSCjc4PhfS=> NV\WeZZjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? MWmyNVYzOTh6Mx?=
UACC62 cells Mke0R5l1d3SxeHnjbZR6KGG|c3H5 NELhWVBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFNkKgZ4VtdHNuIFzDOVA:Pi5|OTFOwG0> NU\td25MOjF4MkG4PFM>
IGROV1 cells MkjCR5l1d3SxeHnjbZR6KGG|c3H5 M3XtN2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGlIWk:YMTDj[YxteyxiTFO1NF01QC57IN88US=> M2e3cFIyPjJzOEiz
OVCAR5 cells M3S1emN6fG:2b4jpZ4l1gSCjc4PhfS=> NF7sZ|REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUkWgZ4VtdHNuIFzDOVA:OzhwOTFOwG0> M1HKRVIyPjJzOEiz
SKOV3 cells NXLUcnRMS3m2b4TvfIlkcXS7IHHzd4F6 M2rmXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCOQ{WwQVI5NjVizszN NWPTfYNSOjF4MkG4PFM>
A498 cells NXjWU2VPS3m2b4TvfIlkcXS7IHHzd4F6 NEDSSldEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDl6IHPlcIx{NCCOQ{WwQVUvQDhizszN NUfmTGI5OjF4MkG4PFM>
Caki1 cells NHvQcoJEgXSxdH;4bYNqfHliYYPzZZk> NULX[49nS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> M3\rR|IyPjJzOEiz
HCT116 cells Mn;HVJJwdGmoZYLheIlwdiCjc4PhfS=> NXLROXlwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEmFNUC9NE4xOTlizszN NU[5PYFNOjF5NEK0PVY>
HCT116 cells M1LFRXBzd2yrZnXyZZRqd25iYYPzZZk> M2LHemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> M3\0NFIyPjVyMkKx
H1299 cells NGHDZZdRem:uaX\ldoF1cW:wIHHzd4F6 MmLSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OD1yLkGg{txO M3rhb|IyPjVyMkKx
HCT116 cells NFjkNIFRem:uaX\ldoF1cW:wIHHzd4F6 NWrkN5FHUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgTGNVOTF4IHPlcIx{KHC{b3zp[oVz[XSrb36sJGlEPTB;MD6wNUDPxE1? MlvaNVQ3OTN|MUK=
RPMI8226 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MnTkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkOg{txO NXO0UldQOjF4MkG4PFM>
CHO cells MonnSpVv[3Srb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDlcIVkfHKxcHj5d4lwdG:peTDhd5NigSxiSVO1NF0yOi5{IN88US=> NGiyUpozODJyNUO5OC=>
HL-60(TB) cells NIn5R|FRem:uaX\ldoF1cW:wIHHzd4F6 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiOLU[wLHRDMSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NEmg{txO NXrFXpBPOjF4MkG4PFM>
RXF393 cells MlGxVJJwdGmoZYLheIlwdiCjc4PhfS=> M4SwZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmjGN|k{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjBzIN88US=> NVm3eIU4OjF4MkG4PFM>
RXF393 cells M1zYbmN6fG:2b4jpZ4l1gSCjc4PhfS=> MorER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN NIK5cpEzOTZ{MUi4Ny=>

... 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]
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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]
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  • 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]
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  • Animal Models: HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
  • 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):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
15 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
Smiles C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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