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 NHPySGhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTFEzQTliaIXtZY4hdHWwZzDjZZJkcW6xbXGgZ4VtdCCpcn;3eIgtKEmFNUC9NE4yPSEQvF2= NYfKdI1COTR3MkG0NlI>
HCT116 NFrwUFhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2LSNGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> M2\OS|E1PTJzNEKy
HCT116 M{noWmN6fG:2b4jpZ4l1gSCjc4PhfS=> MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTBwMEWg{txO Ml\INVc6PDF4MkW=
human mammary epithelial cells M3z5V2N6fG:2b4jpZ4l1gSCjc4PhfS=> M3PoTmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? M{fEblE4QTRzNkK1
HEK293 cells M4\sSmZ2dmO2aX;uJIF{e2G7 NFe2[2hKdmirYnn0bY9vKG:oIFjERWMyKGmwIFjFT|I6OyClZXzsd{whUUN3ME2wMlAxOjZizszN MoW5NVg{ODh3NkO=
HeLa cells NWPjbYpsTnWwY4Tpc44h[XO|YYm= M4TVNlAvOyEQvF2= MVGxOkBp NHKzUG9KdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NEG5XVQyPzl3Nkm4PC=>
HCT116 cells NYfkTG9jWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml6yRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> MYSyNFIxPTN7NB?=
H1299 cells MmLEVJJwdGmoZYLheIlwdiCjc4PhfS=> MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|IHL5JG1VWyCjc4PhfUwhUUN3ME2wMlE3OSEQvF2= M13nRVIxOjB3M{m0
H460 cells NYDrbYo6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{G1U|Q5KGh? NIT4[llIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJPDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xPyEQvF2= NU[0ZnFFOjFyN{OxOlA>
HCT116 cells M1P2XGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWK0PEBp Mlu3S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN Mn7jNlExPzNzNkC=
CCRF-CEM cells NGr4N2pRem:uaX\ldoF1cW:wIHHzd4F6 NXmySFdNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOVEh|ryP M17T[FIyPjJzOEiz
K562 cells Mn3DVJJwdGmoZYLheIlwdiCjc4PhfS=> MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEt3NkKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVUh|ryP MUmyNVYzOTh6Mx?=
MOLT4 cells MkLVVJJwdGmoZYLheIlwdiCjc4PhfS=> NVXL[25GSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO NVrUO|VjOjF4MkG4PFM>
SR cells NUjqVXozWHKxbHnm[ZJifGmxbjDhd5NigQ>? NH7PR5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= MlLDNlE3OjF6OEO=
A549 cells NETjb29Rem:uaX\ldoF1cW:wIHHzd4F6 MkLaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA6KM7:TR?= MoTVNlE3OjF6OEO=
EKVX cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M{i5NmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= NV;Vd4hvOjF4MkG4PFM>
HOP62 cells MkHqVJJwdGmoZYLheIlwdiCjc4PhfS=> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUE[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUxOiEQvF2= MWmyNVYzOTh6Mx?=
HOP92 cells NInu[I9Rem:uaX\ldoF1cW:wIHHzd4F6 M3vnVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QPVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTl7IN88US=> MWWyNVYzOTh6Mx?=
NCI-H226 cells M3frVnBzd2yrZnXyZZRqd25iYYPzZZk> M3z6ZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO Mnv0NlE3OjF6OEO=
NCI-H23 cells NF;Ub2dRem:uaX\ldoF1cW:wIHHzd4F6 M4S2d2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> MmHsNlE3OjF6OEO=
NCI-H322M cells NHq0Z2tRem:uaX\ldoF1cW:wIHHzd4F6 Mk\1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO NHzQeXczOTZ{MUi4Ny=>
NCI-H460 cells NUnTboN5WHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml3WRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> MoLKNlE3OjF6OEO=
COLO205 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NVjqTYtuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? NXjWOnlmOjF4MkG4PFM>
HCT116 cells NUXj[3A2WHKxbHnm[ZJifGmxbjDhd5NigQ>? MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN MkX5NlE3OjF6OEO=
HCT15 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 M4nvbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvODdizszN MXGyNVYzOTh6Mx?=
HT-29 cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU3PiEQvF2= M{ey[lIyPjJzOEiz
KM12 cells NX7CR4VPWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnXFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= MlvaNlE3OjF6OEO=
SW620 cells M3[zfXBzd2yrZnXyZZRqd25iYYPzZZk> NV\FS4ZqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO NWXjXmw{OjF4MkG4PFM>
SF268 cells NIDMeJFRem:uaX\ldoF1cW:wIHHzd4F6 NXTWN3ZxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> MWKyNVYzOTh6Mx?=
SF295 cells NETzcVBRem:uaX\ldoF1cW:wIHHzd4F6 MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= NITwcoEzOTZ{MUi4Ny=>
SF539 cells NW\jbm9QWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIrYbmNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGOVM6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjl4NTFOwG0> NIXBc|EzOTZ{MUi4Ny=>
SNB19 cells M3zyTnBzd2yrZnXyZZRqd25iYYPzZZk> M1rrNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CNVkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN MWSyNVYzOTh6Mx?=
SNB75 cells NELUdlNRem:uaX\ldoF1cW:wIHHzd4F6 NWDhSXdTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmI4PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUig{txO M1rSPFIyPjJzOEiz
U251 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NHj1[WRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> M4\hdVIyPjJzOEiz
LOXIMVI cells M1;iRnBzd2yrZnXyZZRqd25iYYPzZZk> MknGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOT2jJUXZKKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> MXeyNVYzOTh6Mx?=
MALME-3M cells M3HWe3Bzd2yrZnXyZZRqd25iYYPzZZk> NGrvRXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3BUG1GNTOPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkS2NUDPxE1? NHvyNnkzOTZ{MUi4Ny=>
M14 cells NUjrdYJ6WHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml\rRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMUSgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPFQ6KM7:TR?= MmiwNlE3OjF6OEO=
MDA-MB-435 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 NEnEeGVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi12M{WgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOVM4KM7:TR?= MWSyNVYzOTh6Mx?=
SK-MEL-28 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MnTZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? MlXvNlE3OjF6OEO=
SK-MEL-5 cells NIT5UXRRem:uaX\ldoF1cW:wIHHzd4F6 M12zc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkexJO69VQ>? NF[1Tm0zOTZ{MUi4Ny=>
UACC257 cells MnTTVJJwdGmoZYLheIlwdiCjc4PhfS=> MlnkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDNlU4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN7MzFOwG0> NV75do5NOjF4MkG4PFM>
UACC62 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 NGLCS2dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2M3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|N{mg{txO MVKyNVYzOTh6Mx?=
IGROV1 cells NFXJc4hRem:uaX\ldoF1cW:wIHHzd4F6 M2HaPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSVfSU3YyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF6NzFOwG0> NYHN[mZ4OjF4MkG4PFM>
OVCAR3 cells NHrsc|lRem:uaX\ldoF1cW:wIHHzd4F6 NIPDSHpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> MYmyNVYzOTh6Mx?=
OVCAR4 cells MmP4VJJwdGmoZYLheIlwdiCjc4PhfS=> MnLoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvOjFizszN M3v6clIyPjJzOEiz
OVCAR5 cells MnP3VJJwdGmoZYLheIlwdiCjc4PhfS=> NW\KVnRUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMk[g{txO NWH4TpA2OjF4MkG4PFM>
OVCAR8 cells NG\zdphRem:uaX\ldoF1cW:wIHHzd4F6 MmDaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDVizszN NV7uemtmOjF4MkG4PFM>
NCI/ADR-RES cells M1fkUHBzd2yrZnXyZZRqd25iYYPzZZk> MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? M4KxU|IyPjJzOEiz
SKOV3 cells NH3HOGxRem:uaX\ldoF1cW:wIHHzd4F6 M{DWfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> M1mzflIyPjJzOEiz
786-0 cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 Mo\JRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiB5OE[tNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4{QCEQvF2= MVSyNVYzOTh6Mx?=
A498 cells MnzKVJJwdGmoZYLheIlwdiCjc4PhfS=> NGm1T4FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN MVWyNVYzOTh6Mx?=
ACHN cells MluzVJJwdGmoZYLheIlwdiCjc4PhfS=> NWjJ[GJwSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFizszN NEOx[nczOTZ{MUi4Ny=>
Caki1 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 M33UeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> MXOyNVYzOTh6Mx?=
SN12C cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MnjBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTkGyR{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{46OiEQvF2= NWfkPI0{OjF4MkG4PFM>
TK10 cells M{DNSXBzd2yrZnXyZZRqd25iYYPzZZk> MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= MUCyNVYzOTh6Mx?=
UO31 cells M4i5SXBzd2yrZnXyZZRqd25iYYPzZZk> NX\4elVLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> NGS4cWUzOTZ{MUi4Ny=>
PC3 cells MkjRVJJwdGmoZYLheIlwdiCjc4PhfS=> NEizO5JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlAh|ryP NFfBeWEzOTZ{MUi4Ny=>
DU145 cells NV\HdodMWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkeyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlkvQSEQvF2= MYmyNVYzOTh6Mx?=
MCF7 cells M2T0dHBzd2yrZnXyZZRqd25iYYPzZZk> NWL2c5FLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjlzIN88US=> NF7BcWszOTZ{MUi4Ny=>
MDA-MB-231 cells M1XlbnBzd2yrZnXyZZRqd25iYYPzZZk> M2TV[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{GuO{DPxE1? NX2xSJc3OjF4MkG4PFM>
Hs 578T cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 NVPpNmNPSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDId{A2PziWIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13LkiyJO69VQ>? M4\hVlIyPjJzOEiz
BT549 cells MlrWVJJwdGmoZYLheIlwdiCjc4PhfS=> NUfpOG5nSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi5yNDFOwG0> MV:yNVYzOTh6Mx?=
T47D cells NEHMcHhRem:uaX\ldoF1cW:wIHHzd4F6 NVzEN4ozSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQC56IN88US=> MVWyNVYzOTh6Mx?=
MDA-MB-468 cells M3T3WnBzd2yrZnXyZZRqd25iYYPzZZk> M3T0dmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? M3f2blIyPjJzOEiz
NCI-H226 cells M3jpWGN6fG:2b4jpZ4l1gSCjc4PhfS=> MljCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNuIFzDOVA:OjBizszN NYPLN2V7OjF4MkG4PFM>
KM12 cells M17XXGN6fG:2b4jpZ4l1gSCjc4PhfS=> MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzMEBNSzVyPUK5Mlkh|ryP M2TzNFIyPjJzOEiz
SF295 cells M3fnfWN6fG:2b4jpZ4l1gSCjc4PhfS=> NF\3VZREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUTjJ7NTDj[YxteyxiTFO1NF03NjlzIN88US=> MlzQNlE3OjF6OEO=
SNB19 cells M3roZWN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml7aR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25DOTliY3XscJMtKEyFNUC9N|EvPyEQvF2= NWXX[ZhPOjF4MkG4PFM>
U251 cells M13pSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NXi4RoUxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTJ3MTDj[YxteyxiTFO1NF02Njh{IN88US=> NWrvfYo2OjF4MkG4PFM>
LOXIMVI cells M4WwT2N6fG:2b4jpZ4l1gSCjc4PhfS=> NFTTZZFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNV1iLTW\JJINmdGy|LDDMR|UxRTZwMESg{txO M4jZPVIyPjJzOEiz
MDA-MB-435 cells MVzDfZRwfG:6aXPpeJkh[XO|YYm= M1q3PGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? NHrQdpczOTZ{MUi4Ny=>
SK-MEL-28 cells MlXLR5l1d3SxeHnjbZR6KGG|c3H5 M3;tXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD2yPEBk\WyuczygUGM2OD1|MT65JO69VQ>? NU\0To1EOjF4MkG4PFM>
SK-MEL-5 cells MWHDfZRwfG:6aXPpeJkh[XO|YYm= MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyxiTFO1NF01NjB{IN88US=> NHHWbmwzOTZ{MUi4Ny=>
UACC257 cells NGO3ZnhEgXSxdH;4bYNqfHliYYPzZZk> Ml[4R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWWFESzJ3NzDj[YxteyxiTFO1NF01PC56IN88US=> M2XvSlIyPjJzOEiz
UACC62 cells M1\RPGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMtKEyFNUC9Ok4{QSEQvF2= NH;KWW8zOTZ{MUi4Ny=>
IGROV1 cells M{\Ec2N6fG:2b4jpZ4l1gSCjc4PhfS=> M{HW[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGlIWk:YMTDj[YxteyxiTFO1NF01QC57IN88US=> MljQNlE3OjF6OEO=
OVCAR5 cells M{TBZmN6fG:2b4jpZ4l1gSCjc4PhfS=> NU\FfllPS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO M3H4Z|IyPjJzOEiz
SKOV3 cells M3\DdmN6fG:2b4jpZ4l1gSCjc4PhfS=> NYn6SoU4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNuIFzDOVA:OjhwNTFOwG0> MmO2NlE3OjF6OEO=
A498 cells MkPsR5l1d3SxeHnjbZR6KGG|c3H5 MWjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzMEBNSzVyPUWuPFgh|ryP MYmyNVYzOTh6Mx?=
Caki1 cells M1jRZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> MnfoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gR4FscTFiY3XscJMtKEyFNUC9OU44QSEQvF2= MXmyNVYzOTh6Mx?=
HCT116 cells M3rV[3Bzd2yrZnXyZZRqd25iYYPzZZk> M4PSdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= NUfZXpVQOjF5NEK0PVY>
HCT116 cells NInUVXlRem:uaX\ldoF1cW:wIHHzd4F6 NHLjUY5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NF0xNjBzOTFOwG0> MlfkNlE3PTB{MkG=
H1299 cells NEPVZZRRem:uaX\ldoF1cW:wIHHzd4F6 Ml\jRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OD1yLkGg{txO M{DjVVIyPjVyMkKx
HCT116 cells M{LmTnBzd2yrZnXyZZRqd25iYYPzZZk> MX3Jcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKQ2SxNVYh[2WubIOgdJJwdGmoZYLheIlwdixiSVO1NF0xNjBzIN88US=> MlPMNVQ3OTN|MUK=
RPMI8226 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 MlPjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUUF3JPFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MkOg{txO MnPKNlE3OjF6OEO=
CHO cells M2LEUGZ2dmO2aX;uJIF{e2G7 M4H1S2lvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO NInM[FQzODJyNUO5OC=>
HL-60(TB) cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiOLU[wLHRDMSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NEmg{txO MV2yNVYzOTh6Mx?=
RXF393 cells MorjVJJwdGmoZYLheIlwdiCjc4PhfS=> M3n2VGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmjGN|k{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjBzIN88US=> NHLMb|czOTZ{MUi4Ny=>
RXF393 cells MoXER5l1d3SxeHnjbZR6KGG|c3H5 MlfYR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN NUK3SnVbOjF4MkG4PFM>

... 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