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 M4TrR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVmyR2hSUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEhzMkm5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMUWg{txO NX;WbXVvOTR3MkG0NlI>
HCT116 NV\qXmNqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3jGNGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> NUnYbFlpOTR3MkG0NlI>
HCT116 MVvDfZRwfG:6aXPpeJkh[XO|YYm= MnKyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC1JO69VQ>? MmPCNVc6PDF4MkW=
human mammary epithelial cells M4jwOGN6fG:2b4jpZ4l1gSCjc4PhfS=> M4i1cmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? MkLKNVc6PDF4MkW=
HEK293 cells NF2yeVVHfW6ldHnvckBie3OjeR?= NUW0eI5{UW6qaXLpeIlwdiCxZjDISGFEOSCrbjDISWszQTNiY3XscJMtKEmFNUC9NE4xODJ4IN88US=> MYSxPFMxQDV4Mx?=
HeLa cells MV\GeY5kfGmxbjDhd5NigQ>? MYewMlMh|ryP NGLlPJMyPiCq M1u3U2lvcGmkaYTpc44hd2ZiSFTBR|QudWWmaXH0[YQhemWycnXzd4lwdiCxZjDNSWYzNWSncHXu[IVvfCC2cnHud4NzcXC2aX;uJIlvKEinTHGgZ4VtdHNiYYSgNE4{KHWPIHHmeIVzKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= NInYWm8yPzl3Nkm4PC=>
HCT116 cells NIXydJBRem:uaX\ldoF1cW:wIHHzd4F6 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4xOTNizszN Mkj5NlAzODV|OUS=
H1299 cells MknMVJJwdGmoZYLheIlwdiCjc4PhfS=> M4O1emFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> M2PHOFIxOjB3M{m0
H460 cells M1H6eGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M13FUlQ5KGh? M4jZVWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA4KM7:TR?= M3fEd|IyODd|MU[w
HCT116 cells NEXZTXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXu0PEBp NVnEeYduT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO NWDvNGI3OjFyN{OxOlA>
CCRF-CEM cells NH7QSoJRem:uaX\ldoF1cW:wIHHzd4F6 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> M3v4V|IyPjJzOEiz
K562 cells M3jud3Bzd2yrZnXyZZRqd25iYYPzZZk> MlL4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU2KM7:TR?= MWiyNVYzOTh6Mx?=
MOLT4 cells NVHwd41OWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkTsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN NUXWbFZnOjF4MkG4PFM>
SR cells NXPxWlNPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFjwWoNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= Mn\ONlE3OjF6OEO=
A549 cells NYPD[IFJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF\nS3NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NWj2Z5NsOjF4MkG4PFM>
EKVX cells NVPvcoRWWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP NWGz[3p[OjF4MkG4PFM>
HOP62 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 NHn2b5ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjVyMjFOwG0> NFzJTpYzOTZ{MUi4Ny=>
HOP92 cells M13sU3Bzd2yrZnXyZZRqd25iYYPzZZk> Mo\wRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN MYmyNVYzOTh6Mx?=
NCI-H226 cells MoK4VJJwdGmoZYLheIlwdiCjc4PhfS=> MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> NIH4cogzOTZ{MUi4Ny=>
NCI-H23 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 NUK5c|dPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO M1LSR|IyPjJzOEiz
NCI-H322M cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NGPWdWtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzJ{TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj6yOkDPxE1? M3\ZZ|IyPjJzOEiz
NCI-H460 cells M{S4OXBzd2yrZnXyZZRqd25iYYPzZZk> Mn\aRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> M{XyNVIyPjJzOEiz
COLO205 cells MkXFVJJwdGmoZYLheIlwdiCjc4PhfS=> NETJV|FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO NVLiVFhmOjF4MkG4PFM>
HCT116 cells M{joe3Bzd2yrZnXyZZRqd25iYYPzZZk> MkjuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzR5IN88US=> NYXBXI5HOjF4MkG4PFM>
HCT15 cells MmO1VJJwdGmoZYLheIlwdiCjc4PhfS=> NGXUVpBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> MlLmNlE3OjF6OEO=
HT-29 cells NHT6OIdRem:uaX\ldoF1cW:wIHHzd4F6 MmPvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN M3jh[|IyPjJzOEiz
KM12 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPMUKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNFQh|ryP MX6yNVYzOTh6Mx?=
SW620 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 NV;ZR21zSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO NUXJUpBuOjF4MkG4PFM>
SF268 cells NFHwc3BRem:uaX\ldoF1cW:wIHHzd4F6 MlXGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK2PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= NXHyXo9IOjF4MkG4PFM>
SF295 cells M3\ZZ3Bzd2yrZnXyZZRqd25iYYPzZZk> MmnqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK5OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE44PDNizszN MWiyNVYzOTh6Mx?=
SF539 cells M1y5TXBzd2yrZnXyZZRqd25iYYPzZZk> MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOINUO5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk3PSEQvF2= MorJNlE3OjF6OEO=
SNB19 cells NXvtbYxzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXLmb|VbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmIyQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> MkXWNlE3OjF6OEO=
SNB75 cells NITBS4lRem:uaX\ldoF1cW:wIHHzd4F6 M2j4VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> M1zDO|IyPjJzOEiz
U251 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 NHXZPVRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> MkjNNlE3OjF6OEO=
LOXIMVI cells NVLkb45ZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHrw[VZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO MknVNlE3OjF6OEO=
MALME-3M cells MmTMVJJwdGmoZYLheIlwdiCjc4PhfS=> M3G5[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? Ml7yNlE3OjF6OEO=
M14 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1zNDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD64OFkh|ryP M2q3bFIyPjJzOEiz
MDA-MB-435 cells M4nGWHBzd2yrZnXyZZRqd25iYYPzZZk> MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01OzViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUO3JO69VQ>? NVLE[I1{OjF4MkG4PFM>
SK-MEL-28 cells NIq5bXNRem:uaX\ldoF1cW:wIHHzd4F6 Ml31RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? MlnDNlE3OjF6OEO=
SK-MEL-5 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 MoKyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{N{Gg{txO MXiyNVYzOTh6Mx?=
UACC257 cells Mo\lVJJwdGmoZYLheIlwdiCjc4PhfS=> M2jRXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO M{Tj[FIyPjJzOEiz
UACC62 cells NF7KUm5Rem:uaX\ldoF1cW:wIHHzd4F6 NIDWdVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2M3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|N{mg{txO NWize5N1OjF4MkG4PFM>
IGROV1 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN MmLnNlE3OjF6OEO=
OVCAR3 cells NUDWeXhpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NX;WNopKOjF4MkG4PFM>
OVCAR4 cells NX3Zd4FrWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{4zOSEQvF2= Ml25NlE3OjF6OEO=
OVCAR5 cells NFX4WpJRem:uaX\ldoF1cW:wIHHzd4F6 MmHvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOjZizszN M2XZXVIyPjJzOEiz
OVCAR8 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 M{e1e2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> Ml;RNlE3OjF6OEO=
NCI/ADR-RES cells M{LJZXBzd2yrZnXyZZRqd25iYYPzZZk> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? NX7sfI9wOjF4MkG4PFM>
SKOV3 cells MnzWVJJwdGmoZYLheIlwdiCjc4PhfS=> NIDVSYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{NDFOwG0> MXWyNVYzOTh6Mx?=
786-0 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MlTVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiB5OE[tNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4{QCEQvF2= MmS5NlE3OjF6OEO=
A498 cells NXLoRZJ6WHKxbHnm[ZJifGmxbjDhd5NigQ>? NX3sT|J7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> MkXtNlE3OjF6OEO=
ACHN cells M1HPN3Bzd2yrZnXyZZRqd25iYYPzZZk> NX:2ZY1iSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFizszN NVi5b5NPOjF4MkG4PFM>
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TK10 cells NEDGZm5Rem:uaX\ldoF1cW:wIHHzd4F6 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= MWKyNVYzOTh6Mx?=
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MDA-MB-468 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEig{txO MYKyNVYzOTh6Mx?=
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H1299 cells M4TUe3Bzd2yrZnXyZZRqd25iYYPzZZk> M3zQTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOsJGlEPTB;MD6xJO69VQ>? Mm\nNlE3PTB{MkG=
HCT116 cells M3\JcHBzd2yrZnXyZZRqd25iYYPzZZk> MYTJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKQ2SxNVYh[2WubIOgdJJwdGmoZYLheIlwdixiSVO1NF0xNjBzIN88US=> MUixOFYyOzNzMh?=
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HL-60(TB) cells NFTSUGdRem:uaX\ldoF1cW:wIHHzd4F6 MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiOLU[wLHRDMSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NEmg{txO M4nOcFIyPjJzOEiz
RXF393 cells MnHhVJJwdGmoZYLheIlwdiCjc4PhfS=> NVHaUGpvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMEGg{txO MXWyNVYzOTh6Mx?=
RXF393 cells NG\SWIREgXSxdH;4bYNqfHliYYPzZZk> MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMtKEyFNUC9NVUvOyEQvF2= NHzSUZQzOTZ{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]
+ 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:
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
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