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 MnXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M37xUGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJOTJ7OTDoeY1idiCudX7nJINiemOrbn;tZUBk\WyuIHfyc5d1cCxiSVO1NF0xNjF3IN88US=> M3;D[lE1PTJzNEKy
HCT116 M2S5XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFW1[HhKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO NHPWVoQyPDV{MUSyNi=>
HCT116 NUj5RYxqS3m2b4TvfIlkcXS7IHHzd4F6 M1zmZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wOUDPxE1? NGPTPGgyPzl2MU[yOS=>
human mammary epithelial cells MUjDfZRwfG:6aXPpeJkh[XO|YYm= NELE[GFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP NIXoeW4yPzl2MU[yOS=>
HEK293 cells NI[1enNHfW6ldHnvckBie3OjeR?= M33pUmlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= NFz0SWcyQDNyOEW2Ny=>
HeLa cells NHXPfYFHfW6ldHnvckBie3OjeR?= Ml\yNE4{KM7:TR?= NWD6dnR3OTZiaB?= MWjJcohq[mm2aX;uJI9nKEiGQVO0MY1m\GmjdHXkJJJmeHKnc4Ppc44hd2ZiTVXGNk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbjDpckBJ\UyjIHPlcIx{KGG2IECuN{B2VSCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NXfWXYJtOTd7NU[5PFg>
HCT116 cells M{\sVHBzd2yrZnXyZZRqd25iYYPzZZk> Mon2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> NH3jZo4zODJyNUO5OC=>
H1299 cells MlziVJJwdGmoZYLheIlwdiCjc4PhfS=> MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|IHL5JG1VWyCjc4PhfUwhUUN3ME2wMlE3OSEQvF2= M3mzRVIxOjB3M{m0
H460 cells NEPLW2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{\GNFQ5KGh? MUHHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wO{DPxE1? M1rOc|IyODd|MU[w
HCT116 cells MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDWOFghcA>? MmnPS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN M4i1dFIyODd|MU[w
CCRF-CEM cells MmHaVJJwdGmoZYLheIlwdiCjc4PhfS=> NITFUWNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? MYCyNVYzOTh6Mx?=
K562 cells NWfMdY9bWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGn2[4xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTVizszN NXrRcY5JOjF4MkG4PFM>
MOLT4 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGS0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyOSEQvF2= MkTkNlE3OjF6OEO=
SR cells NEH2bJZRem:uaX\ldoF1cW:wIHHzd4F6 M37pcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2KgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuPVkh|ryP NELGdY0zOTZ{MUi4Ny=>
A549 cells M{DpOHBzd2yrZnXyZZRqd25iYYPzZZk> M133OGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= M{X3VlIyPjJzOEiz
EKVX cells NGnaU2RRem:uaX\ldoF1cW:wIHHzd4F6 NIftSpNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFXLWngh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPzVizszN MXiyNVYzOTh6Mx?=
HOP62 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 Mor1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN NVnPeZl[OjF4MkG4PFM>
HOP92 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MmLJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN M4fHN|IyPjJzOEiz
NCI-H226 cells NXrWc3dWWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmPhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> MnTTNlE3OjF6OEO=
NCI-H23 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 M3m4Z2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> NV\STVRQOjF4MkG4PFM>
NCI-H322M cells NUjEXJNxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4jmUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OjKPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{LkK2JO69VQ>? MX2yNVYzOTh6Mx?=
NCI-H460 cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjdizszN MkjYNlE3OjF6OEO=
COLO205 cells MXXQdo9tcW[ncnH0bY9vKGG|c3H5 NXfLcmRKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? MYmyNVYzOTh6Mx?=
HCT116 cells M3v3cHBzd2yrZnXyZZRqd25iYYPzZZk> MoTERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzR5IN88US=> MVqyNVYzOTh6Mx?=
HCT15 cells MlPpVJJwdGmoZYLheIlwdiCjc4PhfS=> MoLXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4xPyEQvF2= MYGyNVYzOTh6Mx?=
HT-29 cells MkPRVJJwdGmoZYLheIlwdiCjc4PhfS=> M2DLdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTZ4IN88US=> M4HuPVIyPjJzOEiz
KM12 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NVOzdFMzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> MlLSNlE3OjF6OEO=
SW620 cells M2HLPXBzd2yrZnXyZZRqd25iYYPzZZk> MmTFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN M3fVdlIyPjJzOEiz
SF268 cells MlzqVJJwdGmoZYLheIlwdiCjc4PhfS=> NGPmZW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlY5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjV|IN88US=> M{i0ZVIyPjJzOEiz
SF295 cells M3rOZXBzd2yrZnXyZZRqd25iYYPzZZk> NUfmN3ZnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO NUPjenNkOjF4MkG4PFM>
SF539 cells NIXON5JRem:uaX\ldoF1cW:wIHHzd4F6 NULFbZRqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlU{QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57NkWg{txO MnryNlE3OjF6OEO=
SNB19 cells M2HmbXBzd2yrZnXyZZRqd25iYYPzZZk> M4XaU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CNVkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN NHTQXWUzOTZ{MUi4Ny=>
SNB75 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 M2XM[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> MUCyNVYzOTh6Mx?=
U251 cells MojmVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn;YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NFOxTYQzOTZ{MUi4Ny=>
LOXIMVI cells M1rNVnBzd2yrZnXyZZRqd25iYYPzZZk> MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN M4jORVIyPjJzOEiz
MALME-3M cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 MnLmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQVzNSU0{VSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NkGg{txO NHv3T5gzOTZ{MUi4Ny=>
M14 cells Ml[0VJJwdGmoZYLheIlwdiCjc4PhfS=> M4PweWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTUG0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlg1QSEQvF2= M4DHS|IyPjJzOEiz
MDA-MB-435 cells NF;4XVlRem:uaX\ldoF1cW:wIHHzd4F6 M{DPfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP NIfuU4EzOTZ{MUi4Ny=>
SK-MEL-28 cells M3Tac3Bzd2yrZnXyZZRqd25iYYPzZZk> NU[3c4x2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= NWXFW5hEOjF4MkG4PFM>
SK-MEL-5 cells MkXWVJJwdGmoZYLheIlwdiCjc4PhfS=> MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ5MTFOwG0> NYe0cIp5OjF4MkG4PFM>
UACC257 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 MkPIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDNlU4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN7MzFOwG0> NFWzVoYzOTZ{MUi4Ny=>
UACC62 cells M2m5UXBzd2yrZnXyZZRqd25iYYPzZZk> M4PpdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|YzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN5OTFOwG0> MlnBNlE3OjF6OEO=
IGROV1 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 MnPoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCLR2LPWlEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTh5IN88US=> M33qclIyPjJzOEiz
OVCAR3 cells NEHDW5NRem:uaX\ldoF1cW:wIHHzd4F6 NELBN2RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> M37SeFIyPjJzOEiz
OVCAR4 cells NWHFNJVoWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHH4SoFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> NVXDNnd{OjF4MkG4PFM>
OVCAR5 cells NVzMc4t4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHyy[3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NjFOwG0> NWHv[m97OjF4MkG4PFM>
OVCAR8 cells NYHNPXpNWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWrjbZJGSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO NF;tbYwzOTZ{MUi4Ny=>
NCI/ADR-RES cells MoflVJJwdGmoZYLheIlwdiCjc4PhfS=> MnHPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mvRWRTNVKHUzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6xPEDPxE1? MWOyNVYzOTh6Mx?=
SKOV3 cells NXHV[WRSWHKxbHnm[ZJifGmxbjDhd5NigQ>? MorSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN NELodYMzOTZ{MUi4Ny=>
786-0 cells M2rJUHBzd2yrZnXyZZRqd25iYYPzZZk> NIPFeINCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEe4Ok0xKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjN6IN88US=> NIPTZWozOTZ{MUi4Ny=>
A498 cells MnzxVJJwdGmoZYLheIlwdiCjc4PhfS=> MnH2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNEm4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEyKM7:TR?= M{PW[|IyPjJzOEiz
ACHN cells NEnWVFNRem:uaX\ldoF1cW:wIHHzd4F6 M4nEO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= MWmyNVYzOTh6Mx?=
Caki1 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NX;qSGZoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC54MUmg{txO MVuyNVYzOTh6Mx?=
SN12C cells NYjtTox[WHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml\nRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTkGyR{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{46OiEQvF2= NUHDe2pEOjF4MkG4PFM>
TK10 cells M2jLRnBzd2yrZnXyZZRqd25iYYPzZZk> NULSfo9sSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> NWC4NIpvOjF4MkG4PFM>
UO31 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 MnK5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXT{OxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ2OiEQvF2= M4rEblIyPjJzOEiz
PC3 cells NGrJVZZRem:uaX\ldoF1cW:wIHHzd4F6 MoLzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKwJO69VQ>? NGXyZWQzOTZ{MUi4Ny=>
DU145 cells NGnTNINRem:uaX\ldoF1cW:wIHHzd4F6 NXP4VFNqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> NUnpTJVMOjF4MkG4PFM>
MCF7 cells M2LBbHBzd2yrZnXyZZRqd25iYYPzZZk> M13kO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok46OSEQvF2= MUiyNVYzOTh6Mx?=
MDA-MB-231 cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 M2m5NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{GuO{DPxE1? MnPTNlE3OjF6OEO=
Hs 578T cells Mnz0VJJwdGmoZYLheIlwdiCjc4PhfS=> NV;QbHpbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDId{A2PziWIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13LkiyJO69VQ>? M2D2[lIyPjJzOEiz
BT549 cells Ml\JVJJwdGmoZYLheIlwdiCjc4PhfS=> M4X5fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvODRizszN NV:xZ3BoOjF4MkG4PFM>
T47D cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 NXvScpM2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQC56IN88US=> M1jPVVIyPjJzOEiz
MDA-MB-468 cells M1L6UnBzd2yrZnXyZZRqd25iYYPzZZk> MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEig{txO NF7hdHQzOTZ{MUi4Ny=>
NCI-H226 cells NHjERXlEgXSxdH;4bYNqfHliYYPzZZk> NHHpboxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> M4PVdFIyPjJzOEiz
KM12 cells MnvqR5l1d3SxeHnjbZR6KGG|c3H5 NXPue3pqS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU01zMjDj[YxteyxiTFO1NF0zQS57IN88US=> NIPJUW4zOTZ{MUi4Ny=>
SF295 cells M3nDc2N6fG:2b4jpZ4l1gSCjc4PhfS=> MoXHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= NGrCdowzOTZ{MUi4Ny=>
SNB19 cells MUnDfZRwfG:6aXPpeJkh[XO|YYm= MV\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTUmIyQSClZXzsd{whVEN3ME2zNU44KM7:TR?= M4jrNVIyPjJzOEiz
U251 cells M2jpNWN6fG:2b4jpZ4l1gSCjc4PhfS=> M{nB[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHUzPTFiY3XscJMtKEyFNUC9OU45OiEQvF2= NHHxU4szOTZ{MUi4Ny=>
LOXIMVI cells MULDfZRwfG:6aXPpeJkh[XO|YYm= NV3mcXcyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE:[SV3WTUBk\WyuczygUGM2OD14LkC0JO69VQ>? NHHPUokzOTZ{MUi4Ny=>
MDA-MB-435 cells NFnXO2xEgXSxdH;4bYNqfHliYYPzZZk> M4\US2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? NIPwS2UzOTZ{MUi4Ny=>
SK-MEL-28 cells Mlr3R5l1d3SxeHnjbZR6KGG|c3H5 Mnf4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy|LDDMR|UxRTNzLkmg{txO MmT3NlE3OjF6OEO=
SK-MEL-5 cells M4jNXWN6fG:2b4jpZ4l1gSCjc4PhfS=> MkXSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUWgZ4VtdHNuIFzDOVA:PC5yMjFOwG0> NHzndHUzOTZ{MUi4Ny=>
UACC257 cells MUnDfZRwfG:6aXPpeJkh[XO|YYm= M4fxb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N{NUegZ4VtdHNuIFzDOVA:PDRwODFOwG0> MV2yNVYzOTh6Mx?=
UACC62 cells NYHmVGh3S3m2b4TvfIlkcXS7IHHzd4F6 NUmzUYFvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{[yJINmdGy|LDDMR|UxRTZwM{mg{txO NH62WFczOTZ{MUi4Ny=>
IGROV1 cells M{XCNWN6fG:2b4jpZ4l1gSCjc4PhfS=> NVTZ[lQ3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO NVLieVRNOjF4MkG4PFM>
OVCAR5 cells MX\DfZRwfG:6aXPpeJkh[XO|YYm= NWfDO5YxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO NF\5TlMzOTZ{MUi4Ny=>
SKOV3 cells MXzDfZRwfG:6aXPpeJkh[XO|YYm= NHm3PI1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUU0:YMzDj[YxteyxiTFO1NF0zQC53IN88US=> M2joRVIyPjJzOEiz
A498 cells NEPqVldEgXSxdH;4bYNqfHliYYPzZZk> NULCdWVHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyxiTFO1NF02Njh6IN88US=> NWH6SYU6OjF4MkG4PFM>
Caki1 cells M{P4OWN6fG:2b4jpZ4l1gSCjc4PhfS=> M2Lac2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNic2lzIHPlcIx{NCCOQ{WwQVUvPzlizszN NEGwcHAzOTZ{MUi4Ny=>
HCT116 cells NIH2[5pRem:uaX\ldoF1cW:wIHHzd4F6 MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczygTWM2OD1yLkCxPUDPxE1? M375VVIyPzR{NEm2
HCT116 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= MlPXNlE3PTB{MkG=
H1299 cells NG\KV5VRem:uaX\ldoF1cW:wIHHzd4F6 MoiyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OD1yLkGg{txO MVyyNVY2ODJ{MR?=
HCT116 cells NF[4TYtRem:uaX\ldoF1cW:wIHHzd4F6 MYfJcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKQ2SxNVYh[2WubIOgdJJwdGmoZYLheIlwdixiSVO1NF0xNjBzIN88US=> NH7WUGkyPDZzM{OxNi=>
RPMI8226 cells NVPOfmdPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYrG[lZOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61NlMh|ryP NHP4d4MzOTZ{MUi4Ny=>
CHO cells MmPzSpVv[3Srb36gZZN{[Xl? MUfJcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KGG3dH;tZZRm\CCyYYTjbEBkdGGvcDDlcIVkfHKxcHj5d4lwdG:peTDhd5NigSxiSVO1NF0yOi5{IN88US=> NInlSI8zODJyNUO5OC=>
HL-60(TB) cells NVLmbY1uWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiOLU[wLHRDMSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NEmg{txO MlezNlE3OjF6OEO=
RXF393 cells M{LIN3Bzd2yrZnXyZZRqd25iYYPzZZk> MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFK[RkO5N{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4xOSEQvF2= MUKyNVYzOTh6Mx?=
RXF393 cells NGPjRlVEgXSxdH;4bYNqfHliYYPzZZk> Mn70R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN MmL4NlE3OjF6OEO=

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 379.459
Formula

C22H25N3O3

CAS No. 404951-53-7
Storage powder
Synonyms NVP-LAQ824

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID