Dacinostat (LAQ824)

Catalog No.S1095 Synonyms: NVP-LAQ824

Dacinostat (LAQ824) Chemical Structure

Molecular Weight(MW): 379.459

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

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In DMSO USD 420 In stock
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Cited by 8 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.

  • 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 NEPP[ZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHqwbJdKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> NVz5WJloOTR3MkG0NlI>
HCT116 NX;pOI95T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHHKUGdKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO NV\repBjOTR3MkG0NlI>
HCT116 MUjDfZRwfG:6aXPpeJkh[XO|YYm= NVq3coJlS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= MnvGNVc6PDF4MkW=
human mammary epithelial cells M3XTWWN6fG:2b4jpZ4l1gSCjc4PhfS=> MlfHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? MXOxO|k1OTZ{NR?=
HEK293 cells NI\sT5dHfW6ldHnvckBie3OjeR?= M2PlcGlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= NHzNUmUyQDNyOEW2Ny=>
HeLa cells NHraclVHfW6ldHnvckBie3OjeR?= MkG2NE4{KM7:TR?= NEnV[IQyPiCq NFfNVGFKdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NIq4PZUyPzl3Nkm4PC=>
HCT116 cells NWf3ZlQzWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYLKbnptSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMEGzJO69VQ>? NIL3cpMzODJyNUO5OC=>
H1299 cells M1nTT3Bzd2yrZnXyZZRqd25iYYPzZZk> NUPqTldCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5zNkGg{txO NFqxSnQzODJyNUO5OC=>
H460 cells NGrGTpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4jCZVQ5KGh? MmXqS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP MXeyNVA4OzF4MB?=
HCT116 cells NIL3UnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PyeVQ5KGh? Mn\OS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN NGHiUokzOTB5M{G2NC=>
CCRF-CEM cells MkTsVJJwdGmoZYLheIlwdiCjc4PhfS=> M1HSRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PSSk1ETU1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkWxJO69VQ>? MXGyNVYzOTh6Mx?=
K562 cells M4\HUHBzd2yrZnXyZZRqd25iYYPzZZk> NWrlN5dqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> MoDKNlE3OjF6OEO=
MOLT4 cells MlHtVJJwdGmoZYLheIlwdiCjc4PhfS=> M1;GVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MWFQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzFzIN88US=> MXyyNVYzOTh6Mx?=
SR cells MlLHVJJwdGmoZYLheIlwdiCjc4PhfS=> MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{Lkm5JO69VQ>? MUWyNVYzOTh6Mx?=
A549 cells M{PXZnBzd2yrZnXyZZRqd25iYYPzZZk> NGrUdWlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NWDNenVyOjF4MkG4PFM>
EKVX cells MljNVJJwdGmoZYLheIlwdiCjc4PhfS=> MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP NXP5UXNSOjF4MkG4PFM>
HOP62 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 MoHFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN MVOyNVYzOTh6Mx?=
HOP92 cells M3\iUnBzd2yrZnXyZZRqd25iYYPzZZk> MnTIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN NYTQfVhZOjF4MkG4PFM>
NCI-H226 cells M3zuWHBzd2yrZnXyZZRqd25iYYPzZZk> NVTLVVZ5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MT60NUDPxE1? NH7JRVAzOTZ{MUi4Ny=>
NCI-H23 cells M3nqOnBzd2yrZnXyZZRqd25iYYPzZZk> NV7VXY9nSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO M{\UblIyPjJzOEiz
NCI-H322M cells NX36cnpYWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IN|IzVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5{NjFOwG0> MVSyNVYzOTh6Mx?=
NCI-H460 cells NHHKcVZRem:uaX\ldoF1cW:wIHHzd4F6 NEXMOJRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkeg{txO NV;xWGZDOjF4MkG4PFM>
COLO205 cells NGjoVpFRem:uaX\ldoF1cW:wIHHzd4F6 MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MXOyNVYzOTh6Mx?=
HCT116 cells M2S0eXBzd2yrZnXyZZRqd25iYYPzZZk> M4jUemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN2NzFOwG0> Mo\wNlE3OjF6OEO=
HCT15 cells NXPpPG4xWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEPWO4xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> MWOyNVYzOTh6Mx?=
HT-29 cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 MnHXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN MUeyNVYzOTh6Mx?=
KM12 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPMUKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNFQh|ryP M2H5dVIyPjJzOEiz
SW620 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 MnGyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN M3q2WVIyPjJzOEiz
SF268 cells NUK5N5ZWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M17vSWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN MV6yNVYzOTh6Mx?=
SF295 cells NFrNXm5Rem:uaX\ldoF1cW:wIHHzd4F6 NYDJdnNySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO MVWyNVYzOTh6Mx?=
SF539 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 Mn33RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkWzPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE46PjVizszN NYq5XmJGOjF4MkG4PFM>
SNB19 cells NF;5UYxRem:uaX\ldoF1cW:wIHHzd4F6 MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NYDC[|IxOjF4MkG4PFM>
SNB75 cells M2nSOnBzd2yrZnXyZZRqd25iYYPzZZk> MmDwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlK3OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OThizszN MXmyNVYzOTh6Mx?=
U251 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MoDoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NYnNZoVtOjF4MkG4PFM>
LOXIMVI cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN Mki4NlE3OjF6OEO=
MALME-3M cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MlrTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQVzNSU0{VSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NkGg{txO MnrMNlE3OjF6OEO=
M14 cells NWPhRmJ{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIO1NnFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2xOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE45PDlizszN NUXvbVdYOjF4MkG4PFM>
MDA-MB-435 cells NYfaSXc4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUHlO3k1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU{PyEQvF2= NFezXXczOTZ{MUi4Ny=>
SK-MEL-28 cells MkDJVJJwdGmoZYLheIlwdiCjc4PhfS=> M2\3fWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkm5N{DPxE1? NWXxNlZ6OjF4MkG4PFM>
SK-MEL-5 cells NYjlVYUxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ5MTFOwG0> MXSyNVYzOTh6Mx?=
UACC257 cells NVSySoxrWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2PtOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO NXPCNlFjOjF4MkG4PFM>
UACC62 cells MkjXVJJwdGmoZYLheIlwdiCjc4PhfS=> NVPrZ5J6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{e5JO69VQ>? NGHtb4czOTZ{MUi4Ny=>
IGROV1 cells Mn76VJJwdGmoZYLheIlwdiCjc4PhfS=> NXryc|NzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? NVfLb41YOjF4MkG4PFM>
OVCAR3 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 MnfhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN Mk\FNlE3OjF6OEO=
OVCAR4 cells NHLnTlhRem:uaX\ldoF1cW:wIHHzd4F6 MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{4zOSEQvF2= NX:2dY5TOjF4MkG4PFM>
OVCAR5 cells M4jv[3Bzd2yrZnXyZZRqd25iYYPzZZk> M1fDXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> MnHPNlE3OjF6OEO=
OVCAR8 cells M4jKeXBzd2yrZnXyZZRqd25iYYPzZZk> M32wfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> MWiyNVYzOTh6Mx?=
NCI/ADR-RES cells NWrrVYQ3WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkTPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mvRWRTNVKHUzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6xPEDPxE1? M{Hnc|IyPjJzOEiz
SKOV3 cells NHjudmlRem:uaX\ldoF1cW:wIHHzd4F6 NGTEU3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{NDFOwG0> MojENlE3OjF6OEO=
786-0 cells MV7Qdo9tcW[ncnH0bY9vKGG|c3H5 NGXwfZRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEe4Ok0xKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjN6IN88US=> M1jxdFIyPjJzOEiz
A498 cells NH:wNmVRem:uaX\ldoF1cW:wIHHzd4F6 M3jEN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NFPSbm0zOTZ{MUi4Ny=>
ACHN cells NWSyfZNWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4jPWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= NFrYXZEzOTZ{MUi4Ny=>
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TK10 cells NVS3[Gt5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NI\TbZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTLNVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDR2IN88US=> NUj3O|RLOjF4MkG4PFM>
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MDA-MB-231 cells NHXnT|VRem:uaX\ldoF1cW:wIHHzd4F6 MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNzLkeg{txO NEDWVXYzOTZ{MUi4Ny=>
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BT549 cells MmfyVJJwdGmoZYLheIlwdiCjc4PhfS=> M3ri[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvODRizszN NWniPWdCOjF4MkG4PFM>
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UACC257 cells NHzmbGlEgXSxdH;4bYNqfHliYYPzZZk> NUXW[JoxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? MU[yNVYzOTh6Mx?=
UACC62 cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= M{TnemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> NGPYVI4zOTZ{MUi4Ny=>
IGROV1 cells NWDSfYlUS3m2b4TvfIlkcXS7IHHzd4F6 MXXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= NGnldI4zOTZ{MUi4Ny=>
OVCAR5 cells M4rEWWN6fG:2b4jpZ4l1gSCjc4PhfS=> MnzUR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ3IHPlcIx{NCCOQ{WwQVM5NjlizszN MWWyNVYzOTh6Mx?=
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Caki1 cells MoOxR5l1d3SxeHnjbZR6KGG|c3H5 MlPiR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR4FscTFiY3XscJMtKEyFNUC9OU44QSEQvF2= M1LKNlIyPjJzOEiz
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HCT116 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 M1XJUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> MVGyNVY2ODJ{MR?=
H1299 cells NGjqOZZRem:uaX\ldoF1cW:wIHHzd4F6 NFrsOWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzMEBKSzVyPUCuNUDPxE1? NV[1e2tQOjF4NUCyNlE>
HCT116 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 M3rV[WlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IFjDWFEyPiClZXzsd{Bxem:uaX\ldoF1cW:wLDDJR|UxRTBwMEGg{txO M1jESFE1PjF|M{Gy
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CHO cells MnTzSpVv[3Srb36gZZN{[Xl? M2TvXGlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO NVv6R4Z2OjB{MEWzPVQ>
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RXF393 cells M1\CS3Bzd2yrZnXyZZRqd25iYYPzZZk> MoXIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN MlzPNlE3OjF6OEO=
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... 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