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)は一種の新たなHDAC阻害剤で、IC50値が 32 nMになって、p21プロモータ(promoter)を作動させます。

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)は一種の新たなHDAC阻害剤で、IC50値が 32 nMになって、p21プロモータ(promoter)を作動させます。
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 M4frO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2LZXGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJOTJ7OTDoeY1idiCudX7nJINiemOrbn;tZUBk\WyuIHfyc5d1cCxiSVO1NF0xNjF3IN88US=> M1;GPFE1PTJzNEKy
HCT116 M3TXemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MorjTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGhEXDFzNjDoeY1idiClb3zvckBk\WyuIHfyc5d1cCxiSVO1NF0xNjBzIN88US=> NULtN3NDOTR3MkG0NlI>
HCT116 MnTsR5l1d3SxeHnjbZR6KGG|c3H5 M{L5[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wOUDPxE1? MnvVNVc6PDF4MkW=
human mammary epithelial cells NUTm[GkzS3m2b4TvfIlkcXS7IHHzd4F6 M2nzemN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? NGjpdm0yPzl2MU[yOS=>
HEK293 cells MVHGeY5kfGmxbjDhd5NigQ>? Mmj1TY5pcWKrdHnvckBw\iCKRFHDNUBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6wNFI3KM7:TR?= M4TFNFE5OzB6NU[z
HeLa cells NEjPOG9HfW6ldHnvckBie3OjeR?= NIPOWpIxNjNizszN NH3B[WwyPiCq MoHOTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NYrEboNSOTd7NU[5PFg>
HCT116 cells NUXiUnUxWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4fQdWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjBzMzFOwG0> M{nOb|IxOjB3M{m0
H1299 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NW[5eYx{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5zNkGg{txO M2DxVVIxOjB3M{m0
H460 cells MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUi0PEBp NX;KUZNOT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUDR4MDDj[YxteyCjZoTldkA1QCCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODdizszN M3[yU|IyODd|MU[w
HCT116 cells MnjKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoLaOFghcA>? NUixNnJET3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO NYrxOIwxOjFyN{OxOlA>
CCRF-CEM cells NWK2SlJIWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> NIKyPHkzOTZ{MUi4Ny=>
K562 cells M{HFOHBzd2yrZnXyZZRqd25iYYPzZZk> NVXqVmFYSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> MYeyNVYzOTh6Mx?=
MOLT4 cells M4S5SnBzd2yrZnXyZZRqd25iYYPzZZk> NVraVmVOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xVPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUGg{txO NFWwZZQzOTZ{MUi4Ny=>
SR cells M4fKRnBzd2yrZnXyZZRqd25iYYPzZZk> MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{Lkm5JO69VQ>? NIS4[GEzOTZ{MUi4Ny=>
A549 cells NFnVNY9Rem:uaX\ldoF1cW:wIHHzd4F6 M1PNV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= NYPQOXMzOjF4MkG4PFM>
EKVX cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 M3HhXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= MYSyNVYzOTh6Mx?=
HOP62 cells MoTLVJJwdGmoZYLheIlwdiCjc4PhfS=> M3jZW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTB{IN88US=> NUDqRVVqOjF4MkG4PFM>
HOP92 cells M3e0dnBzd2yrZnXyZZRqd25iYYPzZZk> MlTTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN Mmi0NlE3OjF6OEO=
NCI-H226 cells M2\rXnBzd2yrZnXyZZRqd25iYYPzZZk> NWn4TWxHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{NjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MT60NUDPxE1? M2rvN|IyPjJzOEiz
NCI-H23 cells MX3Qdo9tcW[ncnH0bY9vKGG|c3H5 M2X1[WFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53IN88US=> M3u3WFIyPjJzOEiz
NCI-H322M cells NWHDW4ZtWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHT0Z3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzJ{TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj6yOkDPxE1? NHG4ZYMzOTZ{MUi4Ny=>
NCI-H460 cells M3rEZ3Bzd2yrZnXyZZRqd25iYYPzZZk> MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjdizszN MUeyNVYzOTh6Mx?=
COLO205 cells M3v6fXBzd2yrZnXyZZRqd25iYYPzZZk> M3i0VWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> MVeyNVYzOTh6Mx?=
HCT116 cells MofzVJJwdGmoZYLheIlwdiCjc4PhfS=> NI[zcIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|NEeg{txO M3rocVIyPjJzOEiz
HCT15 cells MoLBVJJwdGmoZYLheIlwdiCjc4PhfS=> NES1bG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjB5IN88US=> NGLqT2IzOTZ{MUi4Ny=>
HT-29 cells NGTLOmJRem:uaX\ldoF1cW:wIHHzd4F6 M{TafGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTZ4IN88US=> NUP6XY9SOjF4MkG4PFM>
KM12 cells NWjRbWJRWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nHNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xPCEQvF2= NX;IfFhCOjF4MkG4PFM>
SW620 cells NV7lToh7WHKxbHnm[ZJifGmxbjDhd5NigQ>? MnrERY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN NF;ablIzOTZ{MUi4Ny=>
SF268 cells NVTwN2xJWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= MYOyNVYzOTh6Mx?=
SF295 cells NVjtT|E3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NH6wUWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlk2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd2MzFOwG0> NUS3SHpLOjF4MkG4PFM>
SF539 cells MWDQdo9tcW[ncnH0bY9vKGG|c3H5 M{nrOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> MmP1NlE3OjF6OEO=
SNB19 cells NEjiV5JRem:uaX\ldoF1cW:wIHHzd4F6 MmG0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= NHnINY4zOTZ{MUi4Ny=>
SNB75 cells NVvVU3l3WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2PQdGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> NVXMNodROjF4MkG4PFM>
U251 cells Mn7FVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn\WRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMkWxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc4OyEQvF2= NXrzPFJZOjF4MkG4PFM>
LOXIMVI cells NX\lcpFSWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{DUfWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF;YTW1XUSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5yODFOwG0> MXyyNVYzOTh6Mx?=
MALME-3M cells NYrH[4J2WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> NEDwZYIzOTZ{MUi4Ny=>
M14 cells NIrDPWdRem:uaX\ldoF1cW:wIHHzd4F6 NVvJ[o1XSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNNVQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQDR7IN88US=> M3n3[|IyPjJzOEiz
MDA-MB-435 cells NXT2RmtnWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4nMUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP NUjIdnA3OjF4MkG4PFM>
SK-MEL-28 cells Mmm1VJJwdGmoZYLheIlwdiCjc4PhfS=> MlHaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuOjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwOUmzJO69VQ>? NW[xTm5COjF4MkG4PFM>
SK-MEL-5 cells NXO1ZlR5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M1rPd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkexJO69VQ>? NHzXbmgzOTZ{MUi4Ny=>
UACC257 cells M{HuenBzd2yrZnXyZZRqd25iYYPzZZk> NHXTZYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NYTnSYkxOjF4MkG4PFM>
UACC62 cells M4rPWnBzd2yrZnXyZZRqd25iYYPzZZk> M3Lp[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|YzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN5OTFOwG0> M3jwUFIyPjJzOEiz
IGROV1 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 M{DaWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSVfSU3YyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF6NzFOwG0> MWOyNVYzOTh6Mx?=
OVCAR3 cells MmPXVJJwdGmoZYLheIlwdiCjc4PhfS=> NGPGRXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> MXSyNVYzOTh6Mx?=
OVCAR4 cells M1HEd3Bzd2yrZnXyZZRqd25iYYPzZZk> NVP5ZYV1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjRiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTNwMkGg{txO MYmyNVYzOTh6Mx?=
OVCAR5 cells M2mxVHBzd2yrZnXyZZRqd25iYYPzZZk> M4Lj[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> M13jeFIyPjJzOEiz
OVCAR8 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 NHnwPXFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NTFOwG0> M17XXlIyPjJzOEiz
NCI/ADR-RES cells M1jkOHBzd2yrZnXyZZRqd25iYYPzZZk> MmXxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mvRWRTNVKHUzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6xPEDPxE1? MWGyNVYzOTh6Mx?=
SKOV3 cells M4[5[nBzd2yrZnXyZZRqd25iYYPzZZk> MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONT2[zJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUzPCEQvF2= MkD2NlE3OjF6OEO=
786-0 cells MnznVJJwdGmoZYLheIlwdiCjc4PhfS=> MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKDd6Nj2wJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlM5KM7:TR?= NU\ZWJpUOjF4MkG4PFM>
A498 cells MXfQdo9tcW[ncnH0bY9vKGG|c3H5 NH\KNYJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN NETH[|IzOTZ{MUi4Ny=>
ACHN cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 NWKwR497SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFizszN MVmyNVYzOTh6Mx?=
Caki1 cells NEfpdFdRem:uaX\ldoF1cW:wIHHzd4F6 NFLoVmtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhb4kyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjZzOTFOwG0> MYKyNVYzOTh6Mx?=
SN12C cells MlvhVJJwdGmoZYLheIlwdiCjc4PhfS=> MlXLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTkGyR{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{46OiEQvF2= M1:4U|IyPjJzOEiz
TK10 cells M1u5[nBzd2yrZnXyZZRqd25iYYPzZZk> NWK4PXNqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> MUWyNVYzOTh6Mx?=
UO31 cells MlnXVJJwdGmoZYLheIlwdiCjc4PhfS=> NVTPSZRLSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> MlnBNlE3OjF6OEO=
PC3 cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NXrHeYNxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= MV[yNVYzOTh6Mx?=
DU145 cells NXPhTZhZWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yPU46KM7:TR?= NH;J[ZYzOTZ{MUi4Ny=>
MCF7 cells NFjmUIhRem:uaX\ldoF1cW:wIHHzd4F6 MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPU[uPVEh|ryP NWLwbnRGOjF4MkG4PFM>
MDA-MB-231 cells M{f3TnBzd2yrZnXyZZRqd25iYYPzZZk> NEPNbW9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUOxMlch|ryP M3zyPVIyPjJzOEiz
Hs 578T cells NXWwbmc6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkHoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKczC1O|hVKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF02Njh{IN88US=> NE[4OFkzOTZ{MUi4Ny=>
BT549 cells MWXQdo9tcW[ncnH0bY9vKGG|c3H5 NX\aNGQxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDCWFU1QSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi5yNDFOwG0> M2j0V|IyPjJzOEiz
T47D cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NUDaTJg{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUOFdFKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQC56IN88US=> M4nzN|IyPjJzOEiz
MDA-MB-468 cells Ml[1VJJwdGmoZYLheIlwdiCjc4PhfS=> M{fRU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR4ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;NT64PEDPxE1? M1\x[lIyPjJzOEiz
NCI-H226 cells NYjEcHFJS3m2b4TvfIlkcXS7IHHzd4F6 MnfNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUmNKNUh{Mk[gZ4VtdHNuIFzDOVA:OjBizszN NX\DW|g3OjF4MkG4PFM>
KM12 cells NIXJVXVEgXSxdH;4bYNqfHliYYPzZZk> MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzMEBNSzVyPUK5Mlkh|ryP NVvBfVZZOjF4MkG4PFM>
SF295 cells NGe5UJdEgXSxdH;4bYNqfHliYYPzZZk> M2fyVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNHOjl3IHPlcIx{NCCOQ{WwQVYvQTFizszN MXOyNVYzOTh6Mx?=
SNB19 cells MY\DfZRwfG:6aXPpeJkh[XO|YYm= MlPJR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25DOTliY3XscJMtKEyFNUC9N|EvPyEQvF2= NGLiUZozOTZ{MUi4Ny=>
U251 cells NEP6XXBEgXSxdH;4bYNqfHliYYPzZZk> M4frbGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHUzPTFiY3XscJMtKEyFNUC9OU45OiEQvF2= MUeyNVYzOTh6Mx?=
LOXIMVI cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= MkfVR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG9ZUU2YSTDj[YxteyxiTFO1NF03NjB2IN88US=> MonvNlE3OjF6OEO=
MDA-MB-435 cells MXPDfZRwfG:6aXPpeJkh[XO|YYm= NH7LRZJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFM2KGOnbHzzMEBNSzVyPUK4Mlgh|ryP MmP5NlE3OjF6OEO=
SK-MEL-28 cells NVTKPXlSS3m2b4TvfIlkcXS7IHHzd4F6 NYL5SFdoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTVXMMVI5KGOnbHzzMEBNSzVyPUOxMlkh|ryP Mm\INlE3OjF6OEO=
SK-MEL-5 cells NVHxWm5ES3m2b4TvfIlkcXS7IHHzd4F6 MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyxiTFO1NF01NjB{IN88US=> NYXUflJMOjF4MkG4PFM>
UACC257 cells M1PzdWN6fG:2b4jpZ4l1gSCjc4PhfS=> NF36SHBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFMkW3JINmdGy|LDDMR|UxRTR2Lkig{txO NGHOdJYzOTZ{MUi4Ny=>
UACC62 cells NVTzUpRxS3m2b4TvfIlkcXS7IHHzd4F6 NIDITHdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFNkKgZ4VtdHNuIFzDOVA:Pi5|OTFOwG0> MnrONlE3OjF6OEO=
IGROV1 cells M1jZ[mN6fG:2b4jpZ4l1gSCjc4PhfS=> NYT4XFcyS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUUeUT2[xJINmdGy|LDDMR|UxRTR6Lkmg{txO MWGyNVYzOTh6Mx?=
OVCAR5 cells NHjsepZEgXSxdH;4bYNqfHliYYPzZZk> NWG1[WF[S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hV1[FQWK1JINmdGy|LDDMR|UxRTN6Lkmg{txO NWr3UYJpOjF4MkG4PFM>
SKOV3 cells MWjDfZRwfG:6aXPpeJkh[XO|YYm= MVXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= MX2yNVYzOTh6Mx?=
A498 cells NXfUNmMxS3m2b4TvfIlkcXS7IHHzd4F6 Mn23R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVQ6QCClZXzsd{whVEN3ME21Mlg5KM7:TR?= Ml\RNlE3OjF6OEO=
Caki1 cells MWjDfZRwfG:6aXPpeJkh[XO|YYm= NUTNUm5xS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> NFjQOnEzOTZ{MUi4Ny=>
HCT116 cells MXzQdo9tcW[ncnH0bY9vKGG|c3H5 MmPYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOsJGlEPTB;MD6wNVkh|ryP NH25Z48zOTd2MkS5Oi=>
HCT116 cells NVr4Um5YWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{n4U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> NYfRVI9GOjF4NUCyNlE>
H1299 cells MlLuVJJwdGmoZYLheIlwdiCjc4PhfS=> NUGzZZVkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDINVI6QSClZXzsd{whUUN3ME2wMlEh|ryP NUfGRpFyOjF4NUCyNlE>
HCT116 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 NEH0NmRKdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDIR3QyOTZiY3XscJMheHKxbHnm[ZJifGmxbjygTWM2OD1yLkCxJO69VQ>? NV75S3BPOTR4MUOzNVI>
RPMI8226 cells M3HaV3Bzd2yrZnXyZZRqd25iYYPzZZk> M2nIT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? M{X5NFIyPjJzOEiz
CHO cells NXPQVoo3TnWwY4Tpc44h[XO|YYm= NHrGVI9KdmirYnn0bY9vKG:oIHj1cYFvKEWURzDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IHH1eI9u[XSnZDDwZZRkcCClbHHtdEBmdGWldILvdIh6e2mxbH;nfUBie3OjeTygTWM2OD1zMj6yJO69VQ>? MUiyNFIxPTN7NB?=
HL-60(TB) cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 MmHzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTD22NEhVSiliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkS5JO69VQ>? M1XGUFIyPjJzOEiz
RXF393 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 NXr1[XA1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDSXGY{QTNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMEGg{txO NWj0TGVFOjF4MkG4PFM>
RXF393 cells NVWxcVJHS3m2b4TvfIlkcXS7IHHzd4F6 NFHLSFNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTYEZ|OUOgZ4VtdHNuIFzDOVA:OTVwMzFOwG0> NYjO[216OjF4MkG4PFM>

多くの細胞株試験データを見る場合、クリックしてください

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 順序で溶剤を入れること:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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
別名 NVP-LAQ824

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

Related Antibodies

HDAC信号経路図

HDAC Inhibitors with Unique Features

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Tags: Dacinostat (LAQ824)を買う | Dacinostat (LAQ824) ic50 | Dacinostat (LAQ824)供給者 | Dacinostat (LAQ824)を購入する | Dacinostat (LAQ824)費用 | Dacinostat (LAQ824)生産者 | オーダーDacinostat (LAQ824) | Dacinostat (LAQ824)化学構造 | Dacinostat (LAQ824)分子量 | Dacinostat (LAQ824)代理店
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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