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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  • 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 MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{HafGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJOTJ7OTDoeY1idiCudX7nJINiemOrbn;tZUBk\WyuIHfyc5d1cCxiSVO1NF0xNjF3IN88US=> NFf2VpcyPDV{MUSyNi=>
HCT116 M3nFRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWTJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTGNVOTF4IHj1cYFvKGOxbH;uJINmdGxiZ4Lve5RpNCCLQ{WwQVAvODFizszN MoDzNVQ2OjF2MkK=
HCT116 MkfuR5l1d3SxeHnjbZR6KGG|c3H5 MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEWg{txO MmjvNVc6PDF4MkW=
human mammary epithelial cells MmXxR5l1d3SxeHnjbZR6KGG|c3H5 NVHydZFNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hdWGvbXHyfUBmeGm2aHXsbYFtKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF0yKM7:TR?= NGP3cZAyPzl2MU[yOS=>
HEK293 cells MVzGeY5kfGmxbjDhd5NigQ>? NHzZZ4hKdmirYnn0bY9vKG:oIFjERWMyKGmwIFjFT|I6OyClZXzsd{whUUN3ME2wMlAxOjZizszN MWKxPFMxQDV4Mx?=
HeLa cells NH;x[m5HfW6ldHnvckBie3OjeR?= NXTwPHpiOC5|IN88US=> MkPONVYhcA>? MkWyTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= M163OlE4QTV4OUi4
HCT116 cells NV76bXVEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF3OSGxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO NXPNSlhWOjB{MEWzPVQ>
H1299 cells NXvke5l2WHKxbHnm[ZJifGmxbjDhd5NigQ>? MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|IHL5JG1VWyCjc4PhfUwhUUN3ME2wMlE3OSEQvF2= NXXWW3JKOjB{MEWzPVQ>
H460 cells MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYW0PEBp MlzzS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP MUmyNVA4OzF4MB?=
HCT116 cells NWPoR4o4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYL4eIhOPDhiaB?= NInCRnZIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> NXK4T21FOjFyN{OxOlA>
CCRF-CEM cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> NGj6VmEzOTZ{MUi4Ny=>
K562 cells MknwVJJwdGmoZYLheIlwdiCjc4PhfS=> NFrpNIhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTVizszN MWKyNVYzOTh6Mx?=
MOLT4 cells NW\rb5V1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MoDtRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN MmLJNlE3OjF6OEO=
SR cells NULDd4hLWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3zj[2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2KgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuPVkh|ryP MYqyNVYzOTh6Mx?=
A549 cells Mlf3VJJwdGmoZYLheIlwdiCjc4PhfS=> NHjQcWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NUn6SFg1OjF4MkG4PFM>
EKVX cells NYjKepc{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NV;5[m9RSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDFT3ZZKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjd3IN88US=> MYOyNVYzOTh6Mx?=
HOP62 cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 NF;6SmNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjVyMjFOwG0> MWWyNVYzOTh6Mx?=
HOP92 cells NHfvUJNRem:uaX\ldoF1cW:wIHHzd4F6 MlH2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN NXPKcHo4OjF4MkG4PFM>
NCI-H226 cells NXHFNZJUWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nscGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO NGTodWUzOTZ{MUi4Ny=>
NCI-H23 cells MkTLVJJwdGmoZYLheIlwdiCjc4PhfS=> M1izZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> MVmyNVYzOTh6Mx?=
NCI-H322M cells MofpVJJwdGmoZYLheIlwdiCjc4PhfS=> MlvORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO NH73S5IzOTZ{MUi4Ny=>
NCI-H460 cells M4S0dXBzd2yrZnXyZZRqd25iYYPzZZk> M1P4VWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg1PjBiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNzFOwG0> MmXSNlE3OjF6OEO=
COLO205 cells NWrJNJlrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NID1NpZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPPUG8zODViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO M2TLW|IyPjJzOEiz
HCT116 cells NHT6b|FRem:uaX\ldoF1cW:wIHHzd4F6 MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN NWHYT|A2OjF4MkG4PFM>
HCT15 cells M{HKRXBzd2yrZnXyZZRqd25iYYPzZZk> NF62c|lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> NF3zSlIzOTZ{MUi4Ny=>
HT-29 cells MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NG\O[npCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV4NjFOwG0> MXmyNVYzOTh6Mx?=
KM12 cells M{jnW3Bzd2yrZnXyZZRqd25iYYPzZZk> NYDuW4pLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> M1HIO|IyPjJzOEiz
SW620 cells NGnhc5VRem:uaX\ldoF1cW:wIHHzd4F6 NXnxcHJUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO NGSyXYwzOTZ{MUi4Ny=>
SF268 cells M{LUSHBzd2yrZnXyZZRqd25iYYPzZZk> MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= M3;XXlIyPjJzOEiz
SF295 cells M2O2bnBzd2yrZnXyZZRqd25iYYPzZZk> NEnRPIFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlk2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd2MzFOwG0> Ml;rNlE3OjF6OEO=
SF539 cells NWPDXI5TWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOINUO5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk3PSEQvF2= MU[yNVYzOTh6Mx?=
SNB19 cells MmS0VJJwdGmoZYLheIlwdiCjc4PhfS=> M3zGOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CNVkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN M1\6clIyPjJzOEiz
SNB75 cells NFLEWlhRem:uaX\ldoF1cW:wIHHzd4F6 NF3WcWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPORlc2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjNzODFOwG0> NWnBRpI{OjF4MkG4PFM>
U251 cells M1nHV3Bzd2yrZnXyZZRqd25iYYPzZZk> MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV{NUGgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuO|c{KM7:TR?= NVnKXI5OOjF4MkG4PFM>
LOXIMVI cells NHj2TplRem:uaX\ldoF1cW:wIHHzd4F6 NUCzTWVWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMU3hKVV[LIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? MoezNlE3OjF6OEO=
MALME-3M cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NEnGTohCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3BUG1GNTOPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkS2NUDPxE1? NULzbFB5OjF4MkG4PFM>
M14 cells M3jkSnBzd2yrZnXyZZRqd25iYYPzZZk> Mn\6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMUSgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPFQ6KM7:TR?= MWmyNVYzOTh6Mx?=
MDA-MB-435 cells M1nOPHBzd2yrZnXyZZRqd25iYYPzZZk> MmLRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? NEnndW8zOTZ{MUi4Ny=>
SK-MEL-28 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 MoLRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? NXzaN4JuOjF4MkG4PFM>
SK-MEL-5 cells NGSwSWJRem:uaX\ldoF1cW:wIHHzd4F6 NUnJWWtESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yO|Eh|ryP MoHwNlE3OjF6OEO=
UACC257 cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 MmmxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDNlU4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN7MzFOwG0> NXHsbFFQOjF4MkG4PFM>
UACC62 cells MkCzVJJwdGmoZYLheIlwdiCjc4PhfS=> MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWDQ1O2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PzlizszN MWeyNVYzOTh6Mx?=
IGROV1 cells NUHQUINOWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVTZbJVSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? NWXqSGlPOjF4MkG4PFM>
OVCAR3 cells MmrhVJJwdGmoZYLheIlwdiCjc4PhfS=> MlXPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN M4S2XFIyPjJzOEiz
OVCAR4 cells Mmn0VJJwdGmoZYLheIlwdiCjc4PhfS=> M{PWWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjJzIN88US=> M1u1VFIyPjJzOEiz
OVCAR5 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 NX7pcmQ4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMk[g{txO M335TVIyPjJzOEiz
OVCAR8 cells M17m[nBzd2yrZnXyZZRqd25iYYPzZZk> MonORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDVizszN M4HqfFIyPjJzOEiz
NCI/ADR-RES cells Mn7mVJJwdGmoZYLheIlwdiCjc4PhfS=> NFrz[lBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU9CTFJvUlXTJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE5KM7:TR?= NF33SHgzOTZ{MUi4Ny=>
SKOV3 cells MofKVJJwdGmoZYLheIlwdiCjc4PhfS=> NYn2eW9OSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkSg{txO MY[yNVYzOTh6Mx?=
786-0 cells MlP6VJJwdGmoZYLheIlwdiCjc4PhfS=> M3zjOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN MV2yNVYzOTh6Mx?=
A498 cells MlTmVJJwdGmoZYLheIlwdiCjc4PhfS=> NYm0XJMzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> MXuyNVYzOTh6Mx?=
ACHN cells NWX0U2w{WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2nJO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= M1jVPVIyPjJzOEiz
Caki1 cells M2H1[nBzd2yrZnXyZZRqd25iYYPzZZk> NHnPdYNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhb4kyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjZzOTFOwG0> M2L5TFIyPjJzOEiz
SN12C cells Mn72VJJwdGmoZYLheIlwdiCjc4PhfS=> MnLCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTkGyR{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{46OiEQvF2= M4\ndFIyPjJzOEiz
TK10 cells NFXsdGRRem:uaX\ldoF1cW:wIHHzd4F6 M3fYRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVFuxNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PDRizszN MmDXNlE3OjF6OEO=
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PC3 cells NYq0OFdEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHi2NXRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlAh|ryP Mn62NlE3OjF6OEO=
DU145 cells MkfvVJJwdGmoZYLheIlwdiCjc4PhfS=> NF[xPWJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQS57IN88US=> MWWyNVYzOTh6Mx?=
MCF7 cells NHP6W5BRem:uaX\ldoF1cW:wIHHzd4F6 NXrw[GVQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjlzIN88US=> M2HZdVIyPjJzOEiz
MDA-MB-231 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MnXkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1|MT63JO69VQ>? NIrjeoMzOTZ{MUi4Ny=>
Hs 578T cells MoXVVJJwdGmoZYLheIlwdiCjc4PhfS=> M3jNWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIOgOVc5XCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:PS56MjFOwG0> NGfq[VkzOTZ{MUi4Ny=>
BT549 cells MkTmVJJwdGmoZYLheIlwdiCjc4PhfS=> MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlA1KM7:TR?= NWfyNWZsOjF4MkG4PFM>
T47D cells MkfmVJJwdGmoZYLheIlwdiCjc4PhfS=> M2HPN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlgvQCEQvF2= NITDWpczOTZ{MUi4Ny=>
MDA-MB-468 cells NVzvfHJiWHKxbHnm[ZJifGmxbjDhd5NigQ>? MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTVwOEig{txO NXzGdIJFOjF4MkG4PFM>
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SF295 cells M2D2UGN6fG:2b4jpZ4l1gSCjc4PhfS=> NX;Wc|VZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0Z{OUWgZ4VtdHNuIFzDOVA:Pi57MTFOwG0> M3zZclIyPjJzOEiz
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U251 cells NUPK[3B6S3m2b4TvfIlkcXS7IHHzd4F6 MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzMEBNSzVyPUWuPFIh|ryP NWLNXJRLOjF4MkG4PFM>
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MDA-MB-435 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= NF7D[IpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzMEBNSzVyPUK4Mlgh|ryP M4jCW|IyPjJzOEiz
SK-MEL-28 cells MoHrR5l1d3SxeHnjbZR6KGG|c3H5 MnTQR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy|LDDMR|UxRTNzLkmg{txO Mk\WNlE3OjF6OEO=
SK-MEL-5 cells NGLtXY5EgXSxdH;4bYNqfHliYYPzZZk> MUnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyxiTFO1NF01NjB{IN88US=> NUj1SlBkOjF4MkG4PFM>
UACC257 cells Mnv1R5l1d3SxeHnjbZR6KGG|c3H5 NFXI[GFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFMkW3JINmdGy|LDDMR|UxRTR2Lkig{txO NYHCeHVHOjF4MkG4PFM>
UACC62 cells MlHqR5l1d3SxeHnjbZR6KGG|c3H5 MV7DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMtKEyFNUC9Ok4{QSEQvF2= MVuyNVYzOTh6Mx?=
IGROV1 cells M{[wRmN6fG:2b4jpZ4l1gSCjc4PhfS=> MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= M1H2VVIyPjJzOEiz
OVCAR5 cells M2THSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMtKEyFNUC9N|gvQSEQvF2= M1LCT|IyPjJzOEiz
SKOV3 cells M{f1WGN6fG:2b4jpZ4l1gSCjc4PhfS=> Mn:2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2tQXjNiY3XscJMtKEyFNUC9NlgvPSEQvF2= M3LNRVIyPjJzOEiz
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Caki1 cells M4C5T2N6fG:2b4jpZ4l1gSCjc4PhfS=> MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{whVEN3ME21Mlc6KM7:TR?= NEHYfoszOTZ{MUi4Ny=>
HCT116 cells NFXYcVVRem:uaX\ldoF1cW:wIHHzd4F6 MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczygTWM2OD1yLkCxPUDPxE1? NHTNS2wzOTd2MkS5Oi=>
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HCT116 cells NY\BZoZwWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml35TY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> NGSxTnQyPDZzM{OxNi=>
RPMI8226 cells M2fvNnBzd2yrZnXyZZRqd25iYYPzZZk> MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{MzFOwG0> MknLNlE3OjF6OEO=
CHO cells MUHGeY5kfGmxbjDhd5NigQ>? NFrBeGtKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IHH1eI9u[XSnZDDwZZRkcCClbHHtdEBmdGWldILvdIh6e2mxbH;nfUBie3OjeTygTWM2OD1zMj6yJO69VQ>? NH\NWXgzODJyNUO5OC=>
HL-60(TB) cells NYXDeHZ4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MoLQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTD22NEhVSiliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkS5JO69VQ>? MXWyNVYzOTh6Mx?=
RXF393 cells M3Hzb3Bzd2yrZnXyZZRqd25iYYPzZZk> NVzJUHFXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMEGg{txO Ml;SNlE3OjF6OEO=
RXF393 cells MnSwR5l1d3SxeHnjbZR6KGG|c3H5 MnrZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN NWXjTXhUOjF4MkG4PFM>

... 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:
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
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