Dacinostat (LAQ824)

製品コードS1095 別名:NVP-LAQ824

Dacinostat (LAQ824)化学構造

分子量(MW):379.459

Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.

サイズ 価格(税別)  
JPY 69720.00
JPY 53120.00
JPY 161020.00

カスタマーフィードバック(5)

  • 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.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
ターゲット
HDAC [1]
(Cell-free assay)
32 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1299 MnTrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnnYTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGgyOjl7IHj1cYFvKGy3bnegZ4Fz[2mwb33hJINmdGxiZ4Lve5RpNCCLQ{WwQVAvOTVizszN NVO1RmtEOTR3MkG0NlI>
HCT116 NH7vU|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NW\ROWFUUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiFVEGxOkBpfW2jbjDjc4xwdiClZXzsJIdzd3e2aDygTWM2OD1yLkCxJO69VQ>? MYCxOFUzOTR{Mh?=
HCT116 MkTzR5l1d3SxeHnjbZR6KGG|c3H5 Mn3HR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1yLkC1JO69VQ>? NET3fmUyPzl2MU[yOS=>
human mammary epithelial cells M1;yTmN6fG:2b4jpZ4l1gSCjc4PhfS=> M2XOcmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? M3\ue|E4QTRzNkK1
HEK293 cells MUfGeY5kfGmxbjDhd5NigQ>? NXjifGRLUW6qaXLpeIlwdiCxZjDISGFEOSCrbjDISWszQTNiY3XscJMtKEmFNUC9NE4xODJ4IN88US=> NVXM[mtGOTh|MEi1OlM>
HeLa cells M{S2[WZ2dmO2aX;uJIF{e2G7 M{K4eFAvOyEQvF2= M1f3TFE3KGh? NG\XRVBKdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 M13mbFE4QTV4OUi4
HCT116 cells NUPMdIdVWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYTacZZjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMEGzJO69VQ>? NU\3emdCOjB{MEWzPVQ>
H1299 cells M1fxNnBzd2yrZnXyZZRqd25iYYPzZZk> MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|IHL5JG1VWyCjc4PhfUwhUUN3ME2wMlE3OSEQvF2= M4G2VlIxOjB3M{m0
H460 cells MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWG0PEBp M2ThRWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGg1PjBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JHNTSiCjc4PhfUwhUUN3ME2wMlA4KM7:TR?= M3vOZVIyODd|MU[w
HCT116 cells MnHkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4HlV|Q5KGh? M3XMTWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF6IN88US=> MnjMNlExPzNzNkC=
CCRF-CEM cells NWnZeWFPWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVvKZZBuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDR3JHNUOHTTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yOVEh|ryP MnLKNlE3OjF6OEO=
K562 cells MlLLVJJwdGmoZYLheIlwdiCjc4PhfS=> M4fzNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42PSEQvF2= NUHkR3FzOjF4MkG4PFM>
MOLT4 cells NYTPWWZ2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NWTISXpiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO M3XzXVIyPjJzOEiz
SR cells MnL5VJJwdGmoZYLheIlwdiCjc4PhfS=> MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{Lkm5JO69VQ>? NULxfFR4OjF4MkG4PFM>
A549 cells M4faNHBzd2yrZnXyZZRqd25iYYPzZZk> NEfRe4VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NELLdHAzOTZ{MUi4Ny=>
EKVX cells M3ixNXBzd2yrZnXyZZRqd25iYYPzZZk> MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP MlXTNlE3OjF6OEO=
HOP62 cells NIjyTGhRem:uaX\ldoF1cW:wIHHzd4F6 M2jZcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTB{IN88US=> NGX6N|EzOTZ{MUi4Ny=>
HOP92 cells Ml[5VJJwdGmoZYLheIlwdiCjc4PhfS=> NFPZfHhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFkzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF7OTFOwG0> M{[xZVIyPjJzOEiz
NCI-H226 cells MkHXVJJwdGmoZYLheIlwdiCjc4PhfS=> NH7vUo1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjJ4IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkSxJO69VQ>? NFj4eIwzOTZ{MUi4Ny=>
NCI-H23 cells NUftT5BpWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF7LVHFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNTFOwG0> NX\EUZN7OjF4MkG4PFM>
NCI-H322M cells NITXN4RRem:uaX\ldoF1cW:wIHHzd4F6 NWfhbpl7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN{Ml2gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuNlYh|ryP MYeyNVYzOTh6Mx?=
NCI-H460 cells MVPQdo9tcW[ncnH0bY9vKGG|c3H5 MoDCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> M2X5[VIyPjJzOEiz
COLO205 cells NUTqVmJWWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn3nRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> NEfCTpIzOTZ{MUi4Ny=>
HCT116 cells M1PYSHBzd2yrZnXyZZRqd25iYYPzZZk> MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN MVmyNVYzOTh6Mx?=
HCT15 cells NEjXdlZRem:uaX\ldoF1cW:wIHHzd4F6 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= NGXBc4kzOTZ{MUi4Ny=>
HT-29 cells NEexVHFRem:uaX\ldoF1cW:wIHHzd4F6 M3j6Z2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTZ4IN88US=> NVzofZBqOjF4MkG4PFM>
KM12 cells NXHwWIVnWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2mwemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xPCEQvF2= MkP6NlE3OjF6OEO=
SW620 cells M3n5[3Bzd2yrZnXyZZRqd25iYYPzZZk> M33IR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDd6IN88US=> MkfVNlE3OjF6OEO=
SF268 cells MoHBVJJwdGmoZYLheIlwdiCjc4PhfS=> M4jDNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN NHfLdlkzOTZ{MUi4Ny=>
SF295 cells NUfvWZdZWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= NEX6SJgzOTZ{MUi4Ny=>
SF539 cells MmTPVJJwdGmoZYLheIlwdiCjc4PhfS=> Ml23RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkWzPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE46PjVizszN NUX0N|hFOjF4MkG4PFM>
SNB19 cells MkfsVJJwdGmoZYLheIlwdiCjc4PhfS=> MlT1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= Ml3WNlE3OjF6OEO=
SNB75 cells NVPOXFREWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIDHW25CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPORlc2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjNzODFOwG0> MXWyNVYzOTh6Mx?=
U251 cells MYrQdo9tcW[ncnH0bY9vKGG|c3H5 NIrMTndCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> NV3mNHhCOjF4MkG4PFM>
LOXIMVI cells NIS3NXpRem:uaX\ldoF1cW:wIHHzd4F6 NGPmcoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO NEi0d4MzOTZ{MUi4Ny=>
MALME-3M cells NVfqXXZkWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> NWTZR5F[OjF4MkG4PFM>
M14 cells M{\3[3Bzd2yrZnXyZZRqd25iYYPzZZk> MnvlRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMUSgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPFQ6KM7:TR?= MVSyNVYzOTh6Mx?=
MDA-MB-435 cells M1PCN3Bzd2yrZnXyZZRqd25iYYPzZZk> MnzERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? Mlr1NlE3OjF6OEO=
SK-MEL-28 cells MmjOVJJwdGmoZYLheIlwdiCjc4PhfS=> MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE0zQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57OUOg{txO MoTkNlE3OjF6OEO=
SK-MEL-5 cells NYfOO5RsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ5MTFOwG0> MW[yNVYzOTh6Mx?=
UACC257 cells NID2XHRRem:uaX\ldoF1cW:wIHHzd4F6 NYXTN2lrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkO5N{DPxE1? MnG2NlE3OjF6OEO=
UACC62 cells M2jaNnBzd2yrZnXyZZRqd25iYYPzZZk> NUnC[ndCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVRWNEPjJiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{e5JO69VQ>? NFj1bJUzOTZ{MUi4Ny=>
IGROV1 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NWPmPFBUSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? M3vKPFIyPjJzOEiz
OVCAR3 cells MmW3VJJwdGmoZYLheIlwdiCjc4PhfS=> MnWyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN NV[3c5FbOjF4MkG4PFM>
OVCAR4 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 NWTTOHRSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNwMkGg{txO NH3UNmczOTZ{MUi4Ny=>
OVCAR5 cells NEmwUXZRem:uaX\ldoF1cW:wIHHzd4F6 MkD1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOjZizszN MljCNlE3OjF6OEO=
OVCAR8 cells NHTEfZNRem:uaX\ldoF1cW:wIHHzd4F6 NVPpT|VxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO MnTKNlE3OjF6OEO=
NCI/ADR-RES cells M2PkWnBzd2yrZnXyZZRqd25iYYPzZZk> MoPyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mvRWRTNVKHUzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6xPEDPxE1? NI\ac44zOTZ{MUi4Ny=>
SKOV3 cells MnTNVJJwdGmoZYLheIlwdiCjc4PhfS=> MlzTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN MnniNlE3OjF6OEO=
786-0 cells Mn60VJJwdGmoZYLheIlwdiCjc4PhfS=> M1HXOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN M33TelIyPjJzOEiz
A498 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 M{LRcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= M{PUNlIyPjJzOEiz
ACHN cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 M1;kc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQVPIUkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yKM7:TR?= M2W3XVIyPjJzOEiz
Caki1 cells NH\uOndRem:uaX\ldoF1cW:wIHHzd4F6 NFrp[nlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhb4kyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjZzOTFOwG0> NEjBWIIzOTZ{MUi4Ny=>
SN12C cells M3r5PXBzd2yrZnXyZZRqd25iYYPzZZk> MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQMULDJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zMlkzKM7:TR?= M3XvNVIyPjJzOEiz
TK10 cells M2XvU3Bzd2yrZnXyZZRqd25iYYPzZZk> NEHOVHFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTLNVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDR2IN88US=> NGrqNnEzOTZ{MUi4Ny=>
UO31 cells NU\aO2pwWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mon2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXT{OxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlQ2OiEQvF2= NF3rU4IzOTZ{MUi4Ny=>
PC3 cells NF\r[mhRem:uaX\ldoF1cW:wIHHzd4F6 NG[0flJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlAh|ryP M1\RflIyPjJzOEiz
DU145 cells M1\UTnBzd2yrZnXyZZRqd25iYYPzZZk> NXT2NlVkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDEWVE1PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OjlwOTFOwG0> M1Xa[FIyPjJzOEiz
MCF7 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 M17WWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok46OSEQvF2= MXKyNVYzOTh6Mx?=
MDA-MB-231 cells NGPETJZRem:uaX\ldoF1cW:wIHHzd4F6 NYnkc3hLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zNU44KM7:TR?= M3vrd|IyPjJzOEiz
Hs 578T cells MmPuVJJwdGmoZYLheIlwdiCjc4PhfS=> M4i4eGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIOgOVc5XCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:PS56MjFOwG0> NILuU28zOTZ{MUi4Ny=>
BT549 cells NYPVXnZpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEKWNUS5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlA1KM7:TR?= M4rkc|IyPjJzOEiz
T47D cells M1;4W3Bzd2yrZnXyZZRqd25iYYPzZZk> NIHxR4xCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGS0O2Qh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI5NjhizszN NGrGT4QzOTZ{MUi4Ny=>
MDA-MB-468 cells M3nTS3Bzd2yrZnXyZZRqd25iYYPzZZk> M3H5emFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? NHr1S4kzOTZ{MUi4Ny=>
NCI-H226 cells MW\DfZRwfG:6aXPpeJkh[XO|YYm= NF;RcYdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> NH7ye4EzOTZ{MUi4Ny=>
KM12 cells NHf6V5ZEgXSxdH;4bYNqfHliYYPzZZk> MoHBR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT20yOiClZXzsd{whVEN3ME2yPU46KM7:TR?= MUWyNVYzOTh6Mx?=
SF295 cells Mk[zR5l1d3SxeHnjbZR6KGG|c3H5 M3e5N2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjl3IHPlcIx{NCCOQ{WwQVYvQTFizszN MUmyNVYzOTh6Mx?=
SNB19 cells NYLwcIo3S3m2b4TvfIlkcXS7IHHzd4F6 MljKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25DOTliY3XscJMtKEyFNUC9N|EvPyEQvF2= M3m3S|IyPjJzOEiz
U251 cells M4TmT2N6fG:2b4jpZ4l1gSCjc4PhfS=> NXv0[IliS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXTJ3MTDj[YxteyxiTFO1NF02Njh{IN88US=> NFXXXpYzOTZ{MUi4Ny=>
LOXIMVI cells M3XN[GN6fG:2b4jpZ4l1gSCjc4PhfS=> M{D3WWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxQYEmPVlmgZ4VtdHNuIFzDOVA:Pi5yNDFOwG0> NU\aPYQ5OjF4MkG4PFM>
MDA-MB-435 cells M37mZWN6fG:2b4jpZ4l1gSCjc4PhfS=> M1;0R2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? M4ixUVIyPjJzOEiz
SK-MEL-28 cells NWn2XXpPS3m2b4TvfIlkcXS7IHHzd4F6 NWTEcoV{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzMEBNSzVyPUOxMlkh|ryP MWGyNVYzOTh6Mx?=
SK-MEL-5 cells M1jaRmN6fG:2b4jpZ4l1gSCjc4PhfS=> NGruZYJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? M1\y[FIyPjJzOEiz
UACC257 cells NHjrPZVEgXSxdH;4bYNqfHliYYPzZZk> M{SzXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N{NUegZ4VtdHNuIFzDOVA:PDRwODFOwG0> NGXLb2ozOTZ{MUi4Ny=>
UACC62 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= M1LhT2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> Ml3CNlE3OjF6OEO=
IGROV1 cells NI\YW2JEgXSxdH;4bYNqfHliYYPzZZk> NUfmU|dOS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO MWOyNVYzOTh6Mx?=
OVCAR5 cells NIHa[FlEgXSxdH;4bYNqfHliYYPzZZk> NW\4NHJKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO NH3DVmgzOTZ{MUi4Ny=>
SKOV3 cells NF7DSHpEgXSxdH;4bYNqfHliYYPzZZk> MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= NYn5[215OjF4MkG4PFM>
A498 cells MUTDfZRwfG:6aXPpeJkh[XO|YYm= M4TlcGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1QThiY3XscJMtKEyFNUC9OU45QCEQvF2= NWSzTIx4OjF4MkG4PFM>
Caki1 cells M2PFbWN6fG:2b4jpZ4l1gSCjc4PhfS=> MULDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDDZYtqOSClZXzsd{whVEN3ME21Mlc6KM7:TR?= NHzZb3UzOTZ{MUi4Ny=>
HCT116 cells NEXmU|hRem:uaX\ldoF1cW:wIHHzd4F6 NYLuVoRVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEmFNUC9NE4xOTlizszN MUeyNVc1OjR7Nh?=
HCT116 cells NVXuVXdnWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIHaWFFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdixiSVO1NF0xNjBzOTFOwG0> NF7TNYszOTZ3MEKyNS=>
H1299 cells Mn7EVJJwdGmoZYLheIlwdiCjc4PhfS=> MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEhzMkm5JINmdGy|LDDJR|UxRTBwMTFOwG0> M1zYPFIyPjVyMkKx
HCT116 cells M3i0NHBzd2yrZnXyZZRqd25iYYPzZZk> MV\Jcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCKQ2SxNVYh[2WubIOgdJJwdGmoZYLheIlwdixiSVO1NF0xNjBzIN88US=> NUCyZVNiOTR4MUOzNVI>
RPMI8226 cells NGPtfXlRem:uaX\ldoF1cW:wIHHzd4F6 MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKSTVm4NlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{MzFOwG0> Mm\vNlE3OjF6OEO=
CHO cells MYHGeY5kfGmxbjDhd5NigQ>? M4nvW2lvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO M{LVeFIxOjB3M{m0
HL-60(TB) cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 MmTLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTD22NEhVSiliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkS5JO69VQ>? M1zmXVIyPjJzOEiz
RXF393 cells MoL4VJJwdGmoZYLheIlwdiCjc4PhfS=> MoLQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN NEXi[nUzOTZ{MUi4Ny=>
RXF393 cells NIX5VGhEgXSxdH;4bYNqfHliYYPzZZk> NVvObYloS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWliIM{mzJINmdGy|LDDMR|UxRTF3LkOg{txO M1T5fVIyPjJzOEiz

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

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.
細胞試験: [1]
+ 展開
  • 細胞株: H1299, HCT116, DU145, PC3 and MDA435 cells
  • 濃度: 0-10 μM
  • 反応時間: 48 hours
  • 実験の流れ: 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.
    (参考用のみ)
動物試験:[1]
+ 展開
  • 動物モデル: HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
  • 製剤: LAQ824 is dissolved in DMSO.
  • 投薬量: ≤100 mg/kg
  • 投与方法: Administered via i.v.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 76 mg/mL (200.28 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
1% DMSO+30% polyethylene glycol+1% Tween 80
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 379.459
化学式

C22H25N3O3

CAS No. 404951-53-7
保管
in solvent
別名 NVP-LAQ824

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HDACシグナル伝達経路

HDAC Inhibitors with Unique Features

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