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
USD 320 In stock
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5 Customer Reviews

  • 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.

  • 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.

    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.

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 M2Xj[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHNVYNbUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEhzMkm5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMUWg{txO NXHxXmhXOTR3MkG0NlI>
HCT116 NXrr[JhNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEnzXJJKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO Mn7PNVQ2OjF2MkK=
HCT116 NYG3NmZoS3m2b4TvfIlkcXS7IHHzd4F6 NH3NWXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP NYXnWG1LOTd7NEG2NlU>
human mammary epithelial cells NETk[2NEgXSxdH;4bYNqfHliYYPzZZk> NFvHZ4ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP MkDKNVc6PDF4MkW=
HEK293 cells M2rIS2Z2dmO2aX;uJIF{e2G7 NX23VoZmUW6qaXLpeIlwdiCxZjDISGFEOSCrbjDISWszQTNiY3XscJMtKEmFNUC9NE4xODJ4IN88US=> M4P5XVE5OzB6NU[z
HeLa cells MmTvSpVv[3Srb36gZZN{[Xl? M1jQTFAvOyEQvF2= M3j4ZVE3KGh? Mk\PTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= M3rXRlE4QTV4OUi4
HCT116 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 MkPWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> MYCyNFIxPTN7NB?=
H1299 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 Mlr5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN M1X5bVIxOjB3M{m0
H460 cells MofLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFi3SJc1QCCq MlGwS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP NHfYZmgzOTB5M{G2NC=>
HCT116 cells Ml33S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPFVFZ2PDhiaB?= M3P5d2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF6IN88US=> MkjCNlExPzNzNkC=
CCRF-CEM cells MmfaVJJwdGmoZYLheIlwdiCjc4PhfS=> NIDubWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? M{\GRVIyPjJzOEiz
K562 cells NEHQXnNRem:uaX\ldoF1cW:wIHHzd4F6 NHi2ZnpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTVizszN MkXJNlE3OjF6OEO=
MOLT4 cells NI\EO|BRem:uaX\ldoF1cW:wIHHzd4F6 MmO3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN NELBclkzOTZ{MUi4Ny=>
SR cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 MkG4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj65PUDPxE1? M3PLNFIyPjJzOEiz
A549 cells M374VHBzd2yrZnXyZZRqd25iYYPzZZk> MkS2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA6KM7:TR?= MVOyNVYzOTh6Mx?=
EKVX cells NULPfVlnWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGL3UIlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFXLWngh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPzVizszN NV3mPIpZOjF4MkG4PFM>
HOP62 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 MofJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN NHT0PGkzOTZ{MUi4Ny=>
HOP92 cells Mn;KVJJwdGmoZYLheIlwdiCjc4PhfS=> M4fmS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QPVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTl7IN88US=> MYiyNVYzOTh6Mx?=
NCI-H226 cells NYruSYQ5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3rsWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO M13YUVIyPjJzOEiz
NCI-H23 cells MoXGVJJwdGmoZYLheIlwdiCjc4PhfS=> M3\KcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> Mof0NlE3OjF6OEO=
NCI-H322M cells NV\wbFJ3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGDYTWJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzJ{TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj6yOkDPxE1? MoGzNlE3OjF6OEO=
NCI-H460 cells NYTSb3J1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NV\tTZBVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? Mn:4NlE3OjF6OEO=
COLO205 cells NV3meYVTWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYHMOHlHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? M1flRlIyPjJzOEiz
HCT116 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN NVO0TGxiOjF4MkG4PFM>
HCT15 cells NELjZ29Rem:uaX\ldoF1cW:wIHHzd4F6 M3S2WGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvODdizszN M1PQT|IyPjJzOEiz
HT-29 cells M2jlZnBzd2yrZnXyZZRqd25iYYPzZZk> M3:yRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTZ4IN88US=> NIPBRo4zOTZ{MUi4Ny=>
KM12 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 NXHXe2dLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> MXeyNVYzOTh6Mx?=
SW620 cells NWjqbZNZWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ4QCEQvF2= NWfUXHF2OjF4MkG4PFM>
SF268 cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NXfBOW9sOjF4MkG4PFM>
SF295 cells M3\2VHBzd2yrZnXyZZRqd25iYYPzZZk> NX30WWxGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO NUXCXGxKOjF4MkG4PFM>
SF539 cells Mnu2VJJwdGmoZYLheIlwdiCjc4PhfS=> MmHjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkWzPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE46PjVizszN M2HrUVIyPjJzOEiz
SNB19 cells M13NOHBzd2yrZnXyZZRqd25iYYPzZZk> MnSwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= NF3RfnkzOTZ{MUi4Ny=>
SNB75 cells NWPlRZY2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVnMNGxkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmI4PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUig{txO NILhXFYzOTZ{MUi4Ny=>
U251 cells NFPyTZlRem:uaX\ldoF1cW:wIHHzd4F6 NEf1OohCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> NInVe2IzOTZ{MUi4Ny=>
LOXIMVI cells M1zGb3Bzd2yrZnXyZZRqd25iYYPzZZk> M1LUZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF;YTW1XUSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> M2TiXlIyPjJzOEiz
MALME-3M cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NHLxTFVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3BUG1GNTOPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkS2NUDPxE1? NV;oXmRjOjF4MkG4PFM>
M14 cells NIPzTnRRem:uaX\ldoF1cW:wIHHzd4F6 M1zqSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTUG0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlg1QSEQvF2= NX\MN5loOjF4MkG4PFM>
MDA-MB-435 cells MlXvVJJwdGmoZYLheIlwdiCjc4PhfS=> MoXDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? MknKNlE3OjF6OEO=
SK-MEL-28 cells NHPwN2pRem:uaX\ldoF1cW:wIHHzd4F6 NW\4dndpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= NGDP[3QzOTZ{MUi4Ny=>
SK-MEL-5 cells MlXBVJJwdGmoZYLheIlwdiCjc4PhfS=> NG\GNZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? NYTUVJRDOjF4MkG4PFM>
UACC257 cells M{LvPHBzd2yrZnXyZZRqd25iYYPzZZk> MoHTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDNlU4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN7MzFOwG0> M{X5NVIyPjJzOEiz
UACC62 cells NV7nTFY6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWDQ1O2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PzlizszN M4DDZVIyPjJzOEiz
IGROV1 cells MmfXVJJwdGmoZYLheIlwdiCjc4PhfS=> MlHZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCLR2LPWlEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTh5IN88US=> MY[yNVYzOTh6Mx?=
OVCAR3 cells NE\1eJJRem:uaX\ldoF1cW:wIHHzd4F6 MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= MWeyNVYzOTh6Mx?=
OVCAR4 cells MmnjVJJwdGmoZYLheIlwdiCjc4PhfS=> MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{4zOSEQvF2= NYfmTmNXOjF4MkG4PFM>
OVCAR5 cells MoXCVJJwdGmoZYLheIlwdiCjc4PhfS=> MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4zPiEQvF2= Mmf4NlE3OjF6OEO=
OVCAR8 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 NG\mU21CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NTFOwG0> NF\6XXMzOTZ{MUi4Ny=>
NCI/ADR-RES cells NV\zbIU1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NW\xOI91SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= MoH6NlE3OjF6OEO=
SKOV3 cells NGXpenJRem:uaX\ldoF1cW:wIHHzd4F6 M3;wW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> NFXD[HMzOTZ{MUi4Ny=>
786-0 cells M3jiSHBzd2yrZnXyZZRqd25iYYPzZZk> MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= NV3aUmtMOjF4MkG4PFM>
A498 cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 M3\6UmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= MXSyNVYzOTh6Mx?=
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Caki1 cells NHH5O4dRem:uaX\ldoF1cW:wIHHzd4F6 MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOja3mxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlYyQSEQvF2= NFfYc3MzOTZ{MUi4Ny=>
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TK10 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 Moj2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWS{GwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ1PCEQvF2= MVyyNVYzOTh6Mx?=
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PC3 cells NFf3VphRem:uaX\ldoF1cW:wIHHzd4F6 M37T[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yNEDPxE1? NEDLWY4zOTZ{MUi4Ny=>
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MCF7 cells NHvzfFdRem:uaX\ldoF1cW:wIHHzd4F6 NInac3VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvQTFizszN NW\zN5B{OjF4MkG4PFM>
MDA-MB-231 cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 NH[3N|lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUOxMlch|ryP MnnzNlE3OjF6OEO=
Hs 578T cells M{j4R3Bzd2yrZnXyZZRqd25iYYPzZZk> MoDURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKczC1O|hVKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF02Njh{IN88US=> M3fPSVIyPjJzOEiz
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T47D cells M4DnZ3Bzd2yrZnXyZZRqd25iYYPzZZk> NGX3TYRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI5NjhizszN M{PDU|IyPjJzOEiz
MDA-MB-468 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 M4G4fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? NHzHRWozOTZ{MUi4Ny=>
NCI-H226 cells MVPDfZRwfG:6aXPpeJkh[XO|YYm= NGq2R|BEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> M1PZN|IyPjJzOEiz
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SNB19 cells MnmwR5l1d3SxeHnjbZR6KGG|c3H5 M{LZcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPSjF7IHPlcIx{NCCOQ{WwQVMyNjdizszN MnKyNlE3OjF6OEO=
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LOXIMVI cells NFHxeI1EgXSxdH;4bYNqfHliYYPzZZk> NH7N[5VEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNV1iLTW\JJINmdGy|LDDMR|UxRTZwMESg{txO MXuyNVYzOTh6Mx?=
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SK-MEL-28 cells MkKxR5l1d3SxeHnjbZR6KGG|c3H5 NVniT3YxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzMEBNSzVyPUOxMlkh|ryP NVPBN4lLOjF4MkG4PFM>
SK-MEL-5 cells NHjpZVhEgXSxdH;4bYNqfHliYYPzZZk> MWnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyxiTFO1NF01NjB{IN88US=> NV3UeJNCOjF4MkG4PFM>
UACC257 cells MVjDfZRwfG:6aXPpeJkh[XO|YYm= MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{NCCOQ{WwQVQ1NjhizszN M4j0SlIyPjJzOEiz
UACC62 cells NWTJSVlZS3m2b4TvfIlkcXS7IHHzd4F6 M2LxOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> MXyyNVYzOTh6Mx?=
IGROV1 cells MonOR5l1d3SxeHnjbZR6KGG|c3H5 NWDjTWpHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO M13DclIyPjJzOEiz
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SKOV3 cells M4q3[2N6fG:2b4jpZ4l1gSCjc4PhfS=> M1fkO2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCOQ{WwQVI5NjVizszN NWP3Tm0{OjF4MkG4PFM>
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Caki1 cells M2\oRmN6fG:2b4jpZ4l1gSCjc4PhfS=> NEPSR2REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBE[WurMTDj[YxteyxiTFO1NF02Njd7IN88US=> NEHjV5YzOTZ{MUi4Ny=>
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HCT116 cells NUXLTWx{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= Mn\1NlE3PTB{MkG=
H1299 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|LDDJR|UxRTBwMTFOwG0> M1fsSFIyPjVyMkKx
HCT116 cells M4XiUHBzd2yrZnXyZZRqd25iYYPzZZk> NHfEc3FKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDIR3QyOTZiY3XscJMheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCxJO69VQ>? NHzDRWIyPDZzM{OxNi=>
RPMI8226 cells Mn\YVJJwdGmoZYLheIlwdiCjc4PhfS=> NGG5TGZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLQUWk5OjJ4IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWyN{DPxE1? NVzafW4xOjF4MkG4PFM>
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RXF393 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NWXEOI1FSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMEGg{txO NIjL[YszOTZ{MUi4Ny=>
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... 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

Bio Calculators

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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