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 MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3z3[2lvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJOTJ7OTDoeY1idiCudX7nJINiemOrbn;tZUBk\WyuIHfyc5d1cCxiSVO1NF0xNjF3IN88US=> MYmxOFUzOTR{Mh?=
HCT116 M2Oyd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIfOVplKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO NVzWNGF2OTR3MkG0NlI>
HCT116 NES2dWZEgXSxdH;4bYNqfHliYYPzZZk> MnTXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC1JO69VQ>? NU\STnJzOTd7NEG2NlU>
human mammary epithelial cells NYjqNYVYS3m2b4TvfIlkcXS7IHHzd4F6 NIXWXVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP MYOxO|k1OTZ{NR?=
HEK293 cells M4XvN2Z2dmO2aX;uJIF{e2G7 MlvETY5pcWKrdHnvckBw\iCKRFHDNUBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6wNFI3KM7:TR?= M{W2SVE5OzB6NU[z
HeLa cells M3y1[WZ2dmO2aX;uJIF{e2G7 NV[4eHkxOC5|IN88US=> M{S2blE3KGh? NWj1cXFNUW6qaXLpeIlwdiCxZjDISGFEPC2vZXTpZZRm\CC{ZYDy[ZN{cW:wIH;mJG1GTjJvZHXw[Y5l\W62IITyZY5{[3KrcITpc44hcW5iSHXMZUBk\WyuczDheEAxNjNidV2gZYZ1\XJiMU[gbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> M{LIOFE4QTV4OUi4
HCT116 cells NW\rNVlzWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2fjNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjBzMzFOwG0> NGHwOXozODJyNUO5OC=>
H1299 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NWTwbXJLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5zNkGg{txO MVmyNFIxPTN7NB?=
H460 cells MkH0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4nCS|Q5KGh? NGD3OGZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJPDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xPyEQvF2= NHnxTpgzOTB5M{G2NC=>
HCT116 cells NILEfFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkPXOFghcA>? NWXSZ4JRT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO NWr2V5VEOjFyN{OxOlA>
CCRF-CEM cells MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NXTXOYJSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOVEh|ryP NWnZRVJ5OjF4MkG4PFM>
K562 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVUh|ryP MXeyNVYzOTh6Mx?=
MOLT4 cells NGPkcHdRem:uaX\ldoF1cW:wIHHzd4F6 NHfG[opCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUHQ1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjNzMTFOwG0> MkHQNlE3OjF6OEO=
SR cells NInDT25Rem:uaX\ldoF1cW:wIHHzd4F6 NHvPbVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= MWqyNVYzOTh6Mx?=
A549 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 M1;tOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= MUCyNVYzOTh6Mx?=
EKVX cells MXvQdo9tcW[ncnH0bY9vKGG|c3H5 M2nzVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= NWLD[otSOjF4MkG4PFM>
HOP62 cells NEe3eHFRem:uaX\ldoF1cW:wIHHzd4F6 MkGzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN Ml7wNlE3OjF6OEO=
HOP92 cells M3njTHBzd2yrZnXyZZRqd25iYYPzZZk> NHPW[lVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFkzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF7OTFOwG0> MmH6NlE3OjF6OEO=
NCI-H226 cells M1;nenBzd2yrZnXyZZRqd25iYYPzZZk> Mnu5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> M1zhTlIyPjJzOEiz
NCI-H23 cells MmDZVJJwdGmoZYLheIlwdiCjc4PhfS=> MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPSEQvF2= MVmyNVYzOTh6Mx?=
NCI-H322M cells MWLQdo9tcW[ncnH0bY9vKGG|c3H5 M3\UWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OjKPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{LkK2JO69VQ>? MnjQNlE3OjF6OEO=
NCI-H460 cells NYD0[Jl{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NHLyd4VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JPDZyIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkeg{txO NWLmTGpbOjF4MkG4PFM>
COLO205 cells M1fTb3Bzd2yrZnXyZZRqd25iYYPzZZk> NVvETHhWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? NIjqcmszOTZ{MUi4Ny=>
HCT116 cells M1TnfHBzd2yrZnXyZZRqd25iYYPzZZk> M4fEc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN2NzFOwG0> Ml;XNlE3OjF6OEO=
HCT15 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 NX\RWlc2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> M1XOcFIyPjJzOEiz
HT-29 cells MkOxVJJwdGmoZYLheIlwdiCjc4PhfS=> MoO5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PjZizszN MmXrNlE3OjF6OEO=
KM12 cells NWq5clZrWHKxbHnm[ZJifGmxbjDhd5NigQ>? M33kNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xPCEQvF2= NF;sfZkzOTZ{MUi4Ny=>
SW620 cells MnLvVJJwdGmoZYLheIlwdiCjc4PhfS=> MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNkKwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ4QCEQvF2= NIrpVYEzOTZ{MUi4Ny=>
SF268 cells M2fDe3Bzd2yrZnXyZZRqd25iYYPzZZk> M{HmbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN M1rET|IyPjJzOEiz
SF295 cells NVXtcoRXWHKxbHnm[ZJifGmxbjDhd5NigQ>? MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= NE\VO40zOTZ{MUi4Ny=>
SF539 cells Mny1VJJwdGmoZYLheIlwdiCjc4PhfS=> NEHpb5JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGOVM6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjl4NTFOwG0> NYqwVXg3OjF4MkG4PFM>
SNB19 cells M3SyeXBzd2yrZnXyZZRqd25iYYPzZZk> MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NGXFfXUzOTZ{MUi4Ny=>
SNB75 cells NHfsZ3ZRem:uaX\ldoF1cW:wIHHzd4F6 NWKxR4VMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmI4PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUig{txO M3K4b|IyPjJzOEiz
U251 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 Ml30RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= M1XROFIyPjJzOEiz
LOXIMVI cells NYDaTGFnWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGe0Z4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO MWGyNVYzOTh6Mx?=
MALME-3M cells NX;Le|hJWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> M3jBXlIyPjJzOEiz
M14 cells NEnVXG5Rem:uaX\ldoF1cW:wIHHzd4F6 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1zNDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD64OFkh|ryP M4r5OlIyPjJzOEiz
MDA-MB-435 cells M{W5[XBzd2yrZnXyZZRqd25iYYPzZZk> NUS5c|BKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU{PyEQvF2= MnrBNlE3OjF6OEO=
SK-MEL-28 cells NGr2UYxRem:uaX\ldoF1cW:wIHHzd4F6 MkPuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? MWiyNVYzOTh6Mx?=
SK-MEL-5 cells NFToNZhRem:uaX\ldoF1cW:wIHHzd4F6 NFzTW3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? NYf2bHR{OjF4MkG4PFM>
UACC257 cells NFvOS|RRem:uaX\ldoF1cW:wIHHzd4F6 NV3oSotXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkO5N{DPxE1? MXeyNVYzOTh6Mx?=
UACC62 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 NEf6UGFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2M3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|N{mg{txO NXrUOGRUOjF4MkG4PFM>
IGROV1 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN M3f4TlIyPjJzOEiz
OVCAR3 cells M175[3Bzd2yrZnXyZZRqd25iYYPzZZk> NWPueW9kSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMUGg{txO MXOyNVYzOTh6Mx?=
OVCAR4 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MlfSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvOjFizszN NXewPJBVOjF4MkG4PFM>
OVCAR5 cells NFX0cWtRem:uaX\ldoF1cW:wIHHzd4F6 M1jhc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> M4L4UFIyPjJzOEiz
OVCAR8 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NUXXUJBNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO NF\sUGQzOTZ{MUi4Ny=>
NCI/ADR-RES cells M1rEcnBzd2yrZnXyZZRqd25iYYPzZZk> NFP5VXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU9CTFJvUlXTJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE5KM7:TR?= M2r2UFIyPjJzOEiz
SKOV3 cells M2LWe3Bzd2yrZnXyZZRqd25iYYPzZZk> MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUzPCEQvF2= NUf5c2g4OjF4MkG4PFM>
786-0 cells MnLCVJJwdGmoZYLheIlwdiCjc4PhfS=> M{K0W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN MnvONlE3OjF6OEO=
A498 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NVP6Wnp7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> NFnncVMzOTZ{MUi4Ny=>
ACHN cells NVnUR3c{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MoHWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDQ1jOJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEh|ryP NFe1bWIzOTZ{MUi4Ny=>
Caki1 cells MnjsVJJwdGmoZYLheIlwdiCjc4PhfS=> M3zOdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> NFf3VFczOTZ{MUi4Ny=>
SN12C cells Mn\YVJJwdGmoZYLheIlwdiCjc4PhfS=> NYP0bYFKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUlEzSyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy57MjFOwG0> MmnnNlE3OjF6OEO=
TK10 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 Mof4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWS{GwJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ1PCEQvF2= M1zrc|IyPjJzOEiz
UO31 cells NHnhXZVRem:uaX\ldoF1cW:wIHHzd4F6 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWRM{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFUzKM7:TR?= NWDGUGlsOjF4MkG4PFM>
PC3 cells M121[3Bzd2yrZnXyZZRqd25iYYPzZZk> NYLOc5JNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= NWnLOoN4OjF4MkG4PFM>
DU145 cells NGDnXXBRem:uaX\ldoF1cW:wIHHzd4F6 NX\tdZFbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> M2flZVIyPjJzOEiz
MCF7 cells NEPJOnlRem:uaX\ldoF1cW:wIHHzd4F6 MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPU[uPVEh|ryP NIPjPVgzOTZ{MUi4Ny=>
MDA-MB-231 cells M4H4O3Bzd2yrZnXyZZRqd25iYYPzZZk> MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNzLkeg{txO NEDNfXIzOTZ{MUi4Ny=>
Hs 578T cells MmrCVJJwdGmoZYLheIlwdiCjc4PhfS=> NEjwVYdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjzJFU4QFRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEKg{txO NYjCeGlOOjF4MkG4PFM>
BT549 cells Mn6yVJJwdGmoZYLheIlwdiCjc4PhfS=> NIXHeFRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOVQ6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjB2IN88US=> NH3KXlQzOTZ{MUi4Ny=>
T47D cells NFy1blNRem:uaX\ldoF1cW:wIHHzd4F6 M1\qVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlgvQCEQvF2= MXKyNVYzOTh6Mx?=
MDA-MB-468 cells NWLiWW95WHKxbHnm[ZJifGmxbjDhd5NigQ>? NH3FenZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12NkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUWuPFgh|ryP M4D2O|IyPjJzOEiz
NCI-H226 cells NXjwc2doS3m2b4TvfIlkcXS7IHHzd4F6 M3nLdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5EUS2KMkK2JINmdGy|LDDMR|UxRTJyIN88US=> M33EOlIyPjJzOEiz
KM12 cells MmTGR5l1d3SxeHnjbZR6KGG|c3H5 Mkn0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT20yOiClZXzsd{whVEN3ME2yPU46KM7:TR?= NFrPW4MzOTZ{MUi4Ny=>
SF295 cells MWXDfZRwfG:6aXPpeJkh[XO|YYm= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{whVEN3ME22MlkyKM7:TR?= MlO4NlE3OjF6OEO=
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LOXIMVI cells NYnMNnVIS3m2b4TvfIlkcXS7IHHzd4F6 MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDMU3hKVV[LIHPlcIx{NCCOQ{WwQVYvODRizszN NYnGPHpsOjF4MkG4PFM>
MDA-MB-435 cells NWjPd2NRS3m2b4TvfIlkcXS7IHHzd4F6 NGDlVJZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzMEBNSzVyPUK4Mlgh|ryP NXLseoJzOjF4MkG4PFM>
SK-MEL-28 cells NETheJpEgXSxdH;4bYNqfHliYYPzZZk> MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNuIFzDOVA:OzFwOTFOwG0> MUWyNVYzOTh6Mx?=
SK-MEL-5 cells MWLDfZRwfG:6aXPpeJkh[XO|YYm= NWP5Slc1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVUh[2WubIOsJGxEPTB;ND6wNkDPxE1? NHLRSpQzOTZ{MUi4Ny=>
UACC257 cells MojTR5l1d3SxeHnjbZR6KGG|c3H5 NXLnbZhUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? MXeyNVYzOTh6Mx?=
UACC62 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMtKEyFNUC9Ok4{QSEQvF2= MX:yNVYzOTh6Mx?=
IGROV1 cells NIjhSZREgXSxdH;4bYNqfHliYYPzZZk> NYC2T4I6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO NES5S20zOTZ{MUi4Ny=>
OVCAR5 cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= MmC2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gU3ZESVJ3IHPlcIx{NCCOQ{WwQVM5NjlizszN M1X3PVIyPjJzOEiz
SKOV3 cells M1jUW2N6fG:2b4jpZ4l1gSCjc4PhfS=> MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= NWm3VnJFOjF4MkG4PFM>
A498 cells MoDmR5l1d3SxeHnjbZR6KGG|c3H5 M1zY[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1QThiY3XscJMtKEyFNUC9OU45QCEQvF2= NXXNWIZiOjF4MkG4PFM>
Caki1 cells Mk\mR5l1d3SxeHnjbZR6KGG|c3H5 NW\GW41TS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> NFrM[|kzOTZ{MUi4Ny=>
HCT116 cells M3zXfHBzd2yrZnXyZZRqd25iYYPzZZk> M2O1TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= MYqyNVc1OjR7Nh?=
HCT116 cells MUTQdo9tcW[ncnH0bY9vKGG|c3H5 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= MoDnNlE3PTB{MkG=
H1299 cells NGHkVotRem:uaX\ldoF1cW:wIHHzd4F6 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|LDDJR|UxRTBwMTFOwG0> Mk\ZNlE3PTB{MkG=
HCT116 cells M2\DWnBzd2yrZnXyZZRqd25iYYPzZZk> MojqTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> M1Hz[FE1PjF|M{Gy
RPMI8226 cells MVvQdo9tcW[ncnH0bY9vKGG|c3H5 NX\nbWQzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSVG1KQDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61NlMh|ryP M{fMe|IyPjJzOEiz
CHO cells MX3GeY5kfGmxbjDhd5NigQ>? M1rHW2lvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO MWKyNFIxPTN7NB?=
HL-60(TB) cells NWSze4o2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVH2NlVxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUE03OCiWQjmgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNlQ6KM7:TR?= NXmzVGI3OjF4MkG4PFM>
RXF393 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 MnfnRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN MkXjNlE3OjF6OEO=
RXF393 cells MYfDfZRwfG:6aXPpeJkh[XO|YYm= MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMtKEyFNUC9NVUvOyEQvF2= M4e4S|IyPjJzOEiz

... 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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID