Dacinostat (LAQ824)

Catalog No.S1095 Synonyms: NVP-LAQ824

Dacinostat (LAQ824) Chemical Structure

Molecular Weight(MW): 379.459

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

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In DMSO USD 420 In stock
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Cited by 10 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 NH\JPZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkK4TY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN MWexOFUzOTR{Mh?=
HCT116 NFLE[YlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHzNcWRKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO NIT6XYYyPDV{MUSyNi=>
HCT116 NIHSRndEgXSxdH;4bYNqfHliYYPzZZk> NHjQU2ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP M17vOlE4QTRzNkK1
human mammary epithelial cells NFq0NZBEgXSxdH;4bYNqfHliYYPzZZk> MkXLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? MnPINVc6PDF4MkW=
HEK293 cells MY\GeY5kfGmxbjDhd5NigQ>? M1vuTWlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= NG\KT5IyQDNyOEW2Ny=>
HeLa cells M{G2NmZ2dmO2aX;uJIF{e2G7 NYL1WpJYOC5|IN88US=> MV2xOkBp MmjxTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= M1rzclE4QTV4OUi4
HCT116 cells NHnBdIhRem:uaX\ldoF1cW:wIHHzd4F6 MmTpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> MonrNlAzODV|OUS=
H1299 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 M{\1RWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> MkXBNlAzODV|OUS=
H460 cells NFrkUpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYO0PEBp MmSyS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP MmTRNlExPzNzNkC=
HCT116 cells NXHa[WlpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVjkNFdtPDhiaB?= NVPWVFVNT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO NIjmU2EzOTB5M{G2NC=>
CCRF-CEM cells MU\Qdo9tcW[ncnH0bY9vKGG|c3H5 NHPOPWRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? MXSyNVYzOTh6Mx?=
K562 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NUDX[mhxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> MnnrNlE3OjF6OEO=
MOLT4 cells M2XoNnBzd2yrZnXyZZRqd25iYYPzZZk> MnPERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN NFK5d4czOTZ{MUi4Ny=>
SR cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{Lkm5JO69VQ>? MlXmNlE3OjF6OEO=
A549 cells MlrYVJJwdGmoZYLheIlwdiCjc4PhfS=> MlvJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA6KM7:TR?= Mn7vNlE3OjF6OEO=
EKVX cells M2rG[nBzd2yrZnXyZZRqd25iYYPzZZk> MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP NVTpU5gxOjF4MkG4PFM>
HOP62 cells NVXQZZp4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHvQZ4FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjVyMjFOwG0> M1vsW|IyPjJzOEiz
HOP92 cells MnX0VJJwdGmoZYLheIlwdiCjc4PhfS=> NVziR2NvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A6OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5zOUmg{txO NFfXOnozOTZ{MUi4Ny=>
NCI-H226 cells NWPEVGI2WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3vzbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO NFLUdVIzOTZ{MUi4Ny=>
NCI-H23 cells NUHU[mdSWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPSEQvF2= MlvpNlE3OjF6OEO=
NCI-H322M cells M{X4OnBzd2yrZnXyZZRqd25iYYPzZZk> NWTnemZPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN{Ml2gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuNlYh|ryP MljxNlE3OjF6OEO=
NCI-H460 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 M2r3VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PjBiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNzFOwG0> MlPoNlE3OjF6OEO=
COLO205 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 M{HsbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> MmX4NlE3OjF6OEO=
HCT116 cells MnLXVJJwdGmoZYLheIlwdiCjc4PhfS=> Mo\4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzR5IN88US=> MYWyNVYzOTh6Mx?=
HCT15 cells NU\xXGpqWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUXreYNRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> NXHS[JprOjF4MkG4PFM>
HT-29 cells NWfaSo1[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NE\ZN|JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV4NjFOwG0> M3vNWlIyPjJzOEiz
KM12 cells NXfSU4VjWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1nYSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xPCEQvF2= MmXwNlE3OjF6OEO=
SW620 cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ4QCEQvF2= NWDBVIx6OjF4MkG4PFM>
SF268 cells M2XVXnBzd2yrZnXyZZRqd25iYYPzZZk> MnzGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK2PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= MWiyNVYzOTh6Mx?=
SF295 cells NGO2O4ZRem:uaX\ldoF1cW:wIHHzd4F6 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= NYLSSGsxOjF4MkG4PFM>
SF539 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 NF7pSmVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGOVM6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjl4NTFOwG0> MnPpNlE3OjF6OEO=
SNB19 cells MkT6VJJwdGmoZYLheIlwdiCjc4PhfS=> MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NE[5VXkzOTZ{MUi4Ny=>
SNB75 cells NH7DWGNRem:uaX\ldoF1cW:wIHHzd4F6 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= M3jOPVIyPjJzOEiz
U251 cells MmDLVJJwdGmoZYLheIlwdiCjc4PhfS=> NYTSbVA3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> NV76RYF4OjF4MkG4PFM>
LOXIMVI cells NIrGcmVRem:uaX\ldoF1cW:wIHHzd4F6 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN NEexepozOTZ{MUi4Ny=>
MALME-3M cells NVW5RYloWHKxbHnm[ZJifGmxbjDhd5NigQ>? M172TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? Mmr1NlE3OjF6OEO=
M14 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1zNDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD64OFkh|ryP MX:yNVYzOTh6Mx?=
MDA-MB-435 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 NHjOTZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVM4KM7:TR?= MXOyNVYzOTh6Mx?=
SK-MEL-28 cells NXLmXlVMWHKxbHnm[ZJifGmxbjDhd5NigQ>? MliwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? NV7wemJrOjF4MkG4PFM>
SK-MEL-5 cells NUCyZVFXWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWjDNXdySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yO|Eh|ryP MkPyNlE3OjF6OEO=
UACC257 cells NHPjbVJRem:uaX\ldoF1cW:wIHHzd4F6 NILQXmdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NGXMO2czOTZ{MUi4Ny=>
UACC62 cells NVLSO|c3WHKxbHnm[ZJifGmxbjDhd5NigQ>? M17hXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|YzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN5OTFOwG0> M4Pye|IyPjJzOEiz
IGROV1 cells NFPXRXhRem:uaX\ldoF1cW:wIHHzd4F6 MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN Ml;QNlE3OjF6OEO=
OVCAR3 cells NFfJWHRRem:uaX\ldoF1cW:wIHHzd4F6 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NHS0XoczOTZ{MUi4Ny=>
OVCAR4 cells M2TmcnBzd2yrZnXyZZRqd25iYYPzZZk> M{TKT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjJzIN88US=> NGn6eXczOTZ{MUi4Ny=>
OVCAR5 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 M13pOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> M1;nVVIyPjJzOEiz
OVCAR8 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 M1u0UWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> NV:3VlZvOjF4MkG4PFM>
NCI/ADR-RES cells M2TES3Bzd2yrZnXyZZRqd25iYYPzZZk> NYXT[ZYxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= M1nMRlIyPjJzOEiz
SKOV3 cells NFzaT5dRem:uaX\ldoF1cW:wIHHzd4F6 M4rqOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> M4D5N|IyPjJzOEiz
786-0 cells NH;hcI5Rem:uaX\ldoF1cW:wIHHzd4F6 MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= MkLNNlE3OjF6OEO=
A498 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NFHnU4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN NGnCPVczOTZ{MUi4Ny=>
ACHN cells MmTTVJJwdGmoZYLheIlwdiCjc4PhfS=> MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? NYDEPY1oOjF4MkG4PFM>
Caki1 cells M1HuNXBzd2yrZnXyZZRqd25iYYPzZZk> NH7qdJdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhb4kyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjZzOTFOwG0> MV[yNVYzOTh6Mx?=
SN12C cells MnHsVJJwdGmoZYLheIlwdiCjc4PhfS=> M4\ISWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU16xNmMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvQTJizszN NGfT[nkzOTZ{MUi4Ny=>
TK10 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= NIjMW3EzOTZ{MUi4Ny=>
UO31 cells MnPXVJJwdGmoZYLheIlwdiCjc4PhfS=> NEnafphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXPN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDV{IN88US=> Mn3wNlE3OjF6OEO=
PC3 cells Ml;mVJJwdGmoZYLheIlwdiCjc4PhfS=> MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MkCg{txO NHH4bXAzOTZ{MUi4Ny=>
DU145 cells NWDWN4Z[WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVfifHVqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> NHfHXHAzOTZ{MUi4Ny=>
MCF7 cells NGCwXWVRem:uaX\ldoF1cW:wIHHzd4F6 MlLaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlkyKM7:TR?= MYKyNVYzOTh6Mx?=
MDA-MB-231 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNzLkeg{txO NW\CNG9SOjF4MkG4PFM>
Hs 578T cells NImwTHpRem:uaX\ldoF1cW:wIHHzd4F6 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi|IEW3PHQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVUvQDJizszN NHize44zOTZ{MUi4Ny=>
BT549 cells MnPGVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn:zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= MVWyNVYzOTh6Mx?=
T47D cells MlHPVJJwdGmoZYLheIlwdiCjc4PhfS=> NWHmfodVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQC56IN88US=> NXztTXZiOjF4MkG4PFM>
MDA-MB-468 cells NFPhZ|FRem:uaX\ldoF1cW:wIHHzd4F6 NXXFbYdnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= Mn[zNlE3OjF6OEO=
NCI-H226 cells MVXDfZRwfG:6aXPpeJkh[XO|YYm= MnnrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNuIFzDOVA:OjBizszN NYn2fYdtOjF4MkG4PFM>
KM12 cells NGfKZnREgXSxdH;4bYNqfHliYYPzZZk> NXLZeYR[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU01zMjDj[YxteyxiTFO1NF0zQS57IN88US=> MofENlE3OjF6OEO=
SF295 cells NVHWNYNCS3m2b4TvfIlkcXS7IHHzd4F6 MkLQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= NUjEOJBzOjF4MkG4PFM>
SNB19 cells NVLZfWRsS3m2b4TvfIlkcXS7IHHzd4F6 MmDhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25DOTliY3XscJMtKEyFNUC9N|EvPyEQvF2= MnTqNlE3OjF6OEO=
U251 cells MkHaR5l1d3SxeHnjbZR6KGG|c3H5 Mnr1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWVI2OSClZXzsd{whVEN3ME21MlgzKM7:TR?= MWWyNVYzOTh6Mx?=
LOXIMVI cells MnGwR5l1d3SxeHnjbZR6KGG|c3H5 MY\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMU3hKVV[LIHPlcIx{NCCOQ{WwQVYvODRizszN MVmyNVYzOTh6Mx?=
MDA-MB-435 cells MlnER5l1d3SxeHnjbZR6KGG|c3H5 M1m2PWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? M4XU[VIyPjJzOEiz
SK-MEL-28 cells M1PI[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NUDndpZKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzMEBNSzVyPUOxMlkh|ryP NXzoRm1YOjF4MkG4PFM>
SK-MEL-5 cells NXfSb5pZS3m2b4TvfIlkcXS7IHHzd4F6 NWLlTGFGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVUh[2WubIOsJGxEPTB;ND6wNkDPxE1? NX;ZSVg2OjF4MkG4PFM>
UACC257 cells MVTDfZRwfG:6aXPpeJkh[XO|YYm= NX7YPWhCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? MWWyNVYzOTh6Mx?=
UACC62 cells MVvDfZRwfG:6aXPpeJkh[XO|YYm= NILDeHdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFNkKgZ4VtdHNuIFzDOVA:Pi5|OTFOwG0> M4PCPFIyPjJzOEiz
IGROV1 cells MlzsR5l1d3SxeHnjbZR6KGG|c3H5 M4nCTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGlIWk:YMTDj[YxteyxiTFO1NF01QC57IN88US=> Ml\0NlE3OjF6OEO=
OVCAR5 cells NHnuSIhEgXSxdH;4bYNqfHliYYPzZZk> MX7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMtKEyFNUC9N|gvQSEQvF2= NEnWRXczOTZ{MUi4Ny=>
SKOV3 cells MYDDfZRwfG:6aXPpeJkh[XO|YYm= MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= MXSyNVYzOTh6Mx?=
A498 cells M37xdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NGG1NllEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPDl6IHPlcIx{NCCOQ{WwQVUvQDhizszN NEfsd4UzOTZ{MUi4Ny=>
Caki1 cells Ml;MR5l1d3SxeHnjbZR6KGG|c3H5 NHqzXllEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBE[WurMTDj[YxteyxiTFO1NF02Njd7IN88US=> M3PpdFIyPjJzOEiz
HCT116 cells M{HUN3Bzd2yrZnXyZZRqd25iYYPzZZk> NWL1UGt{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEmFNUC9NE4xOTlizszN NITPWogzOTd2MkS5Oi=>
HCT116 cells M3Hj[HBzd2yrZnXyZZRqd25iYYPzZZk> MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= NWXtXJNTOjF4NUCyNlE>
H1299 cells M3;nT3Bzd2yrZnXyZZRqd25iYYPzZZk> M4f6dWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOsJGlEPTB;MD6xJO69VQ>? NVqySXh{OjF4NUCyNlE>
HCT116 cells M4XSRXBzd2yrZnXyZZRqd25iYYPzZZk> MYfJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKQ2SxNVYh[2WubIOgdJJwdGmoZYLheIlwdixiSVO1NF0xNjBzIN88US=> MmfQNVQ3OTN|MUK=
RPMI8226 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NISyVHNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLQUWk5OjJ4IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWyN{DPxE1? NHzicmozOTZ{MUi4Ny=>
CHO cells M3;sRWZ2dmO2aX;uJIF{e2G7 NUjreIRoUW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDheZRwdWG2ZXSgdIF1[2hiY3zhcZAh\WynY4Tyc5BpgXOrb3zv[5kh[XO|YYmsJGlEPTB;MUKuNkDPxE1? M4CzNlIxOjB3M{m0
HL-60(TB) cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 MlraRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTD22NEhVSiliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkS5JO69VQ>? NYPa[IgzOjF4MkG4PFM>
RXF393 cells NITmVHdRem:uaX\ldoF1cW:wIHHzd4F6 Mk\mRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN MXyyNVYzOTh6Mx?=
RXF393 cells M4[5[2N6fG:2b4jpZ4l1gSCjc4PhfS=> NV\QcHJpS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWliIM{mzJINmdGy|LDDMR|UxRTF3LkOg{txO NEfrdXEzOTZ{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]
+ 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]
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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]
+ 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):
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

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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