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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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.

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 NIf0T2xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmXMTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN MUmxOFUzOTR{Mh?=
HCT116 M3XsTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NY\wdYljUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiFVEGxOkBpfW2jbjDjc4xwdiClZXzsJIdzd3e2aDygTWM2OD1yLkCxJO69VQ>? NYXMPG16OTR3MkG0NlI>
HCT116 NGezcnpEgXSxdH;4bYNqfHliYYPzZZk> NHXDVodEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP Ml:1NVc6PDF4MkW=
human mammary epithelial cells NEexT2tEgXSxdH;4bYNqfHliYYPzZZk> MnLtR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NH\Rb4cyPzl2MU[yOS=>
HEK293 cells M1Lwc2Z2dmO2aX;uJIF{e2G7 M{P6dWlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= MmHONVg{ODh3NkO=
HeLa cells MnPuSpVv[3Srb36gZZN{[Xl? M2TpcFAvOyEQvF2= MXWxOkBp MkT0TY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NF;OfJYyPzl3Nkm4PC=>
HCT116 cells NH3TVFdRem:uaX\ldoF1cW:wIHHzd4F6 NVe4WZhnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMEGzJO69VQ>? MnmyNlAzODV|OUS=
H1299 cells Ml7lVJJwdGmoZYLheIlwdiCjc4PhfS=> NYHNWZU6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5zNkGg{txO MXuyNFIxPTN7NB?=
H460 cells NUf4UXBbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoG2OFghcA>? M1iyV2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA4KM7:TR?= MnXjNlExPzNzNkC=
HCT116 cells NUWxbpRPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkKwOFghcA>? NEHmXVFIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> NFHiSVUzOTB5M{G2NC=>
CCRF-CEM cells MkT5VJJwdGmoZYLheIlwdiCjc4PhfS=> M1KzPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PSSk1ETU1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkWxJO69VQ>? NGPLPVkzOTZ{MUi4Ny=>
K562 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVUh|ryP MmHmNlE3OjF6OEO=
MOLT4 cells NGW0dGhRem:uaX\ldoF1cW:wIHHzd4F6 NWfLT2dpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MUiyNVYzOTh6Mx?=
SR cells M{fVZ3Bzd2yrZnXyZZRqd25iYYPzZZk> NUGxUpd[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTVkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk46QSEQvF2= M3XDfVIyPjJzOEiz
A549 cells NUfKNYtDWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkLvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA6KM7:TR?= NVfOZZRCOjF4MkG4PFM>
EKVX cells NE\WcHRRem:uaX\ldoF1cW:wIHHzd4F6 M{\D[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= NWXiSIk6OjF4MkG4PFM>
HOP62 cells NEjrdndRem:uaX\ldoF1cW:wIHHzd4F6 M1LzVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTB{IN88US=> MWqyNVYzOTh6Mx?=
HOP92 cells NYXYe2xpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmnORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN NIrYSZYzOTZ{MUi4Ny=>
NCI-H226 cells NXrEVYkxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> MVuyNVYzOTh6Mx?=
NCI-H23 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NUe3eWlwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO NEfrUWIzOTZ{MUi4Ny=>
NCI-H322M cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 NI\nUoNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzJ{TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj6yOkDPxE1? MViyNVYzOTh6Mx?=
NCI-H460 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 NW\MOphiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? MV6yNVYzOTh6Mx?=
COLO205 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MXGyNVYzOTh6Mx?=
HCT116 cells NXXwVHhpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN MkTBNlE3OjF6OEO=
HCT15 cells MnrmVJJwdGmoZYLheIlwdiCjc4PhfS=> MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= NV7EcVJZOjF4MkG4PFM>
HT-29 cells M4H1VHBzd2yrZnXyZZRqd25iYYPzZZk> Ml7lRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN MWmyNVYzOTh6Mx?=
KM12 cells NYS4SpR1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NX\pR4l5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> NFT4WFMzOTZ{MUi4Ny=>
SW620 cells NV63d24zWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH3k[XNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOlIxKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR5ODFOwG0> NFm0TGYzOTZ{MUi4Ny=>
SF268 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NEXwOoNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlY5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjV|IN88US=> Mn:xNlE3OjF6OEO=
SF295 cells NYfMZZYyWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4r5fmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yPVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzR|IN88US=> NWLjPVU4OjF4MkG4PFM>
SF539 cells NVPNTmZsWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1LIRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> NY[0fGI1OjF4MkG4PFM>
SNB19 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 NWHRfmVJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmIyQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> NF7UXJkzOTZ{MUi4Ny=>
SNB75 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 M2r1UmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> MYKyNVYzOTh6Mx?=
U251 cells NHX6c5NRem:uaX\ldoF1cW:wIHHzd4F6 NXvKPGpySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> NXryenZuOjF4MkG4PFM>
LOXIMVI cells MYfQdo9tcW[ncnH0bY9vKGG|c3H5 Mn7IRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOT2jJUXZKKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> NWPNTXBiOjF4MkG4PFM>
MALME-3M cells NUTtOHZYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVHzU29FSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNRWxOTS1|TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD60OlEh|ryP NIf0O4wzOTZ{MUi4Ny=>
M14 cells NHWzfJBRem:uaX\ldoF1cW:wIHHzd4F6 NX7xXVFbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNNVQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQDR7IN88US=> MYiyNVYzOTh6Mx?=
MDA-MB-435 cells NEPxWY1Rem:uaX\ldoF1cW:wIHHzd4F6 MoXrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? MViyNVYzOTh6Mx?=
SK-MEL-28 cells MoHyVJJwdGmoZYLheIlwdiCjc4PhfS=> NHXFNIpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD65PVMh|ryP MXyyNVYzOTh6Mx?=
SK-MEL-5 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NXTXUYQzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yO|Eh|ryP NUj5ZnR4OjF4MkG4PFM>
UACC257 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 NFTjUZVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NEfhWIgzOTZ{MUi4Ny=>
UACC62 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWDQ1O2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PzlizszN MmK4NlE3OjF6OEO=
IGROV1 cells MoPHVJJwdGmoZYLheIlwdiCjc4PhfS=> NV;m[4NSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? MnTzNlE3OjF6OEO=
OVCAR3 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 NX\rfo8ySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMUGg{txO M1XzbVIyPjJzOEiz
OVCAR4 cells M33yTHBzd2yrZnXyZZRqd25iYYPzZZk> M3TlfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjJzIN88US=> MX2yNVYzOTh6Mx?=
OVCAR5 cells M3LlcHBzd2yrZnXyZZRqd25iYYPzZZk> NHq2[mVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NjFOwG0> NX7G[|RwOjF4MkG4PFM>
OVCAR8 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 NFLOOGlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NTFOwG0> MY[yNVYzOTh6Mx?=
NCI/ADR-RES cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NXP5RVZTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= MXqyNVYzOTh6Mx?=
SKOV3 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 MnntRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN MVyyNVYzOTh6Mx?=
786-0 cells M2H5W3Bzd2yrZnXyZZRqd25iYYPzZZk> MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= MVuyNVYzOTh6Mx?=
A498 cells M{XyO3Bzd2yrZnXyZZRqd25iYYPzZZk> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNVEh|ryP MoDuNlE3OjF6OEO=
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MDA-MB-231 cells NFLDbIxRem:uaX\ldoF1cW:wIHHzd4F6 NF;IUlFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUOxMlch|ryP MV[yNVYzOTh6Mx?=
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T47D cells NXr5cW45WHKxbHnm[ZJifGmxbjDhd5NigQ>? NFnRUlVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI5NjhizszN NIrvOVczOTZ{MUi4Ny=>
MDA-MB-468 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 NV\zZWNxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= NIjBSpAzOTZ{MUi4Ny=>
NCI-H226 cells NXTjT2Z4S3m2b4TvfIlkcXS7IHHzd4F6 MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyxiTFO1NF0zOCEQvF2= Mn3PNlE3OjF6OEO=
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IGROV1 cells MU\DfZRwfG:6aXPpeJkh[XO|YYm= NVXSTXp2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO NVjRR5lXOjF4MkG4PFM>
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HCT116 cells NV;6OWdMWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{TEPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= M3jiRlIyPzR{NEm2
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HCT116 cells M{nWOHBzd2yrZnXyZZRqd25iYYPzZZk> M17nfWlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IFjDWFEyPiClZXzsd{Bxem:uaX\ldoF1cW:wLDDJR|UxRTBwMEGg{txO M1G0eFE1PjF|M{Gy
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CHO cells NUnPOo9OTnWwY4Tpc44h[XO|YYm= NEjuUJZKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IHH1eI9u[XSnZDDwZZRkcCClbHHtdEBmdGWldILvdIh6e2mxbH;nfUBie3OjeTygTWM2OD1zMj6yJO69VQ>? MV2yNFIxPTN7NB?=
HL-60(TB) cells NUfGfYs2WHKxbHnm[ZJifGmxbjDhd5NigQ>? M175TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFytOlApXEJrIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK0PUDPxE1? MoPzNlE3OjF6OEO=
RXF393 cells M4HSbnBzd2yrZnXyZZRqd25iYYPzZZk> M4i4T2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmjGN|k{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjBzIN88US=> MorhNlE3OjF6OEO=
RXF393 cells MYLDfZRwfG:6aXPpeJkh[XO|YYm= NH\udXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTYEZ|OUOgZ4VtdHNuIFzDOVA:OTVwMzFOwG0> NEjXSXYzOTZ{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.
  • 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

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