Dacinostat (LAQ824)

For research use only. Not for use in humans.

Catalog No.S1095 Synonyms: NVP-LAQ824

12 publications

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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Selleck's Dacinostat (LAQ824) has been cited by 12 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) 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 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIXEeYlKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> MoDHNVQ2OjF2MkK=
HCT116 MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXT1U2tWUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiFVEGxOkBpfW2jbjDjc4xwdiClZXzsJIdzd3e2aDygTWM2OD1yLkCxJO69VQ>? Mn3VNVQ2OjF2MkK=
HCT116 MmjPR5l1d3SxeHnjbZR6KGG|c3H5 NUf5fppoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= MnXONVc6PDF4MkW=
human mammary epithelial cells M1;yOGN6fG:2b4jpZ4l1gSCjc4PhfS=> NYrNdWpVS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdWGvbXHyfUBmeGm2aHXsbYFtKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF0yKM7:TR?= M{PCR|E4QTRzNkK1
HEK293 cells M1XOfWZ2dmO2aX;uJIF{e2G7 M37MfWlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= Mom4NVg{ODh3NkO=
HeLa cells M3\2OWZ2dmO2aX;uJIF{e2G7 MXywMlMh|ryP M4jZ[lE3KGh? MoHlTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= M1vURlE4QTV4OUi4
HCT116 cells MoXBVJJwdGmoZYLheIlwdiCjc4PhfS=> Ml;1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> MUGyNFIxPTN7NB?=
H1299 cells NGHWNXRRem:uaX\ldoF1cW:wIHHzd4F6 M4T1PWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> NUPZb3pHOjB{MEWzPVQ>
H460 cells MlHNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3rHU|Q5KGh? MYPHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wO{DPxE1? M3rLZ|IyODd|MU[w
HCT116 cells NWr4b41RT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV60PEBp Mke2S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN MUOyNVA4OzF4MB?=
CCRF-CEM cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 NHLmUXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? NHniOVYzOTZ{MUi4Ny=>
K562 cells NWPESXRLWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYLp[ohpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> NIG4bmczOTZ{MUi4Ny=>
MOLT4 cells NFjsfWZRem:uaX\ldoF1cW:wIHHzd4F6 MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGS0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyOSEQvF2= NFrDN4gzOTZ{MUi4Ny=>
SR cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{Lkm5JO69VQ>? NUHpS|A6OjF4MkG4PFM>
A549 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NEPpW2hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN MlzINlE3OjF6OEO=
EKVX cells NV3O[VFrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYLPXnpVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDFT3ZZKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjd3IN88US=> MVyyNVYzOTh6Mx?=
HOP62 cells NHnl[oxRem:uaX\ldoF1cW:wIHHzd4F6 NYnrSnZ2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MEKg{txO NH2yR4QzOTZ{MUi4Ny=>
HOP92 cells NGrKVoJRem:uaX\ldoF1cW:wIHHzd4F6 M3Lie2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QPVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTl7IN88US=> NYj0XHJVOjF4MkG4PFM>
NCI-H226 cells NHLmOJZRem:uaX\ldoF1cW:wIHHzd4F6 MkfrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> MYmyNVYzOTh6Mx?=
NCI-H23 cells M3W5eHBzd2yrZnXyZZRqd25iYYPzZZk> MoS4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN MYKyNVYzOTh6Mx?=
NCI-H322M cells NEnFdWJRem:uaX\ldoF1cW:wIHHzd4F6 NX:1UWtpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN{Ml2gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuNlYh|ryP M{LSV|IyPjJzOEiz
NCI-H460 cells MnL2VJJwdGmoZYLheIlwdiCjc4PhfS=> NUfqZ4RWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? NUTXelFYOjF4MkG4PFM>
COLO205 cells MoXGVJJwdGmoZYLheIlwdiCjc4PhfS=> NXziTVl7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? Mnr1NlE3OjF6OEO=
HCT116 cells NVzlOogxWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn7XRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzR5IN88US=> NFz5[3IzOTZ{MUi4Ny=>
HCT15 cells MlTwVJJwdGmoZYLheIlwdiCjc4PhfS=> MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= NXf5UlBiOjF4MkG4PFM>
HT-29 cells NGDLUZFRem:uaX\ldoF1cW:wIHHzd4F6 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU3PiEQvF2= NEfXVZIzOTZ{MUi4Ny=>
KM12 cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 NFPBU5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODRizszN NViyWIp2OjF4MkG4PFM>
SW620 cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ4QCEQvF2= Mlv2NlE3OjF6OEO=
SF268 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 NXrQUJNCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> NEjrRlczOTZ{MUi4Ny=>
SF295 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 M2HYOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yPVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzR|IN88US=> M4\HW|IyPjJzOEiz
SF539 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 NULWdXVpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlU{QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57NkWg{txO NFj0[5ozOTZ{MUi4Ny=>
SNB19 cells NG\pSmxRem:uaX\ldoF1cW:wIHHzd4F6 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= MUeyNVYzOTh6Mx?=
SNB75 cells M1j2ZXBzd2yrZnXyZZRqd25iYYPzZZk> M4nuNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> MU[yNVYzOTh6Mx?=
U251 cells M{PuTXBzd2yrZnXyZZRqd25iYYPzZZk> NXfhXWQySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> M1LMO|IyPjJzOEiz
LOXIMVI cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 MmfMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOT2jJUXZKKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> NWXF[5NpOjF4MkG4PFM>
MALME-3M cells M4[2[3Bzd2yrZnXyZZRqd25iYYPzZZk> NXf1V3VUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNRWxOTS1|TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD60OlEh|ryP NHf5OGszOTZ{MUi4Ny=>
M14 cells MmS1VJJwdGmoZYLheIlwdiCjc4PhfS=> NWPXVo12SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNNVQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQDR7IN88US=> M2XwN|IyPjJzOEiz
MDA-MB-435 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01OzViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUO3JO69VQ>? NYDPeINvOjF4MkG4PFM>
SK-MEL-28 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NXHVbINOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= MkX3NlE3OjF6OEO=
SK-MEL-5 cells MlLXVJJwdGmoZYLheIlwdiCjc4PhfS=> MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ5MTFOwG0> NHrJfpgzOTZ{MUi4Ny=>
UACC257 cells NHzOVZhRem:uaX\ldoF1cW:wIHHzd4F6 NYLoOHk3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkO5N{DPxE1? NGrrRYszOTZ{MUi4Ny=>
UACC62 cells M2\WbXBzd2yrZnXyZZRqd25iYYPzZZk> NGT5O|RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2M3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|N{mg{txO NIXrcG8zOTZ{MUi4Ny=>
IGROV1 cells NEPWOVNRem:uaX\ldoF1cW:wIHHzd4F6 NUHuPVV1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? NI\qT5UzOTZ{MUi4Ny=>
OVCAR3 cells NYDaTIxDWHKxbHnm[ZJifGmxbjDhd5NigQ>? M37CN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> NEfidGczOTZ{MUi4Ny=>
OVCAR4 cells NIXkVlVRem:uaX\ldoF1cW:wIHHzd4F6 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{4zOSEQvF2= NXXQZnlsOjF4MkG4PFM>
OVCAR5 cells NGLWW4tRem:uaX\ldoF1cW:wIHHzd4F6 NVmwdGtYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMk[g{txO NVWxU5dNOjF4MkG4PFM>
OVCAR8 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 M1rQeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> M3Hkb|IyPjJzOEiz
NCI/ADR-RES cells M1HFPHBzd2yrZnXyZZRqd25iYYPzZZk> M{nMT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJM2FFWi2URWOgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNVgh|ryP NGTFeIEzOTZ{MUi4Ny=>
SKOV3 cells NUDRc5dyWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml2yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN M33UflIyPjJzOEiz
786-0 cells NHXoOnJRem:uaX\ldoF1cW:wIHHzd4F6 NVzHdWc6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjC3PFYuOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5|ODFOwG0> MUOyNVYzOTh6Mx?=
A498 cells M3;0[3Bzd2yrZnXyZZRqd25iYYPzZZk> MojLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNEm4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEyKM7:TR?= NVTqXYd1OjF4MkG4PFM>
ACHN cells NGrN[|FRem:uaX\ldoF1cW:wIHHzd4F6 NEPQOZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFHDTG4h[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOSEQvF2= M4XONFIyPjJzOEiz
Caki1 cells Mm\VVJJwdGmoZYLheIlwdiCjc4PhfS=> MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOja3mxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlYyQSEQvF2= MYiyNVYzOTh6Mx?=
SN12C cells MmTQVJJwdGmoZYLheIlwdiCjc4PhfS=> MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQMULDJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zMlkzKM7:TR?= NWH4[4h{OjF4MkG4PFM>
TK10 cells M4SzOXBzd2yrZnXyZZRqd25iYYPzZZk> NXPxUVZbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> NYfEXmVTOjF4MkG4PFM>
UO31 cells M3PXeXBzd2yrZnXyZZRqd25iYYPzZZk> MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWRM{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFUzKM7:TR?= NXT2NJdwOjF4MkG4PFM>
PC3 cells MoXSVJJwdGmoZYLheIlwdiCjc4PhfS=> NVj4R2k1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= MYqyNVYzOTh6Mx?=
DU145 cells Ml64VJJwdGmoZYLheIlwdiCjc4PhfS=> NWL5S5RvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> NVzmVXZ7OjF4MkG4PFM>
MCF7 cells NGS3NlRRem:uaX\ldoF1cW:wIHHzd4F6 NUPES|BRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjlzIN88US=> NXXVbFF7OjF4MkG4PFM>
MDA-MB-231 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 NETUVY1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUOxMlch|ryP M17hdVIyPjJzOEiz
Hs 578T cells MoTuVJJwdGmoZYLheIlwdiCjc4PhfS=> M1LJVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIOgOVc5XCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:PS56MjFOwG0> M{\tZVIyPjJzOEiz
BT549 cells NVL4RYJEWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmLTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= M2jkR|IyPjJzOEiz
T47D cells M2GwSnBzd2yrZnXyZZRqd25iYYPzZZk> MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUK4Mlgh|ryP NYfoV2RsOjF4MkG4PFM>
MDA-MB-468 cells NXnPZ5U1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NFPzS2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12NkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUWuPFgh|ryP MWqyNVYzOTh6Mx?=
NCI-H226 cells NUCwWo4{S3m2b4TvfIlkcXS7IHHzd4F6 NILwVHFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> MljpNlE3OjF6OEO=
KM12 cells MnnXR5l1d3SxeHnjbZR6KGG|c3H5 MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzMEBNSzVyPUK5Mlkh|ryP M370ZVIyPjJzOEiz
SF295 cells NYD3[I9lS3m2b4TvfIlkcXS7IHHzd4F6 MmHuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= NWPsOldkOjF4MkG4PFM>
SNB19 cells MV\DfZRwfG:6aXPpeJkh[XO|YYm= NWGzeVVJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06EMUmgZ4VtdHNuIFzDOVA:OzFwNzFOwG0> MmfTNlE3OjF6OEO=
U251 cells MVPDfZRwfG:6aXPpeJkh[XO|YYm= MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzMEBNSzVyPUWuPFIh|ryP NVPoWZBzOjF4MkG4PFM>
LOXIMVI cells NIfYXItEgXSxdH;4bYNqfHliYYPzZZk> MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMU3hKVV[LIHPlcIx{NCCOQ{WwQVYvODRizszN NWHkfo9jOjF4MkG4PFM>
MDA-MB-435 cells NVjxb5RxS3m2b4TvfIlkcXS7IHHzd4F6 Mn7oR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygUGM2OD1{OD64JO69VQ>? NFz0UG4zOTZ{MUi4Ny=>
SK-MEL-28 cells NIOwSHREgXSxdH;4bYNqfHliYYPzZZk> MmjMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy|LDDMR|UxRTNzLkmg{txO NUDzZXV2OjF4MkG4PFM>
SK-MEL-5 cells NWjoXno1S3m2b4TvfIlkcXS7IHHzd4F6 M3r2PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD21JINmdGy|LDDMR|UxRTRwMEKg{txO M3PSTVIyPjJzOEiz
UACC257 cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{NCCOQ{WwQVQ1NjhizszN NF31cWQzOTZ{MUi4Ny=>
UACC62 cells M3frOWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2LFPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> MonrNlE3OjF6OEO=
IGROV1 cells MnHJR5l1d3SxeHnjbZR6KGG|c3H5 NIPpOFBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBKT1KRVkGgZ4VtdHNuIFzDOVA:PDhwOTFOwG0> M2nFOlIyPjJzOEiz
OVCAR5 cells MW\DfZRwfG:6aXPpeJkh[XO|YYm= NXv0Z5cxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO NHLhRXAzOTZ{MUi4Ny=>
SKOV3 cells NH24d4lEgXSxdH;4bYNqfHliYYPzZZk> MlX6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMtKEyFNUC9NlgvPSEQvF2= MVKyNVYzOTh6Mx?=
A498 cells MX7DfZRwfG:6aXPpeJkh[XO|YYm= MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzMEBNSzVyPUWuPFgh|ryP NGPkZoMzOTZ{MUi4Ny=>
Caki1 cells NXXVbIVDS3m2b4TvfIlkcXS7IHHzd4F6 MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{whVEN3ME21Mlc6KM7:TR?= NInnZoszOTZ{MUi4Ny=>
HCT116 cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 Mn7YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOsJGlEPTB;MD6wNVkh|ryP NW\Db5NiOjF5NEK0PVY>
HCT116 cells NGLQU|JRem:uaX\ldoF1cW:wIHHzd4F6 MofRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh\3Kxd4ToJIlvcGmkaYTpc44tKEmFNUC9NE4xOTlizszN NFTHV|gzOTZ3MEKyNS=>
H1299 cells NHzSPIJRem:uaX\ldoF1cW:wIHHzd4F6 NHOxW5ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzMEBKSzVyPUCuNUDPxE1? Ml\KNlE3PTB{MkG=
HCT116 cells M16xPHBzd2yrZnXyZZRqd25iYYPzZZk> Moe4TY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> NV3JTJltOTR4MUOzNVI>
RPMI8226 cells MWDQdo9tcW[ncnH0bY9vKGG|c3H5 MmHwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkOg{txO NIjzR4szOTZ{MUi4Ny=>
CHO cells M175bGZ2dmO2aX;uJIF{e2G7 M1rJdWlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO MoHjNlAzODV|OUS=
HL-60(TB) cells MkTtVJJwdGmoZYLheIlwdiCjc4PhfS=> M1HrOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFytOlApXEJrIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK0PUDPxE1? NWPNW4M{OjF4MkG4PFM>
RXF393 cells MkHZVJJwdGmoZYLheIlwdiCjc4PhfS=> MmX5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN MYmyNVYzOTh6Mx?=
RXF393 cells MmXTR5l1d3SxeHnjbZR6KGG|c3H5 MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMtKEyFNUC9NVUvOyEQvF2= Ml:1NlE3OjF6OEO=

... 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.
  • 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):
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 OCCN(CCC1=C[NH]C2=C1C=CC=C2)CC3=CC=C(\C=C\C(=O)NO)C=C3

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID