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 Mo[4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUTK[2tOUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEhzMkm5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMUWg{txO NHvFVmYyPDV{MUSyNi=>
HCT116 NWjTcHh6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVXJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTGNVOTF4IHj1cYFvKGOxbH;uJINmdGxiZ4Lve5RpNCCLQ{WwQVAvODFizszN NV7qS3RbOTR3MkG0NlI>
HCT116 NUHJbVVLS3m2b4TvfIlkcXS7IHHzd4F6 NHTLUJFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP M{TvUVE4QTRzNkK1
human mammary epithelial cells M2PqZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NH7SOGhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP M1XHVFE4QTRzNkK1
HEK293 cells M1PBeGZ2dmO2aX;uJIF{e2G7 NXfaZ5BHUW6qaXLpeIlwdiCxZjDISGFEOSCrbjDISWszQTNiY3XscJMtKEmFNUC9NE4xODJ4IN88US=> MUWxPFMxQDV4Mx?=
HeLa cells NH3q[pNHfW6ldHnvckBie3OjeR?= MXSwMlMh|ryP MkK5NVYhcA>? M3e3SmlvcGmkaYTpc44hd2ZiSFTBR|QudWWmaXH0[YQhemWycnXzd4lwdiCxZjDNSWYzNWSncHXu[IVvfCC2cnHud4NzcXC2aX;uJIlvKEinTHGgZ4VtdHNiYYSgNE4{KHWPIHHmeIVzKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MXexO|k2Pjl6OB?=
HCT116 cells MmrjVJJwdGmoZYLheIlwdiCjc4PhfS=> NF3aXFBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO M3PqU|IxOjB3M{m0
H1299 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M1LBPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSEGyPVkh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvOTZzIN88US=> MY[yNFIxPTN7NB?=
H460 cells NULsc3ExT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknxOFghcA>? NGK4Zm9Iem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJPDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xPyEQvF2= MnPENlExPzNzNkC=
HCT116 cells MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWq0PEBp M2PidWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODF6IN88US=> NXH3coZJOjFyN{OxOlA>
CCRF-CEM cells MoqwVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn7qRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQ2LGMWNGVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NUGg{txO MYSyNVYzOTh6Mx?=
K562 cells MmD4VJJwdGmoZYLheIlwdiCjc4PhfS=> NWPQR3U5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> M4\TbVIyPjJzOEiz
MOLT4 cells NFf1c4lRem:uaX\ldoF1cW:wIHHzd4F6 NVfEbWs1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO MXWyNVYzOTh6Mx?=
SR cells M{Dib3Bzd2yrZnXyZZRqd25iYYPzZZk> Mmm4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj65PUDPxE1? NXvxRWtQOjF4MkG4PFM>
A549 cells M4XtW3Bzd2yrZnXyZZRqd25iYYPzZZk> MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNFkh|ryP NEX0S4gzOTZ{MUi4Ny=>
EKVX cells MnPSVJJwdGmoZYLheIlwdiCjc4PhfS=> NIG5VXhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFXLWngh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPzVizszN M4nYRVIyPjJzOEiz
HOP62 cells M{PW[HBzd2yrZnXyZZRqd25iYYPzZZk> NWf1W3VjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A3OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53MEKg{txO NW\0e2lROjF4MkG4PFM>
HOP92 cells MYHQdo9tcW[ncnH0bY9vKGG|c3H5 NUXYZ3lNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A6OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5zOUmg{txO M3j1PFIyPjJzOEiz
NCI-H226 cells NHzyO2ZRem:uaX\ldoF1cW:wIHHzd4F6 MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> M1LufFIyPjJzOEiz
NCI-H23 cells NFPPN2NRem:uaX\ldoF1cW:wIHHzd4F6 Mme0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN MnXCNlE3OjF6OEO=
NCI-H322M cells MnHrVJJwdGmoZYLheIlwdiCjc4PhfS=> M4ryc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OjKPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{LkK2JO69VQ>? MmmxNlE3OjF6OEO=
NCI-H460 cells NYXYcFV5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NWS1ZVlrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? M{\JVVIyPjJzOEiz
COLO205 cells MkPYVJJwdGmoZYLheIlwdiCjc4PhfS=> NWXqdIRjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? NXTQT2c{OjF4MkG4PFM>
HCT116 cells MnHWVJJwdGmoZYLheIlwdiCjc4PhfS=> NE\4XXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|NEeg{txO NHLi[4czOTZ{MUi4Ny=>
HCT15 cells M4X5R3Bzd2yrZnXyZZRqd25iYYPzZZk> MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= MVmyNVYzOTh6Mx?=
HT-29 cells NFLy[oNRem:uaX\ldoF1cW:wIHHzd4F6 NVHkUFV[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO MWOyNVYzOTh6Mx?=
KM12 cells Mlf1VJJwdGmoZYLheIlwdiCjc4PhfS=> MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPMUKgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNFQh|ryP MYWyNVYzOTh6Mx?=
SW620 cells M4fTOHBzd2yrZnXyZZRqd25iYYPzZZk> NU\zXJBXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52N{ig{txO Moi1NlE3OjF6OEO=
SF268 cells MmfPVJJwdGmoZYLheIlwdiCjc4PhfS=> NFyyWI9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlY5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjV|IN88US=> NVz5OmNKOjF4MkG4PFM>
SF295 cells MnO1VJJwdGmoZYLheIlwdiCjc4PhfS=> MmXmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK5OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE44PDNizszN NUHOfFJwOjF4MkG4PFM>
SF539 cells MojkVJJwdGmoZYLheIlwdiCjc4PhfS=> MnvRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkWzPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE46PjVizszN MX:yNVYzOTh6Mx?=
SNB19 cells M1r1cXBzd2yrZnXyZZRqd25iYYPzZZk> MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQkG5JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= NHftSmszOTZ{MUi4Ny=>
SNB75 cells MlTHVJJwdGmoZYLheIlwdiCjc4PhfS=> NITU[HNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPORlc2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjNzODFOwG0> M{LwOVIyPjJzOEiz
U251 cells NV:weXg6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MmPkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NWPJ[HVVOjF4MkG4PFM>
LOXIMVI cells MVjQdo9tcW[ncnH0bY9vKGG|c3H5 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN NF\4N4wzOTZ{MUi4Ny=>
MALME-3M cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 NUL3eYs1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNRWxOTS1|TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD60OlEh|ryP M1PFXVIyPjJzOEiz
M14 cells NVXkdmpxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M2fIUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTUG0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlg1QSEQvF2= M{fpfFIyPjJzOEiz
MDA-MB-435 cells M{PBXnBzd2yrZnXyZZRqd25iYYPzZZk> M3TrdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP NF7CVowzOTZ{MUi4Ny=>
SK-MEL-28 cells NHnDe4lRem:uaX\ldoF1cW:wIHHzd4F6 MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE0zQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57OUOg{txO MWmyNVYzOTh6Mx?=
SK-MEL-5 cells NY\McnpKWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4DhO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkexJO69VQ>? M3jNb|IyPjJzOEiz
UACC257 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 MlvuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDNlU4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN7MzFOwG0> MX6yNVYzOTh6Mx?=
UACC62 cells M1XtfnBzd2yrZnXyZZRqd25iYYPzZZk> MkTVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> NULldVAzOjF4MkG4PFM>
IGROV1 cells NUfFWW5WWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1HqV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSVfSU3YyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF6NzFOwG0> MXqyNVYzOTh6Mx?=
OVCAR3 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= MmHpNlE3OjF6OEO=
OVCAR4 cells MUTQdo9tcW[ncnH0bY9vKGG|c3H5 MlLMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvOjFizszN Mk\4NlE3OjF6OEO=
OVCAR5 cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 MofLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOjZizszN NULBbo9sOjF4MkG4PFM>
OVCAR8 cells NIPsZ3NRem:uaX\ldoF1cW:wIHHzd4F6 NI\kUGJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NTFOwG0> NETFTpkzOTZ{MUi4Ny=>
NCI/ADR-RES cells M2G1OnBzd2yrZnXyZZRqd25iYYPzZZk> NXzLbHE4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= M4jaVlIyPjJzOEiz
SKOV3 cells MlPRVJJwdGmoZYLheIlwdiCjc4PhfS=> MnnWRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN NYXiNng{OjF4MkG4PFM>
786-0 cells NGe2R5hRem:uaX\ldoF1cW:wIHHzd4F6 NWXITXZTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjC3PFYuOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5|ODFOwG0> NUK2fGp7OjF4MkG4PFM>
A498 cells MWfQdo9tcW[ncnH0bY9vKGG|c3H5 NUOwN3BsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> M1vjelIyPjJzOEiz
ACHN cells M2DrRXBzd2yrZnXyZZRqd25iYYPzZZk> MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? MYiyNVYzOTh6Mx?=
Caki1 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 M1W3SmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> NVv4UXR6OjF4MkG4PFM>
SN12C cells MnnoVJJwdGmoZYLheIlwdiCjc4PhfS=> MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQMULDJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zMlkzKM7:TR?= MoX4NlE3OjF6OEO=
TK10 cells MnG2VJJwdGmoZYLheIlwdiCjc4PhfS=> MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= NGLK[WozOTZ{MUi4Ny=>
UO31 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NGPGNVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXPN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDV{IN88US=> M3T6VVIyPjJzOEiz
PC3 cells NYfte4RWWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MkCg{txO NHzEWFQzOTZ{MUi4Ny=>
DU145 cells MVLQdo9tcW[ncnH0bY9vKGG|c3H5 MofwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCGVUG0OUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlkvQSEQvF2= MnSzNlE3OjF6OEO=
MCF7 cells NH\6VHpRem:uaX\ldoF1cW:wIHHzd4F6 M{jleWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok46OSEQvF2= MnPWNlE3OjF6OEO=
MDA-MB-231 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 MoK2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1|MT63JO69VQ>? M1[1TFIyPjJzOEiz
Hs 578T cells NUDZTJpCWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmPJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKczC1O|hVKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF02Njh{IN88US=> M3PwXFIyPjJzOEiz
BT549 cells MmHYVJJwdGmoZYLheIlwdiCjc4PhfS=> NIf3fIFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFLUOVQ6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjB2IN88US=> NFnuNXozOTZ{MUi4Ny=>
T47D cells M3SwSnBzd2yrZnXyZZRqd25iYYPzZZk> MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUK4Mlgh|ryP MXmyNVYzOTh6Mx?=
MDA-MB-468 cells M2TQNnBzd2yrZnXyZZRqd25iYYPzZZk> NVnyWoJySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= NYfTfFJnOjF4MkG4PFM>
NCI-H226 cells MWPDfZRwfG:6aXPpeJkh[XO|YYm= MnntR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNuIFzDOVA:OjBizszN MlrBNlE3OjF6OEO=
KM12 cells MYTDfZRwfG:6aXPpeJkh[XO|YYm= M3j6SmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtOOTJiY3XscJMtKEyFNUC9NlkvQSEQvF2= MnTuNlE3OjF6OEO=
SF295 cells MlTnR5l1d3SxeHnjbZR6KGG|c3H5 MlvDR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= M4Pme|IyPjJzOEiz
SNB19 cells NIjtTnBEgXSxdH;4bYNqfHliYYPzZZk> NYTR[I9rS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW06EMUmgZ4VtdHNuIFzDOVA:OzFwNzFOwG0> MVeyNVYzOTh6Mx?=
U251 cells MmTTR5l1d3SxeHnjbZR6KGG|c3H5 NF7FfVZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWOjVzIHPlcIx{NCCOQ{WwQVUvQDJizszN M2XGdlIyPjJzOEiz
LOXIMVI cells MWTDfZRwfG:6aXPpeJkh[XO|YYm= NVTKbpY1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE:[SV3WTUBk\WyuczygUGM2OD14LkC0JO69VQ>? NG[zRYgzOTZ{MUi4Ny=>
MDA-MB-435 cells NYm5ZXFWS3m2b4TvfIlkcXS7IHHzd4F6 NFzqVppEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzMEBNSzVyPUK4Mlgh|ryP M2GwclIyPjJzOEiz
SK-MEL-28 cells NF7NOW1EgXSxdH;4bYNqfHliYYPzZZk> MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNuIFzDOVA:OzFwOTFOwG0> Mor4NlE3OjF6OEO=
SK-MEL-5 cells NFzTenZEgXSxdH;4bYNqfHliYYPzZZk> M1TxbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD21JINmdGy|LDDMR|UxRTRwMEKg{txO MnfRNlE3OjF6OEO=
UACC257 cells Ml[4R5l1d3SxeHnjbZR6KGG|c3H5 MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVRWNEOjV5IHPlcIx{NCCOQ{WwQVQ1NjhizszN NGWycmszOTZ{MUi4Ny=>
UACC62 cells NYL1[FNzS3m2b4TvfIlkcXS7IHHzd4F6 M3TXfWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> MVWyNVYzOTh6Mx?=
IGROV1 cells NEnjU5hEgXSxdH;4bYNqfHliYYPzZZk> NHrpeodEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBKT1KRVkGgZ4VtdHNuIFzDOVA:PDhwOTFOwG0> M{naclIyPjJzOEiz
OVCAR5 cells NHP3enhEgXSxdH;4bYNqfHliYYPzZZk> M4C5XmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUNTDj[YxteyxiTFO1NF0{QC57IN88US=> MV:yNVYzOTh6Mx?=
SKOV3 cells MonLR5l1d3SxeHnjbZR6KGG|c3H5 M{\Zb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMV1Z|IHPlcIx{NCCOQ{WwQVI5NjVizszN M3jjbFIyPjJzOEiz
A498 cells MmjMR5l1d3SxeHnjbZR6KGG|c3H5 MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOFk5KGOnbHzzMEBNSzVyPUWuPFgh|ryP Mk\LNlE3OjF6OEO=
Caki1 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= NVPNN2JWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> NVXLdYlxOjF4MkG4PFM>
HCT116 cells M1Pxd3Bzd2yrZnXyZZRqd25iYYPzZZk> NWH1WVJ1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMtKEmFNUC9NE4xOTlizszN NE\YRXMzOTd2MkS5Oi=>
HCT116 cells NXfzc2c{WHKxbHnm[ZJifGmxbjDhd5NigQ>? MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Boem:5dHigbY5pcWKrdHnvckwhUUN3ME2wMlAyQSEQvF2= MYeyNVY2ODJ{MR?=
H1299 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 NWWwO5A1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{whUUN3ME2wMlEh|ryP Mn34NlE3PTB{MkG=
HCT116 cells M1TxRXBzd2yrZnXyZZRqd25iYYPzZZk> NIPVUXRKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDIR3QyOTZiY3XscJMheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCxJO69VQ>? MkP5NVQ3OTN|MUK=
RPMI8226 cells MV3Qdo9tcW[ncnH0bY9vKGG|c3H5 M4Dve2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? MmfvNlE3OjF6OEO=
CHO cells NYnRb5VTTnWwY4Tpc44h[XO|YYm= NH7RXIhKdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IHH1eI9u[XSnZDDwZZRkcCClbHHtdEBmdGWldILvdIh6e2mxbH;nfUBie3OjeTygTWM2OD1zMj6yJO69VQ>? NW\Ueo5YOjB{MEWzPVQ>
HL-60(TB) cells NYjNXXREWHKxbHnm[ZJifGmxbjDhd5NigQ>? NV\i[I9uSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUE03OCiWQjmgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNlQ6KM7:TR?= M1rwVlIyPjJzOEiz
RXF393 cells MX\Qdo9tcW[ncnH0bY9vKGG|c3H5 MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFK[RkO5N{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4xOSEQvF2= NEHaS2czOTZ{MUi4Ny=>
RXF393 cells NEf6emZEgXSxdH;4bYNqfHliYYPzZZk> MnmyR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVnhHOzl|IHPlcIx{NCCOQ{WwQVE2NjNizszN MkTKNlE3OjF6OEO=

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

相関HDAC製品

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID