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 NVTwZVg4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NInTcplKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> MXixOFUzOTR{Mh?=
HCT116 MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHp[YZnUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiFVEGxOkBpfW2jbjDjc4xwdiClZXzsJIdzd3e2aDygTWM2OD1yLkCxJO69VQ>? NEDLblQyPDV{MUSyNi=>
HCT116 MWrDfZRwfG:6aXPpeJkh[XO|YYm= Mn;3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC1JO69VQ>? MXuxO|k1OTZ{NR?=
human mammary epithelial cells M1Hk[GN6fG:2b4jpZ4l1gSCjc4PhfS=> M1zJW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? Mki3NVc6PDF4MkW=
HEK293 cells MWnGeY5kfGmxbjDhd5NigQ>? MYXJcohq[mm2aX;uJI9nKEiGQVOxJIlvKEiHS{K5N{Bk\WyuczygTWM2OD1yLkCwNlYh|ryP M{T0T|E5OzB6NU[z
HeLa cells MULGeY5kfGmxbjDhd5NigQ>? M3H3WlAvOyEQvF2= MWixOkBp NI\qO3dKdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MWOxO|k2Pjl6OB?=
HCT116 cells M3ixbXBzd2yrZnXyZZRqd25iYYPzZZk> NInBNYlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO MUKyNFIxPTN7NB?=
H1299 cells M3\lRnBzd2yrZnXyZZRqd25iYYPzZZk> M4G5dWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> NVqybW9ZOjB{MEWzPVQ>
H460 cells M3jJUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGrjWXE1QCCq NEjEfJBIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJPDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xPyEQvF2= M4nMNFIyODd|MU[w
HCT116 cells MoO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGGycJk1QCCq MWPHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlAyQCEQvF2= M4LlXlIyODd|MU[w
CCRF-CEM cells NUXrcmJPWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2nofmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1PSSk1ETU1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkWxJO69VQ>? MWSyNVYzOTh6Mx?=
K562 cells NXzLVZA5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3nrbmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PSEQvF2= NHrRRZczOTZ{MUi4Ny=>
MOLT4 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NXXBOYdJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO NI\xOVIzOTZ{MUi4Ny=>
SR cells Mn[0VJJwdGmoZYLheIlwdiCjc4PhfS=> NH\GNIpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= MoHXNlE3OjF6OEO=
A549 cells M3LNcHBzd2yrZnXyZZRqd25iYYPzZZk> M1Tq[GFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= M4fUdFIyPjJzOEiz
EKVX cells M3TOeHBzd2yrZnXyZZRqd25iYYPzZZk> NYr1OHhbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDFT3ZZKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjd3IN88US=> MlXmNlE3OjF6OEO=
HOP62 cells NFnybFRRem:uaX\ldoF1cW:wIHHzd4F6 NFzVNFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjVyMjFOwG0> MoL5NlE3OjF6OEO=
HOP92 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 NHnIfJFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFkzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF7OTFOwG0> M{\DbVIyPjJzOEiz
NCI-H226 cells M{[3RXBzd2yrZnXyZZRqd25iYYPzZZk> MkLDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> M2DzR|IyPjJzOEiz
NCI-H23 cells NHzrdnlRem:uaX\ldoF1cW:wIHHzd4F6 NUHnUmxWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO NF\qRZQzOTZ{MUi4Ny=>
NCI-H322M cells MlTBVJJwdGmoZYLheIlwdiCjc4PhfS=> NF\QcVNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzJ{TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj6yOkDPxE1? NGjUR2ozOTZ{MUi4Ny=>
NCI-H460 cells NUXHTmZvWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnjiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> M1[1dVIyPjJzOEiz
COLO205 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 M4XCS2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> MV2yNVYzOTh6Mx?=
HCT116 cells MkXtVJJwdGmoZYLheIlwdiCjc4PhfS=> NFjhUHRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|NEeg{txO NI\yNpAzOTZ{MUi4Ny=>
HCT15 cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= MUmyNVYzOTh6Mx?=
HT-29 cells M1HZSHBzd2yrZnXyZZRqd25iYYPzZZk> MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU3PiEQvF2= MljJNlE3OjF6OEO=
KM12 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 M3H2bmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xPCEQvF2= MofhNlE3OjF6OEO=
SW620 cells NEjabYdRem:uaX\ldoF1cW:wIHHzd4F6 M1;V[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDd6IN88US=> MlnsNlE3OjF6OEO=
SF268 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= MYOyNVYzOTh6Mx?=
SF295 cells MnPGVJJwdGmoZYLheIlwdiCjc4PhfS=> NF\CeWpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlk2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd2MzFOwG0> NHnaUXEzOTZ{MUi4Ny=>
SF539 cells NGjjfVBRem:uaX\ldoF1cW:wIHHzd4F6 MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOINUO5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlk3PSEQvF2= NXvFPYhQOjF4MkG4PFM>
SNB19 cells NXS2e|dKWHKxbHnm[ZJifGmxbjDhd5NigQ>? MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= M4fHNFIyPjJzOEiz
SNB75 cells MlrIVJJwdGmoZYLheIlwdiCjc4PhfS=> MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= MlruNlE3OjF6OEO=
U251 cells M3n3O3Bzd2yrZnXyZZRqd25iYYPzZZk> MoH1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= Mk\MNlE3OjF6OEO=
LOXIMVI cells NVWwOJY6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN NWe0TYNUOjF4MkG4PFM>
MALME-3M cells NH3WV|BRem:uaX\ldoF1cW:wIHHzd4F6 NHfDd|dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3BUG1GNTOPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkS2NUDPxE1? MXuyNVYzOTh6Mx?=
M14 cells NH\lem9Rem:uaX\ldoF1cW:wIHHzd4F6 MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE1zNDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD64OFkh|ryP NULPUIx3OjF4MkG4PFM>
MDA-MB-435 cells M1XNZnBzd2yrZnXyZZRqd25iYYPzZZk> M3nHcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP M1rB[lIyPjJzOEiz
SK-MEL-28 cells M1zHZ3Bzd2yrZnXyZZRqd25iYYPzZZk> MnvQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? NE\6cY4zOTZ{MUi4Ny=>
SK-MEL-5 cells NF;JUVJRem:uaX\ldoF1cW:wIHHzd4F6 MkTWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{N{Gg{txO MlXVNlE3OjF6OEO=
UACC257 cells NVraNIJNWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3\0ZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|I2PyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|OUOg{txO M3n6XlIyPjJzOEiz
UACC62 cells NIXMeHdRem:uaX\ldoF1cW:wIHHzd4F6 M4nyVWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|YzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN5OTFOwG0> MkmyNlE3OjF6OEO=
IGROV1 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 NYLoeGpMSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? MX:yNVYzOTh6Mx?=
OVCAR3 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 M2LZRmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> M2juclIyPjJzOEiz
OVCAR4 cells M4LhdnBzd2yrZnXyZZRqd25iYYPzZZk> NH\CfWdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> MUWyNVYzOTh6Mx?=
OVCAR5 cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 MYTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4zPiEQvF2= M2X1S|IyPjJzOEiz
OVCAR8 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSPEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PSEQvF2= NIHNdHMzOTZ{MUi4Ny=>
NCI/ADR-RES cells M4jJ[XBzd2yrZnXyZZRqd25iYYPzZZk> MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? MkPrNlE3OjF6OEO=
SKOV3 cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUzPCEQvF2= NXzvcWFIOjF4MkG4PFM>
786-0 cells MoPkVJJwdGmoZYLheIlwdiCjc4PhfS=> M3;XfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN NHTq[IozOTZ{MUi4Ny=>
A498 cells MnLwVJJwdGmoZYLheIlwdiCjc4PhfS=> NWrTVWdkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> M4q5SVIyPjJzOEiz
ACHN cells NH;6UmZRem:uaX\ldoF1cW:wIHHzd4F6 M2jWTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= MoTrNlE3OjF6OEO=
Caki1 cells NYrDUXlKWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4G3O2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> NEHtT2ozOTZ{MUi4Ny=>
SN12C cells M4ni[nBzd2yrZnXyZZRqd25iYYPzZZk> M4DNNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU16xNmMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvQTJizszN NF7IO4szOTZ{MUi4Ny=>
TK10 cells MoCwVJJwdGmoZYLheIlwdiCjc4PhfS=> NWLIbHN[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> M1HSflIyPjJzOEiz
UO31 cells MnjUVJJwdGmoZYLheIlwdiCjc4PhfS=> MkW3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXT{OxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ2OiEQvF2= NHnUbVEzOTZ{MUi4Ny=>
PC3 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MkCg{txO MVqyNVYzOTh6Mx?=
DU145 cells NYnNbIpvWHKxbHnm[ZJifGmxbjDhd5NigQ>? NX7vPY1DSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> MYGyNVYzOTh6Mx?=
MCF7 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 MmPrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlkyKM7:TR?= NWfBbGNxOjF4MkG4PFM>
MDA-MB-231 cells NVnRT3ZEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUnkSW5CSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zNU44KM7:TR?= NG\TeI8zOTZ{MUi4Ny=>
Hs 578T cells MoS0VJJwdGmoZYLheIlwdiCjc4PhfS=> M2G5[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIOgOVc5XCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:PS56MjFOwG0> MV2yNVYzOTh6Mx?=
BT549 cells NXz3XIVmWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWPsNWdlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi5yNDFOwG0> NX7CSHpvOjF4MkG4PFM>
T47D cells M3X2[3Bzd2yrZnXyZZRqd25iYYPzZZk> M{Lsc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVES3SEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlgvQCEQvF2= NFrV[pkzOTZ{MUi4Ny=>
MDA-MB-468 cells NU\1SlNlWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4TmeGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? MWqyNVYzOTh6Mx?=
NCI-H226 cells NVHMVHB4S3m2b4TvfIlkcXS7IHHzd4F6 MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyxiTFO1NF0zOCEQvF2= NVvjVIo6OjF4MkG4PFM>
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SF295 cells M2e5fmN6fG:2b4jpZ4l1gSCjc4PhfS=> M4rVS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjl3IHPlcIx{NCCOQ{WwQVYvQTFizszN M4rtOlIyPjJzOEiz
SNB19 cells M4[1TWN6fG:2b4jpZ4l1gSCjc4PhfS=> NFLnfXlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUVkJzOTDj[YxteyxiTFO1NF0{OS55IN88US=> MWmyNVYzOTh6Mx?=
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LOXIMVI cells MYnDfZRwfG:6aXPpeJkh[XO|YYm= NUi4NGpvS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE:[SV3WTUBk\WyuczygUGM2OD14LkC0JO69VQ>? NHHlNVUzOTZ{MUi4Ny=>
MDA-MB-435 cells NF;TTmNEgXSxdH;4bYNqfHliYYPzZZk> M165OmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? MojFNlE3OjF6OEO=
SK-MEL-28 cells MYHDfZRwfG:6aXPpeJkh[XO|YYm= NFX1e4NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytNlgh[2WubIOsJGxEPTB;M{GuPUDPxE1? NFrMNogzOTZ{MUi4Ny=>
SK-MEL-5 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= NFnpcZZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? MnjLNlE3OjF6OEO=
UACC257 cells M3HJXmN6fG:2b4jpZ4l1gSCjc4PhfS=> MlvwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWWFESzJ3NzDj[YxteyxiTFO1NF01PC56IN88US=> M1K3fVIyPjJzOEiz
UACC62 cells M1nyOWN6fG:2b4jpZ4l1gSCjc4PhfS=> MmrCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWWFESzZ{IHPlcIx{NCCOQ{WwQVYvOzlizszN NXHzRWtbOjF4MkG4PFM>
IGROV1 cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= MXOyNVYzOTh6Mx?=
OVCAR5 cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= MX\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMtKEyFNUC9N|gvQSEQvF2= MYeyNVYzOTh6Mx?=
SKOV3 cells MmDFR5l1d3SxeHnjbZR6KGG|c3H5 MXPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= MViyNVYzOTh6Mx?=
A498 cells NWHHU4VES3m2b4TvfIlkcXS7IHHzd4F6 MYjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzMEBNSzVyPUWuPFgh|ryP NXfKTlZPOjF4MkG4PFM>
Caki1 cells MXvDfZRwfG:6aXPpeJkh[XO|YYm= MkL1R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR4FscTFiY3XscJMtKEyFNUC9OU44QSEQvF2= MYOyNVYzOTh6Mx?=
HCT116 cells NFfSWHZRem:uaX\ldoF1cW:wIHHzd4F6 NV;nNZA4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEmFNUC9NE4xOTlizszN MYmyNVc1OjR7Nh?=
HCT116 cells MoHnVJJwdGmoZYLheIlwdiCjc4PhfS=> NFvZN25CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NF0xNjBzOTFOwG0> NEDydHgzOTZ3MEKyNS=>
H1299 cells NYi0VXpvWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|LDDJR|UxRTBwMTFOwG0> MlzqNlE3PTB{MkG=
HCT116 cells NFnvNJNRem:uaX\ldoF1cW:wIHHzd4F6 NXjOUWtYUW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgTGNVOTF4IHPlcIx{KHC{b3zp[oVz[XSrb36sJGlEPTB;MD6wNUDPxE1? MX[xOFYyOzNzMh?=
RPMI8226 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 MlO0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkOg{txO MViyNVYzOTh6Mx?=
CHO cells NXe4SnJYTnWwY4Tpc44h[XO|YYm= M{\U[mlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO Ml;tNlAzODV|OUS=
HL-60(TB) cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 MlfzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTD22NEhVSiliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkS5JO69VQ>? NHvmRlIzOTZ{MUi4Ny=>
RXF393 cells NUT4fndKWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFK[RkO5N{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4xOSEQvF2= Mm\ONlE3OjF6OEO=
RXF393 cells NYnzU3RyS3m2b4TvfIlkcXS7IHHzd4F6 MoLLR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN MXSyNVYzOTh6Mx?=

... 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

Bio Calculators

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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