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.

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.

Purity & Quality Control

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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 MnfiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEKwVGFKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> MV:xOFUzOTR{Mh?=
HCT116 MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTGNVOTF4IHj1cYFvKGOxbH;uJINmdGxiZ4Lve5RpNCCLQ{WwQVAvODFizszN MYKxOFUzOTR{Mh?=
HCT116 M4LlbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEWg{txO MV6xO|k1OTZ{NR?=
human mammary epithelial cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MoPiR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NHfYeWwyPzl2MU[yOS=>
HEK293 cells NIeyOFBHfW6ldHnvckBie3OjeR?= MlyyTY5pcWKrdHnvckBw\iCKRFHDNUBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6wNFI3KM7:TR?= NHjqW44yQDNyOEW2Ny=>
HeLa cells MlLPSpVv[3Srb36gZZN{[Xl? NEXXRmwxNjNizszN M1jkWFE3KGh? NH22OHVKdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 Mo\RNVc6PTZ7OEi=
HCT116 cells MmLHVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn;JRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> NXm5TmZFOjB{MEWzPVQ>
H1299 cells M3K1R3Bzd2yrZnXyZZRqd25iYYPzZZk> M4\WRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> NH7sVGUzODJyNUO5OC=>
H460 cells MknpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;oUGk1QCCq M2LFemdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA4KM7:TR?= MlHmNlExPzNzNkC=
HCT116 cells M1PKemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXudGg1QCCq MVHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAyQCEQvF2= M{X2blIyODd|MU[w
CCRF-CEM cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> NEO3RlIzOTZ{MUi4Ny=>
K562 cells NVT5e2o{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVUh|ryP NIe2cXEzOTZ{MUi4Ny=>
MOLT4 cells NIGwcmhRem:uaX\ldoF1cW:wIHHzd4F6 NXjHb2lmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MV6yNVYzOTh6Mx?=
SR cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 MorORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj65PUDPxE1? NXm3WIk1OjF4MkG4PFM>
A549 cells Mlm5VJJwdGmoZYLheIlwdiCjc4PhfS=> M1L3RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= NI\HWIszOTZ{MUi4Ny=>
EKVX cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP NFv1dWczOTZ{MUi4Ny=>
HOP62 cells M2nYOHBzd2yrZnXyZZRqd25iYYPzZZk> NV:0NmcySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MEKg{txO M3W2XlIyPjJzOEiz
HOP92 cells NFnhWYpRem:uaX\ldoF1cW:wIHHzd4F6 MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUEmyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE6QSEQvF2= NED4V4YzOTZ{MUi4Ny=>
NCI-H226 cells NXrJW2kzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmW2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> MmfVNlE3OjF6OEO=
NCI-H23 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 M3LtfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> M36zbVIyPjJzOEiz
NCI-H322M cells M2O0OHBzd2yrZnXyZZRqd25iYYPzZZk> MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|IzVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5{NjFOwG0> M3\RO|IyPjJzOEiz
NCI-H460 cells NGnI[ZpRem:uaX\ldoF1cW:wIHHzd4F6 M4LQWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PjBiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNzFOwG0> MWWyNVYzOTh6Mx?=
COLO205 cells NGjlSVZRem:uaX\ldoF1cW:wIHHzd4F6 NHzqdG9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO NV;sclV4OjF4MkG4PFM>
HCT116 cells NEC0SXFRem:uaX\ldoF1cW:wIHHzd4F6 M3qweGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN2NzFOwG0> MYiyNVYzOTh6Mx?=
HCT15 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 NYDtd|AxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> NVPTdmFVOjF4MkG4PFM>
HT-29 cells MlzGVJJwdGmoZYLheIlwdiCjc4PhfS=> MnX5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN NYflOpNLOjF4MkG4PFM>
KM12 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NGnrS5FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODRizszN MUSyNVYzOTh6Mx?=
SW620 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 MlfaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN NFviVWYzOTZ{MUi4Ny=>
SF268 cells NXPvd5dlWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWnh[op7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> NWPQ[GFpOjF4MkG4PFM>
SF295 cells MkP3VJJwdGmoZYLheIlwdiCjc4PhfS=> NITUXWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlk2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd2MzFOwG0> NFHMXnUzOTZ{MUi4Ny=>
SF539 cells Mk\oVJJwdGmoZYLheIlwdiCjc4PhfS=> NXvoV2dGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlU{QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57NkWg{txO NYn0R3plOjF4MkG4PFM>
SNB19 cells NGLaU4NRem:uaX\ldoF1cW:wIHHzd4F6 MkCxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= NE\oWJAzOTZ{MUi4Ny=>
SNB75 cells NH\Dbm1Rem:uaX\ldoF1cW:wIHHzd4F6 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= M4\Jc|IyPjJzOEiz
U251 cells NYTXdoVEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVzpW28xSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> NVG5NWNmOjF4MkG4PFM>
LOXIMVI cells Mn;iVJJwdGmoZYLheIlwdiCjc4PhfS=> MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MUiyNVYzOTh6Mx?=
MALME-3M cells Mli3VJJwdGmoZYLheIlwdiCjc4PhfS=> MkXmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQVzNSU0{VSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NkGg{txO M4D3S|IyPjJzOEiz
M14 cells NXPnOW01WHKxbHnm[ZJifGmxbjDhd5NigQ>? NEDCSoZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2xOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE45PDlizszN MXOyNVYzOTh6Mx?=
MDA-MB-435 cells NIrrWJZRem:uaX\ldoF1cW:wIHHzd4F6 MnztRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? NXPjN|FwOjF4MkG4PFM>
SK-MEL-28 cells MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 NI\xcmZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD65PVMh|ryP NYPNfJYzOjF4MkG4PFM>
SK-MEL-5 cells NIHPbG1Rem:uaX\ldoF1cW:wIHHzd4F6 Ml64RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{N{Gg{txO M2DxNVIyPjJzOEiz
UACC257 cells NYLqPZBWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1zQW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO MVuyNVYzOTh6Mx?=
UACC62 cells M1;zSXBzd2yrZnXyZZRqd25iYYPzZZk> MnvkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> NIW3WZkzOTZ{MUi4Ny=>
IGROV1 cells MmfKVJJwdGmoZYLheIlwdiCjc4PhfS=> MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN NFL3SnUzOTZ{MUi4Ny=>
OVCAR3 cells M{S0[3Bzd2yrZnXyZZRqd25iYYPzZZk> NX3CTFBDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMUGg{txO MljtNlE3OjF6OEO=
OVCAR4 cells M4PU[HBzd2yrZnXyZZRqd25iYYPzZZk> NHvNe5pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> NUD4UlhIOjF4MkG4PFM>
OVCAR5 cells NXG1[op{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlTORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOjZizszN NHPIXYwzOTZ{MUi4Ny=>
OVCAR8 cells MoTVVJJwdGmoZYLheIlwdiCjc4PhfS=> M{e4VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> MnriNlE3OjF6OEO=
NCI/ADR-RES cells MoHuVJJwdGmoZYLheIlwdiCjc4PhfS=> NHniTlhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU9CTFJvUlXTJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE5KM7:TR?= MX2yNVYzOTh6Mx?=
SKOV3 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUzPCEQvF2= MW[yNVYzOTh6Mx?=
786-0 cells MkPqVJJwdGmoZYLheIlwdiCjc4PhfS=> MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= MnfhNlE3OjF6OEO=
A498 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M1\XUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NFPteFgzOTZ{MUi4Ny=>
ACHN cells MXvQdo9tcW[ncnH0bY9vKGG|c3H5 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? MVOyNVYzOTh6Mx?=
Caki1 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 MlTJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYXvpNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE43OTlizszN NGLVXoszOTZ{MUi4Ny=>
SN12C cells NWWzdVBYWHKxbHnm[ZJifGmxbjDhd5NigQ>? NITSSJZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPONVJEKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{Njl{IN88US=> M4TrSlIyPjJzOEiz
TK10 cells Mn\XVJJwdGmoZYLheIlwdiCjc4PhfS=> MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= MXiyNVYzOTh6Mx?=
UO31 cells NVLifml7WHKxbHnm[ZJifGmxbjDhd5NigQ>? NX3CcHY1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> MYmyNVYzOTh6Mx?=
PC3 cells MoHEVJJwdGmoZYLheIlwdiCjc4PhfS=> MnHwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKwJO69VQ>? M3L0NFIyPjJzOEiz
DU145 cells NFj2S2dRem:uaX\ldoF1cW:wIHHzd4F6 NIjsW2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQS57IN88US=> MlfZNlE3OjF6OEO=
MCF7 cells NUTlUYJpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPU[uPVEh|ryP M{\rPVIyPjJzOEiz
MDA-MB-231 cells NE[0UFBRem:uaX\ldoF1cW:wIHHzd4F6 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNzLkeg{txO MXuyNVYzOTh6Mx?=
Hs 578T cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NI\nUlZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjzJFU4QFRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEKg{txO NIrZVnEzOTZ{MUi4Ny=>
BT549 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlA1KM7:TR?= M3n4e|IyPjJzOEiz
T47D cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 NGHO[4RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI5NjhizszN MoS4NlE3OjF6OEO=
MDA-MB-468 cells Mn35VJJwdGmoZYLheIlwdiCjc4PhfS=> M1TWUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? NFjheXkzOTZ{MUi4Ny=>
NCI-H226 cells MmTDR5l1d3SxeHnjbZR6KGG|c3H5 NYnGVYRFS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLViyNlYh[2WubIOsJGxEPTB;MkCg{txO MXmyNVYzOTh6Mx?=
KM12 cells M3XufmN6fG:2b4jpZ4l1gSCjc4PhfS=> NHTZVnpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMVTF{IHPlcIx{NCCOQ{WwQVI6NjlizszN NEfqU2YzOTZ{MUi4Ny=>
SF295 cells NIfNZ3JEgXSxdH;4bYNqfHliYYPzZZk> M{Szb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjl3IHPlcIx{NCCOQ{WwQVYvQTFizszN MV6yNVYzOTh6Mx?=
SNB19 cells M{LjSmN6fG:2b4jpZ4l1gSCjc4PhfS=> NYLZco5HS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06EMUmgZ4VtdHNuIFzDOVA:OzFwNzFOwG0> MX2yNVYzOTh6Mx?=
U251 cells NF\tWZNEgXSxdH;4bYNqfHliYYPzZZk> NX3xXGQ2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTJ3MTDj[YxteyxiTFO1NF02Njh{IN88US=> M2fvSFIyPjJzOEiz
LOXIMVI cells M{TuR2N6fG:2b4jpZ4l1gSCjc4PhfS=> M3HkbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxQYEmPVlmgZ4VtdHNuIFzDOVA:Pi5yNDFOwG0> NHLTdVQzOTZ{MUi4Ny=>
MDA-MB-435 cells NGP4UnNEgXSxdH;4bYNqfHliYYPzZZk> NFHlW3ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzMEBNSzVyPUK4Mlgh|ryP MV[yNVYzOTh6Mx?=
SK-MEL-28 cells M2PvTGN6fG:2b4jpZ4l1gSCjc4PhfS=> NUG3UlZxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzMEBNSzVyPUOxMlkh|ryP MmOyNlE3OjF6OEO=
SK-MEL-5 cells NYDDbItnS3m2b4TvfIlkcXS7IHHzd4F6 NEDhVFhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? MWCyNVYzOTh6Mx?=
UACC257 cells Mmq5R5l1d3SxeHnjbZR6KGG|c3H5 NXr6V5NqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? M1Lj[|IyPjJzOEiz
UACC62 cells NIfzPGREgXSxdH;4bYNqfHliYYPzZZk> NITEdYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFNkKgZ4VtdHNuIFzDOVA:Pi5|OTFOwG0> MoH0NlE3OjF6OEO=
IGROV1 cells MoTvR5l1d3SxeHnjbZR6KGG|c3H5 Mn3JR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTWdTV1ZzIHPlcIx{NCCOQ{WwQVQ5NjlizszN M{ntSlIyPjJzOEiz
OVCAR5 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= NHXXWFJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBQXkODUkWgZ4VtdHNuIFzDOVA:OzhwOTFOwG0> NXHiSY1SOjF4MkG4PFM>
SKOV3 cells NHHQVnREgXSxdH;4bYNqfHliYYPzZZk> M1rrWWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCOQ{WwQVI5NjVizszN NGHHWYEzOTZ{MUi4Ny=>
A498 cells MmDiR5l1d3SxeHnjbZR6KGG|c3H5 NVrNcVA{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyxiTFO1NF02Njh6IN88US=> MXyyNVYzOTh6Mx?=
Caki1 cells MmPyR5l1d3SxeHnjbZR6KGG|c3H5 MojCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR4FscTFiY3XscJMtKEyFNUC9OU44QSEQvF2= NHzPXpYzOTZ{MUi4Ny=>
HCT116 cells M4XIPHBzd2yrZnXyZZRqd25iYYPzZZk> MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczygTWM2OD1yLkCxPUDPxE1? NHnFSIQzOTd2MkS5Oi=>
HCT116 cells M2DUXHBzd2yrZnXyZZRqd25iYYPzZZk> M3rM[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> MY[yNVY2ODJ{MR?=
H1299 cells M12zcnBzd2yrZnXyZZRqd25iYYPzZZk> MnL3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OD1yLkGg{txO NH7WO2ozOTZ3MEKyNS=>
HCT116 cells NUTmNpZWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NETjTmtKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDIR3QyOTZiY3XscJMheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCxJO69VQ>? MoTaNVQ3OTN|MUK=
RPMI8226 cells NWjHblNWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVjQT4JwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61NlMh|ryP MYKyNVYzOTh6Mx?=
CHO cells M{jWN2Z2dmO2aX;uJIF{e2G7 M17XW2lvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO MXyyNFIxPTN7NB?=
HL-60(TB) cells NF7VPWhRem:uaX\ldoF1cW:wIHHzd4F6 NVK3RW9HSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUE03OCiWQjmgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNlQ6KM7:TR?= M1XI[FIyPjJzOEiz
RXF393 cells NV33Z5VRWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFK[RkO5N{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4xOSEQvF2= MljQNlE3OjF6OEO=
RXF393 cells NGXiSpFEgXSxdH;4bYNqfHliYYPzZZk> M4ew[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJZTjN7MzDj[YxteyxiTFO1NF0yPS5|IN88US=> NEXnWJIzOTZ{MUi4Ny=>

... Click to View More Cell Line Experimental Data

In vivo In HCT116 and human colon tumor xenografts in nude mice, LAQ824 treatment at 100 mg/kg produces the inhibitory effects on tumor growth in a dose-dependent mode without general cytotoxicity. [1]

Protocol

Kinase Assay:[1]
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In Vitro Histone Deacetylase Assay:

HDAC enzymes are partially purified from H1299 cell lysate by ion exchange chromatography using the Q Sepharose Fast Flow column. Enzyme complexes are collected from 500 mg of total cell lysate by immunoprecipitation with cdk2 polyclonal antibody or cdk1/cdc2 monoclonal antibody. Immunoprecipitates are resuspended in kinase buffer (50 mM Hepes, pH 8, 10 mM MgCl2, 2.5 mM EDTA, 1 mM dithiothreitol, 20 mM ATP, 10 mM β-glycerophosphate, 0.1 mM NaVO4, 1 mM sodium fluoride, 50 mM ATP, 10 μCi of [γ-32P]ATP) along with 1 μg of pRb recombinant protein substrate (cdk2) or 10 mL of H1 histone mixture containing 20 μg of substrate (cdc2). Phosphorylated Rb and H1 histone are resolved by electrophoresis and quantitated using a PhosphorImager.
Cell Research:[1]
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  • Cell lines: H1299, HCT116, DU145, PC3 and MDA435 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 48 hours
  • Method: Cell proliferation is measured using an adaptation of published procedures (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxy-phenyl)-2-(4-sulfonyl)-2H-tetrazolium assay). The cells are seeded in 12-well dishes and cultured in RPMI 1640 containing 10% FBS. The cells are cultured in the presence of various concentrations of TSA (up to 1,000 ng/mL). To examine the growth inhibition by TSA, viable cell numbers are determined by trypan blue dye exclusion, counted in a Nesbauer-type hemocytometer for 0 hour, 24 hours, and 48 hours. The same amount of ethanol is added to the RPMI 1640 medium as the control experiment. All experiments are performed in duplicate and repeated 3 times The average background value (treatment with medium alone) is subtracted from each experimental well; triplicate values are averaged for each compound dilution. The following formulas are used to calculate the percentage of growth: If X0, %Growth=(X-T0)/T0*100; If X>T0, %Growth=(X-T0)/(GC-T0)*100. where T0 is the average value of T0 − background, GC is the average value of untreated cells (in triplicate) − background, and X is the average value of compound-treated cells (in triplicate)-background. The “% Growth” is plotted against compound concentration and used to calculate the IC50 using the linear regression techniques between data points to predict the concentration of compounds at 50% inhibition.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
  • 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

In vivo Formulation Calculator (Clear solution)

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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