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 MmPrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnnHTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN M2LZSFE1PTJzNEKy
HCT116 NVTGbnlZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4PINmlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> M1X6UlE1PTJzNEKy
HCT116 MVTDfZRwfG:6aXPpeJkh[XO|YYm= MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEWg{txO NV3rfmM6OTd7NEG2NlU>
human mammary epithelial cells MoHTR5l1d3SxeHnjbZR6KGG|c3H5 MmTrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NHH2RWYyPzl2MU[yOS=>
HEK293 cells M1TjcWZ2dmO2aX;uJIF{e2G7 NFTaPIpKdmirYnn0bY9vKG:oIFjERWMyKGmwIFjFT|I6OyClZXzsd{whUUN3ME2wMlAxOjZizszN M{Xm[FE5OzB6NU[z
HeLa cells NGXveplHfW6ldHnvckBie3OjeR?= NGXwRYQxNjNizszN M{fXe|E3KGh? NXHSUYRkUW6qaXLpeIlwdiCxZjDISGFEPC2vZXTpZZRm\CC{ZYDy[ZN{cW:wIH;mJG1GTjJvZHXw[Y5l\W62IITyZY5{[3KrcITpc44hcW5iSHXMZUBk\WyuczDheEAxNjNidV2gZYZ1\XJiMU[gbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NGj2SJkyPzl3Nkm4PC=>
HCT116 cells NFLB[XJRem:uaX\ldoF1cW:wIHHzd4F6 NHLxb3dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO M2X5SFIxOjB3M{m0
H1299 cells M1jFWHBzd2yrZnXyZZRqd25iYYPzZZk> Moq2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN MWKyNFIxPTN7NB?=
H460 cells MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVfGSJZwPDhiaB?= MVLHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wO{DPxE1? NFPTUHIzOTB5M{G2NC=>
HCT116 cells NFztc|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4G4WVQ5KGh? NHiyeJlIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> M4nwN|IyODd|MU[w
CCRF-CEM cells M3r4[XBzd2yrZnXyZZRqd25iYYPzZZk> M{TPZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PSSk1ETU1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkWxJO69VQ>? NV\XT21NOjF4MkG4PFM>
K562 cells NIDWSG9Rem:uaX\ldoF1cW:wIHHzd4F6 NXnH[lJuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> NVXWZZg5OjF4MkG4PFM>
MOLT4 cells NWXSWo5tWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXXLZm15SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MlfQNlE3OjF6OEO=
SR cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 NHvtd|NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= NH3COlAzOTZ{MUi4Ny=>
A549 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 NUjiUGI1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB7IN88US=> NXqxfJY{OjF4MkG4PFM>
EKVX cells NV:xW2M3WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mm\0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHS2\YJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlc2KM7:TR?= NFq3UIQzOTZ{MUi4Ny=>
HOP62 cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 MlfFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN NFfUOHMzOTZ{MUi4Ny=>
HOP92 cells NUO2OXhOWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlnqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN M4nkd|IyPjJzOEiz
NCI-H226 cells NYXIdYdWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3TxTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO NVj0OWJqOjF4MkG4PFM>
NCI-H23 cells M1f6c3Bzd2yrZnXyZZRqd25iYYPzZZk> MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPSEQvF2= NWG0ToRROjF4MkG4PFM>
NCI-H322M cells Mme5VJJwdGmoZYLheIlwdiCjc4PhfS=> MnrMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO MkDCNlE3OjF6OEO=
NCI-H460 cells NGSwN|RRem:uaX\ldoF1cW:wIHHzd4F6 NWOwZoZSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? M37ST|IyPjJzOEiz
COLO205 cells NULPfGJrWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoDlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> MWmyNVYzOTh6Mx?=
HCT116 cells NUPP[GVnWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN NFLZOogzOTZ{MUi4Ny=>
HCT15 cells MoX0VJJwdGmoZYLheIlwdiCjc4PhfS=> M3jzfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvODdizszN NFjSZlczOTZ{MUi4Ny=>
HT-29 cells NWLHWWZ4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlfNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN NI[5d5AzOTZ{MUi4Ny=>
KM12 cells NXnPOYxIWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mo\LRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= NGPQRW8zOTZ{MUi4Ny=>
SW620 cells NXLyWVRGWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUDsT|Q3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO NUTZemFTOjF4MkG4PFM>
SF268 cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 NVPiW2NwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> MkLtNlE3OjF6OEO=
SF295 cells NGPiZolRem:uaX\ldoF1cW:wIHHzd4F6 M2XNXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yPVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzR|IN88US=> MnPkNlE3OjF6OEO=
SF539 cells M3rNc3Bzd2yrZnXyZZRqd25iYYPzZZk> M17BRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> NWruW5BFOjF4MkG4PFM>
SNB19 cells M{fLRXBzd2yrZnXyZZRqd25iYYPzZZk> M4rj[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CNVkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN NULhZmdxOjF4MkG4PFM>
SNB75 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= MWGyNVYzOTh6Mx?=
U251 cells M1XXVXBzd2yrZnXyZZRqd25iYYPzZZk> NHGzUXBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> M{TNbVIyPjJzOEiz
LOXIMVI cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 M2TE[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF;YTW1XUSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> NFPsWIYzOTZ{MUi4Ny=>
MALME-3M cells NVXV[Wp6WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3;WSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? M3rIWVIyPjJzOEiz
M14 cells M1nrO3Bzd2yrZnXyZZRqd25iYYPzZZk> NGH6SnFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2xOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE45PDlizszN NUf1[Zh[OjF4MkG4PFM>
MDA-MB-435 cells NXvrdGRxWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mo\ZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? NXO2dGIxOjF4MkG4PFM>
SK-MEL-28 cells NHXjNWxRem:uaX\ldoF1cW:wIHHzd4F6 M1Hub2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkm5N{DPxE1? M3O3bFIyPjJzOEiz
SK-MEL-5 cells NYTkNXQ2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIDHV2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? M3\vTVIyPjJzOEiz
UACC257 cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 NE\mc2pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NHTLcm4zOTZ{MUi4Ny=>
UACC62 cells M4DEW3Bzd2yrZnXyZZRqd25iYYPzZZk> NXTUfYtmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{e5JO69VQ>? M2niR|IyPjJzOEiz
IGROV1 cells M{ntdXBzd2yrZnXyZZRqd25iYYPzZZk> NWntO3hVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? NVXaPGRLOjF4MkG4PFM>
OVCAR3 cells MoHJVJJwdGmoZYLheIlwdiCjc4PhfS=> M{fWPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> NVeyVlMxOjF4MkG4PFM>
OVCAR4 cells NH3QNG9Rem:uaX\ldoF1cW:wIHHzd4F6 NHrEenpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> M2jESVIyPjJzOEiz
OVCAR5 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 NGfjd2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NjFOwG0> NIDlN|IzOTZ{MUi4Ny=>
OVCAR8 cells NWjudVFWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1vWdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> MnfFNlE3OjF6OEO=
NCI/ADR-RES cells M{H3eXBzd2yrZnXyZZRqd25iYYPzZZk> M2K3W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJM2FFWi2URWOgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNVgh|ryP M2i0N|IyPjJzOEiz
SKOV3 cells NGjLZZJRem:uaX\ldoF1cW:wIHHzd4F6 NX\FTXZ4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkSg{txO MUiyNVYzOTh6Mx?=
786-0 cells NILSXlhRem:uaX\ldoF1cW:wIHHzd4F6 Mnz6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiB5OE[tNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4{QCEQvF2= MVyyNVYzOTh6Mx?=
A498 cells NF7BPZVRem:uaX\ldoF1cW:wIHHzd4F6 MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNVEh|ryP MXuyNVYzOTh6Mx?=
ACHN cells NXnqPXBoWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? MofaNlE3OjF6OEO=
Caki1 cells NWK4SZRjWHKxbHnm[ZJifGmxbjDhd5NigQ>? M36xSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> NHSwbVQzOTZ{MUi4Ny=>
SN12C cells MkD5VJJwdGmoZYLheIlwdiCjc4PhfS=> NUnocHF5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUlEzSyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy57MjFOwG0> NILDXZEzOTZ{MUi4Ny=>
TK10 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 M1nGR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFuxNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PDRizszN MorINlE3OjF6OEO=
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PC3 cells M2e5WXBzd2yrZnXyZZRqd25iYYPzZZk> MmLaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKwJO69VQ>? MknyNlE3OjF6OEO=
DU145 cells MmnCVJJwdGmoZYLheIlwdiCjc4PhfS=> MoDURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlkvQSEQvF2= M2jD[lIyPjJzOEiz
MCF7 cells NGrGS2pRem:uaX\ldoF1cW:wIHHzd4F6 NXzzOWs2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjlzIN88US=> MnXWNlE3OjF6OEO=
MDA-MB-231 cells Mmm2VJJwdGmoZYLheIlwdiCjc4PhfS=> NWLQeWpWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zNU44KM7:TR?= NX33UphOOjF4MkG4PFM>
Hs 578T cells NICzOpdRem:uaX\ldoF1cW:wIHHzd4F6 MljDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKczC1O|hVKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF02Njh{IN88US=> NHvo[ZIzOTZ{MUi4Ny=>
BT549 cells NXnuXXp1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkDXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= NUnJeVhOOjF4MkG4PFM>
T47D cells NVvxW3ZpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUK4Mlgh|ryP MlTlNlE3OjF6OEO=
MDA-MB-468 cells M1fmenBzd2yrZnXyZZRqd25iYYPzZZk> NIjIV5BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12NkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUWuPFgh|ryP NITGOHMzOTZ{MUi4Ny=>
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KM12 cells MkDVR5l1d3SxeHnjbZR6KGG|c3H5 NVvr[Y5lS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU01zMjDj[YxteyxiTFO1NF0zQS57IN88US=> MY[yNVYzOTh6Mx?=
SF295 cells Mmq0R5l1d3SxeHnjbZR6KGG|c3H5 M3u0b2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjl3IHPlcIx{NCCOQ{WwQVYvQTFizszN Mn\4NlE3OjF6OEO=
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U251 cells M1zQeWN6fG:2b4jpZ4l1gSCjc4PhfS=> M4TZU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHUzPTFiY3XscJMtKEyFNUC9OU45OiEQvF2= MVSyNVYzOTh6Mx?=
LOXIMVI cells NVXTNm9DS3m2b4TvfIlkcXS7IHHzd4F6 MnnMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG9ZUU2YSTDj[YxteyxiTFO1NF03NjB2IN88US=> MVGyNVYzOTh6Mx?=
MDA-MB-435 cells MljOR5l1d3SxeHnjbZR6KGG|c3H5 MkXGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygUGM2OD1{OD64JO69VQ>? NIX3SZQzOTZ{MUi4Ny=>
SK-MEL-28 cells NVixOHM{S3m2b4TvfIlkcXS7IHHzd4F6 MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNuIFzDOVA:OzFwOTFOwG0> NX3Jd4w1OjF4MkG4PFM>
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UACC257 cells NVq3bXRXS3m2b4TvfIlkcXS7IHHzd4F6 MVfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{NCCOQ{WwQVQ1NjhizszN NV;4[XZROjF4MkG4PFM>
UACC62 cells MVrDfZRwfG:6aXPpeJkh[XO|YYm= M2LxeGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> NXu2PGxoOjF4MkG4PFM>
IGROV1 cells MmPvR5l1d3SxeHnjbZR6KGG|c3H5 MWHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= MlfUNlE3OjF6OEO=
OVCAR5 cells NGHXN4REgXSxdH;4bYNqfHliYYPzZZk> NYS3UWZjS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO NWLLcI82OjF4MkG4PFM>
SKOV3 cells M4jETGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= NISwR5EzOTZ{MUi4Ny=>
A498 cells MVXDfZRwfG:6aXPpeJkh[XO|YYm= MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzMEBNSzVyPUWuPFgh|ryP M2nuT|IyPjJzOEiz
Caki1 cells M1TIWWN6fG:2b4jpZ4l1gSCjc4PhfS=> NXzFc5VJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> NG\PTJAzOTZ{MUi4Ny=>
HCT116 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 NH:2Z5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{whUUN3ME2wMlAyQSEQvF2= NESyRWczOTd2MkS5Oi=>
HCT116 cells M3rSdXBzd2yrZnXyZZRqd25iYYPzZZk> NFy1VVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NF0xNjBzOTFOwG0> MlPRNlE3PTB{MkG=
H1299 cells MWTQdo9tcW[ncnH0bY9vKGG|c3H5 NUG4WWFMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{whUUN3ME2wMlEh|ryP NILCWI0zOTZ3MEKyNS=>
HCT116 cells NUnrdnBDWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml7sTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> MVGxOFYyOzNzMh?=
RPMI8226 cells M{jjOHBzd2yrZnXyZZRqd25iYYPzZZk> MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{MzFOwG0> M3[2V|IyPjJzOEiz
CHO cells MXnGeY5kfGmxbjDhd5NigQ>? NWe3W4JIUW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDheZRwdWG2ZXSgdIF1[2hiY3zhcZAh\WynY4Tyc5BpgXOrb3zv[5kh[XO|YYmsJGlEPTB;MUKuNkDPxE1? M4nndlIxOjB3M{m0
HL-60(TB) cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 NEHOdXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMMVYxMFSEKTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOFkh|ryP NFK3WHgzOTZ{MUi4Ny=>
RXF393 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 MmPsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN NULUZWpJOjF4MkG4PFM>
RXF393 cells NGD5fopEgXSxdH;4bYNqfHliYYPzZZk> MoCxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN MnLxNlE3OjF6OEO=

... 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

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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