Dacinostat (LAQ824)

For research use only.

Catalog No.S1095 Synonyms: NVP-LAQ824

18 publications

Dacinostat (LAQ824) Chemical Structure

CAS No. 404951-53-7

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

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10mM (1mL in DMSO) EUR 412 In stock
EUR 314 In stock
EUR 953 In stock
EUR 1955 In stock
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Selleck's Dacinostat (LAQ824) has been cited by 18 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.

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Choose Selective HDAC Inhibitors

Biological Activity

Description Dacinostat (LAQ824, NVP-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 MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NG\zVphKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> M1TKN|E1PTJzNEKy
HCT116 MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2rVPWlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> M2Dxc|E1PTJzNEKy
HCT116 M1WzdmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEWg{txO Mon2NVc6PDF4MkW=
human mammary epithelial cells NEXYVXVEgXSxdH;4bYNqfHliYYPzZZk> MoLKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NUjEcXZGOTd7NEG2NlU>
HEK293 cells NGnXbnRHfW6ldHnvckBie3OjeR?= NFXmU2lKdmirYnn0bY9vKG:oIFjERWMyKGmwIFjFT|I6OyClZXzsd{whUUN3ME2wMlAxOjZizszN NIHyOXoyQDNyOEW2Ny=>
HeLa cells MWfGeY5kfGmxbjDhd5NigQ>? NUnYb3RUOC5|IN88US=> MXSxOkBp MUHJcohq[mm2aX;uJI9nKEiGQVO0MY1m\GmjdHXkJJJmeHKnc4Ppc44hd2ZiTVXGNk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbjDpckBJ\UyjIHPlcIx{KGG2IECuN{B2VSCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 MkjoNVc6PTZ7OEi=
HCT116 cells NH3WfmVRem:uaX\ldoF1cW:wIHHzd4F6 NG\3SINCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO MVWyNFIxPTN7NB?=
H1299 cells MmrYVJJwdGmoZYLheIlwdiCjc4PhfS=> MnTsRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN NV7ZfJRbOjB{MEWzPVQ>
H460 cells MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1;6clQ5KGh? M1:xR2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA4KM7:TR?= NEjFdYszOTB5M{G2NC=>
HCT116 cells NUjZempjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXi0PEBp Mn7mS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN NHfleo8zOTB5M{G2NC=>
CCRF-CEM cells M1[4V3Bzd2yrZnXyZZRqd25iYYPzZZk> NVvTbpI3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOVEh|ryP MoLDNlE3OjF6OEO=
K562 cells M4PjdXBzd2yrZnXyZZRqd25iYYPzZZk> NWLkRmx[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> NWH2SYszOjF4MkG4PFM>
MOLT4 cells M{DlTHBzd2yrZnXyZZRqd25iYYPzZZk> NXfDXWRZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MUSyNVYzOTh6Mx?=
SR cells MmjTVJJwdGmoZYLheIlwdiCjc4PhfS=> M3WzdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2KgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuPVkh|ryP NXTkbXJXOjF4MkG4PFM>
A549 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NHz3cYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NYj3SXFjOjF4MkG4PFM>
EKVX cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP MUeyNVYzOTh6Mx?=
HOP62 cells MkHOVJJwdGmoZYLheIlwdiCjc4PhfS=> MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUE[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUxOiEQvF2= NF:3VIQzOTZ{MUi4Ny=>
HOP92 cells MkPJVJJwdGmoZYLheIlwdiCjc4PhfS=> NXr6bpFuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A6OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5zOUmg{txO MojpNlE3OjF6OEO=
NCI-H226 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> NUSwe|B5OjF4MkG4PFM>
NCI-H23 cells NXrhXoRUWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn7tRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN NV:1NIV{OjF4MkG4PFM>
NCI-H322M cells Ml;uVJJwdGmoZYLheIlwdiCjc4PhfS=> NWfjTI9xSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN{Ml2gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuNlYh|ryP NX2zVXZ7OjF4MkG4PFM>
NCI-H460 cells NHi0eJdRem:uaX\ldoF1cW:wIHHzd4F6 NHjZXXRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkeg{txO MojVNlE3OjF6OEO=
COLO205 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NF;6SldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO NVfTS4FnOjF4MkG4PFM>
HCT116 cells MoK3VJJwdGmoZYLheIlwdiCjc4PhfS=> MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN MU[yNVYzOTh6Mx?=
HCT15 cells NILCeHBRem:uaX\ldoF1cW:wIHHzd4F6 NWrh[pMySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> MWSyNVYzOTh6Mx?=
HT-29 cells NXzRe5RCWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUPmRVZVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO M1vV[lIyPjJzOEiz
KM12 cells NIXy[lZRem:uaX\ldoF1cW:wIHHzd4F6 NF20UnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODRizszN M{HOOFIyPjJzOEiz
SW620 cells NEPKTVBRem:uaX\ldoF1cW:wIHHzd4F6 MlXFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN MmnYNlE3OjF6OEO=
SF268 cells NYDjSopwWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4L5dGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN MWWyNVYzOTh6Mx?=
SF295 cells Mor6VJJwdGmoZYLheIlwdiCjc4PhfS=> NWS4WGEySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO M1LpTlIyPjJzOEiz
SF539 cells MmTIVJJwdGmoZYLheIlwdiCjc4PhfS=> M1PoO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> MWSyNVYzOTh6Mx?=
SNB19 cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NWj4XFN5OjF4MkG4PFM>
SNB75 cells NWnZc|JTWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4nXb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> NX7re2o5OjF4MkG4PFM>
U251 cells M2\PUHBzd2yrZnXyZZRqd25iYYPzZZk> MmSyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= MXKyNVYzOTh6Mx?=
LOXIMVI cells M3e5cXBzd2yrZnXyZZRqd25iYYPzZZk> MnfIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOT2jJUXZKKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> MWmyNVYzOTh6Mx?=
MALME-3M cells NVvqfnhKWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> M2izfVIyPjJzOEiz
M14 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 M{XnfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTUG0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlg1QSEQvF2= M2jyTVIyPjJzOEiz
MDA-MB-435 cells M1OwUnBzd2yrZnXyZZRqd25iYYPzZZk> NFLCdZhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVM4KM7:TR?= MYiyNVYzOTh6Mx?=
SK-MEL-28 cells M2izTHBzd2yrZnXyZZRqd25iYYPzZZk> NXjmTnExSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= MY[yNVYzOTh6Mx?=
SK-MEL-5 cells M1\VbHBzd2yrZnXyZZRqd25iYYPzZZk> NH;LTotCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? MoCwNlE3OjF6OEO=
UACC257 cells MoPUVJJwdGmoZYLheIlwdiCjc4PhfS=> NVPp[G1iSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkO5N{DPxE1? NX3iPIxMOjF4MkG4PFM>
UACC62 cells MnzHVJJwdGmoZYLheIlwdiCjc4PhfS=> NFjIfW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2M3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|N{mg{txO NW[1S2o2OjF4MkG4PFM>
IGROV1 cells MlfDVJJwdGmoZYLheIlwdiCjc4PhfS=> MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN M371UFIyPjJzOEiz
OVCAR3 cells NULuV3FjWHKxbHnm[ZJifGmxbjDhd5NigQ>? NILpR4NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> NYjsUG5pOjF4MkG4PFM>
OVCAR4 cells NWDCW4hDWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1n5dmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjJzIN88US=> MWKyNVYzOTh6Mx?=
OVCAR5 cells NI[ycm1Rem:uaX\ldoF1cW:wIHHzd4F6 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4zPiEQvF2= Moj0NlE3OjF6OEO=
OVCAR8 cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 M4DTOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> MUGyNVYzOTh6Mx?=
NCI/ADR-RES cells NV\XV4F3WHKxbHnm[ZJifGmxbjDhd5NigQ>? Mlr0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mvRWRTNVKHUzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6xPEDPxE1? M4nGWVIyPjJzOEiz
SKOV3 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 NEDwWG9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{NDFOwG0> MV:yNVYzOTh6Mx?=
786-0 cells M4L2U3Bzd2yrZnXyZZRqd25iYYPzZZk> NUe1VW5TSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjC3PFYuOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5|ODFOwG0> M{Pme|IyPjJzOEiz
A498 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 M2DYVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= M2XDZVIyPjJzOEiz
ACHN cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 MmOzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDQ1jOJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEh|ryP M2fhOFIyPjJzOEiz
Caki1 cells NETKbnNRem:uaX\ldoF1cW:wIHHzd4F6 MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOja3mxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlYyQSEQvF2= NFraUWszOTZ{MUi4Ny=>
SN12C cells Mn3EVJJwdGmoZYLheIlwdiCjc4PhfS=> MmH4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTkGyR{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{46OiEQvF2= MnzLNlE3OjF6OEO=
TK10 cells NFSyd|dRem:uaX\ldoF1cW:wIHHzd4F6 MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= MnTyNlE3OjF6OEO=
UO31 cells NH;TRppRem:uaX\ldoF1cW:wIHHzd4F6 NXjEeoNFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> NYfWfmJ2OjF4MkG4PFM>
PC3 cells NGLLRW5Rem:uaX\ldoF1cW:wIHHzd4F6 M{P1RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yNEDPxE1? M1TYU|IyPjJzOEiz
DU145 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 NWXTVYprSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> NUTkNJp[OjF4MkG4PFM>
MCF7 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MkLuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlkyKM7:TR?= NXHBW25TOjF4MkG4PFM>
MDA-MB-231 cells M4XBVnBzd2yrZnXyZZRqd25iYYPzZZk> NYjUUpNxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zNU44KM7:TR?= MlXSNlE3OjF6OEO=
Hs 578T cells Mor0VJJwdGmoZYLheIlwdiCjc4PhfS=> NInQS3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjzJFU4QFRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEKg{txO NW\E[3pnOjF4MkG4PFM>
BT549 cells M4PLXHBzd2yrZnXyZZRqd25iYYPzZZk> Ml7zRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= NWrYO4Z2OjF4MkG4PFM>
T47D cells NVvNNGVjWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF;PVXdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI5NjhizszN NXHPO4FUOjF4MkG4PFM>
MDA-MB-468 cells M1LiVHBzd2yrZnXyZZRqd25iYYPzZZk> NWj2cmF4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= MkDrNlE3OjF6OEO=
NCI-H226 cells M3vBO2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnrER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNuIFzDOVA:OjBizszN MonENlE3OjF6OEO=
KM12 cells NFP1[YpEgXSxdH;4bYNqfHliYYPzZZk> Mn\QR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT20yOiClZXzsd{whVEN3ME2yPU46KM7:TR?= NVnvcWUyOjF4MkG4PFM>
SF295 cells M3S0[GN6fG:2b4jpZ4l1gSCjc4PhfS=> NIX3S5hEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUTjJ7NTDj[YxteyxiTFO1NF03NjlzIN88US=> MWKyNVYzOTh6Mx?=
SNB19 cells M{HMTGN6fG:2b4jpZ4l1gSCjc4PhfS=> MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUmIyQSClZXzsd{whVEN3ME2zNU44KM7:TR?= NX\y[G5QOjF4MkG4PFM>
U251 cells MX3DfZRwfG:6aXPpeJkh[XO|YYm= MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzMEBNSzVyPUWuPFIh|ryP NEnoeIYzOTZ{MUi4Ny=>
LOXIMVI cells NYjrOW0yS3m2b4TvfIlkcXS7IHHzd4F6 MmqzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG9ZUU2YSTDj[YxteyxiTFO1NF03NjB2IN88US=> MVWyNVYzOTh6Mx?=
MDA-MB-435 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MmPHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUSzOUBk\WyuczygUGM2OD1{OD64JO69VQ>? Moe3NlE3OjF6OEO=
SK-MEL-28 cells NE\TNWZEgXSxdH;4bYNqfHliYYPzZZk> M4f1b2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD2yPEBk\WyuczygUGM2OD1|MT65JO69VQ>? NXrz[4dVOjF4MkG4PFM>
SK-MEL-5 cells NEjWcoJEgXSxdH;4bYNqfHliYYPzZZk> NYK5Rog5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVUh[2WubIOsJGxEPTB;ND6wNkDPxE1? MkTyNlE3OjF6OEO=
UACC257 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= NIT5OppEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFMkW3JINmdGy|LDDMR|UxRTR2Lkig{txO MoHlNlE3OjF6OEO=
UACC62 cells M2fXN2N6fG:2b4jpZ4l1gSCjc4PhfS=> NEDMfllEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFNkKgZ4VtdHNuIFzDOVA:Pi5|OTFOwG0> NUSzVpROOjF4MkG4PFM>
IGROV1 cells MUXDfZRwfG:6aXPpeJkh[XO|YYm= NXHjUpRNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO M3LVVFIyPjJzOEiz
OVCAR5 cells NGjPe3JEgXSxdH;4bYNqfHliYYPzZZk> Ml7SR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ3IHPlcIx{NCCOQ{WwQVM5NjlizszN M2O1eFIyPjJzOEiz
SKOV3 cells NFKyN|FEgXSxdH;4bYNqfHliYYPzZZk> NUPC[5pwS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNuIFzDOVA:OjhwNTFOwG0> NXu2NXl3OjF4MkG4PFM>
A498 cells NInKPYxEgXSxdH;4bYNqfHliYYPzZZk> NXrKNW9QS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyxiTFO1NF02Njh6IN88US=> Ml;iNlE3OjF6OEO=
Caki1 cells M{ezdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NUf2XGlYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> M3noZlIyPjJzOEiz
HCT116 cells M4PSXHBzd2yrZnXyZZRqd25iYYPzZZk> M4nueGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= NGXPW4MzOTd2MkS5Oi=>
HCT116 cells NGTGVWFRem:uaX\ldoF1cW:wIHHzd4F6 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= NFfxWHczOTZ3MEKyNS=>
H1299 cells M3rjbnBzd2yrZnXyZZRqd25iYYPzZZk> M4myS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOsJGlEPTB;MD6xJO69VQ>? NYX5NoFZOjF4NUCyNlE>
HCT116 cells MWLQdo9tcW[ncnH0bY9vKGG|c3H5 M2XkUmlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IFjDWFEyPiClZXzsd{Bxem:uaX\ldoF1cW:wLDDJR|UxRTBwMEGg{txO MWWxOFYyOzNzMh?=
RPMI8226 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M1zEeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? MYqyNVYzOTh6Mx?=
CHO cells NU\aVIg3TnWwY4Tpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDlcIVkfHKxcHj5d4lwdG:peTDhd5NigSxiSVO1NF0yOi5{IN88US=> MWSyNFIxPTN7NB?=
HL-60(TB) cells MojEVJJwdGmoZYLheIlwdiCjc4PhfS=> NFS4SVFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMMVYxMFSEKTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOFkh|ryP NULaXlhQOjF4MkG4PFM>
RXF393 cells NXr3VIFsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFK[RkO5N{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4xOSEQvF2= Mme5NlE3OjF6OEO=
RXF393 cells NEfWcZZEgXSxdH;4bYNqfHliYYPzZZk> NU\2ZlJYS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWliIM{mzJINmdGy|LDDMR|UxRTF3LkOg{txO NVz0dJpmOjF4MkG4PFM>

... 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.
  • 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
Smiles C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO

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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID