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 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfQ[JlKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUDF{OUmgbJVu[W5ibIXu[{Bk[XKlaX7vcYEh[2WubDDndo94fGhuIFnDOVA:OC5zNTFOwG0> MWmxOFUzOTR{Mh?=
HCT116 NHfhRlBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vWS2lvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> MV:xOFUzOTR{Mh?=
HCT116 MmjRR5l1d3SxeHnjbZR6KGG|c3H5 NV35NpIzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= MojwNVc6PDF4MkW=
human mammary epithelial cells MVnDfZRwfG:6aXPpeJkh[XO|YYm= NGrnZnNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP NWmzfm9MOTd7NEG2NlU>
HEK293 cells MYLGeY5kfGmxbjDhd5NigQ>? M4Ts[2lvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= MkfzNVg{ODh3NkO=
HeLa cells MYTGeY5kfGmxbjDhd5NigQ>? M2jzXlAvOyEQvF2= NFLpOnIyPiCq MYXJcohq[mm2aX;uJI9nKEiGQVO0MY1m\GmjdHXkJJJmeHKnc4Ppc44hd2ZiTVXGNk1l\XCnbnTlcpQhfHKjboPjdolxfGmxbjDpckBJ\UyjIHPlcIx{KGG2IECuN{B2VSCjZoTldkAyPiCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7 NHjmfnMyPzl3Nkm4PC=>
HCT116 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4xOTNizszN M32yflIxOjB3M{m0
H1299 cells MoHoVJJwdGmoZYLheIlwdiCjc4PhfS=> MknIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN NI\jPWgzODJyNUO5OC=>
H460 cells M3vJdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jDVlQ5KGh? NITWV5pIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJPDZyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xPyEQvF2= M1\yU|IyODd|MU[w
HCT116 cells M1r5XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfOOFghcA>? MnHpS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFQ5KGi{czDifUBUWkJiYYPzZZktKEmFNUC9NE4xOThizszN NIT0XHozOTB5M{G2NC=>
CCRF-CEM cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 MlfIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQ2LGMWNGVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NUGg{txO NHrrVpQzOTZ{MUi4Ny=>
K562 cells NGfZeGVRem:uaX\ldoF1cW:wIHHzd4F6 NFe3ZmhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTVizszN NXXwRpVROjF4MkG4PFM>
MOLT4 cells NWnabod7WHKxbHnm[ZJifGmxbjDhd5NigQ>? MoXaRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN MlfqNlE3OjF6OEO=
SR cells MoH3VJJwdGmoZYLheIlwdiCjc4PhfS=> Ml\wRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj65PUDPxE1? NHKzPVUzOTZ{MUi4Ny=>
A549 cells NH\LOVJRem:uaX\ldoF1cW:wIHHzd4F6 M3W2fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= MmCxNlE3OjF6OEO=
EKVX cells NWPHNJdPWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmDxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCHS2\YJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlc2KM7:TR?= NE\iOYUzOTZ{MUi4Ny=>
HOP62 cells NXWyOFY3WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlvNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN Mm\oNlE3OjF6OEO=
HOP92 cells NH;xUolRem:uaX\ldoF1cW:wIHHzd4F6 NF3nOnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFkzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF7OTFOwG0> NGe3N2wzOTZ{MUi4Ny=>
NCI-H226 cells NIfiUGpRem:uaX\ldoF1cW:wIHHzd4F6 MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlI3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjRzIN88US=> MlHUNlE3OjF6OEO=
NCI-H23 cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 MlLJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN MY[yNVYzOTh6Mx?=
NCI-H322M cells M1r1dHBzd2yrZnXyZZRqd25iYYPzZZk> M3jDOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OjKPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{LkK2JO69VQ>? MmPlNlE3OjF6OEO=
NCI-H460 cells Mm\nVJJwdGmoZYLheIlwdiCjc4PhfS=> MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IOFYxKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjdizszN MUCyNVYzOTh6Mx?=
COLO205 cells MmjqVJJwdGmoZYLheIlwdiCjc4PhfS=> MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MVuyNVYzOTh6Mx?=
HCT116 cells M17NWnBzd2yrZnXyZZRqd25iYYPzZZk> M3j2TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN2NzFOwG0> M{nZeFIyPjJzOEiz
HCT15 cells MoHPVJJwdGmoZYLheIlwdiCjc4PhfS=> NWHrTZIySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> NVrMO5RXOjF4MkG4PFM>
HT-29 cells MlLEVJJwdGmoZYLheIlwdiCjc4PhfS=> NVPXPJp2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO M1T2XFIyPjJzOEiz
KM12 cells NWC1NlZHWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkLMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= MnfENlE3OjF6OEO=
SW620 cells NXPqSoI5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NIrDcWtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOlIxKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR5ODFOwG0> MXKyNVYzOTh6Mx?=
SF268 cells NH;4TotRem:uaX\ldoF1cW:wIHHzd4F6 MnexRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK2PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= MoXkNlE3OjF6OEO=
SF295 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NVPTNlJ{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO MVGyNVYzOTh6Mx?=
SF539 cells M1XwZnBzd2yrZnXyZZRqd25iYYPzZZk> M3XaPGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> MVKyNVYzOTh6Mx?=
SNB19 cells M4myeXBzd2yrZnXyZZRqd25iYYPzZZk> NInBWohCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPORlE6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjV|IN88US=> MVmyNVYzOTh6Mx?=
SNB75 cells M1HyPXBzd2yrZnXyZZRqd25iYYPzZZk> M3XU[mFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> Mn23NlE3OjF6OEO=
U251 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV{NUGgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuO|c{KM7:TR?= MV2yNVYzOTh6Mx?=
LOXIMVI cells NYna[2t3WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkTxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOT2jJUXZKKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB6IN88US=> NF:3fo0zOTZ{MUi4Ny=>
MALME-3M cells NYWxPGtJWHKxbHnm[ZJifGmxbjDhd5NigQ>? NX:wPY9OSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNRWxOTS1|TTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD60OlEh|ryP MmOzNlE3OjF6OEO=
M14 cells NEjC[2lRem:uaX\ldoF1cW:wIHHzd4F6 NUTTdlF{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNNVQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQDR7IN88US=> MlT1NlE3OjF6OEO=
MDA-MB-435 cells NVrnNHU1WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2r5bGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP NF;BXGUzOTZ{MUi4Ny=>
SK-MEL-28 cells MmHUVJJwdGmoZYLheIlwdiCjc4PhfS=> M3zXWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkm5N{DPxE1? NF3WbXkzOTZ{MUi4Ny=>
SK-MEL-5 cells M2S2NXBzd2yrZnXyZZRqd25iYYPzZZk> MkfKRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVSz3NSWwuPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{N{Gg{txO M160eFIyPjJzOEiz
UACC257 cells NIm0cGdRem:uaX\ldoF1cW:wIHHzd4F6 NGjufJlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? MWiyNVYzOTh6Mx?=
UACC62 cells NGXCdGRRem:uaX\ldoF1cW:wIHHzd4F6 M3jSTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVVHDR|YzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjN5OTFOwG0> MVSyNVYzOTh6Mx?=
IGROV1 cells MlzaVJJwdGmoZYLheIlwdiCjc4PhfS=> MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN MmD6NlE3OjF6OEO=
OVCAR3 cells M2q5XHBzd2yrZnXyZZRqd25iYYPzZZk> MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= MYmyNVYzOTh6Mx?=
OVCAR4 cells NHqwZ|ZRem:uaX\ldoF1cW:wIHHzd4F6 NIixe5ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> NHjsS48zOTZ{MUi4Ny=>
OVCAR5 cells NWnFTY14WHKxbHnm[ZJifGmxbjDhd5NigQ>? MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4zPiEQvF2= NVPjTo1rOjF4MkG4PFM>
OVCAR8 cells M4jzbnBzd2yrZnXyZZRqd25iYYPzZZk> NGDRUG1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC52NTFOwG0> NXXQUVgxOjF4MkG4PFM>
NCI/ADR-RES cells MlXNVJJwdGmoZYLheIlwdiCjc4PhfS=> NYGydXA1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kwSUSULWLFV{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQCEQvF2= MomyNlE3OjF6OEO=
SKOV3 cells NWTHflJuWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3TVcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> MnH3NlE3OjF6OEO=
786-0 cells M17wV3Bzd2yrZnXyZZRqd25iYYPzZZk> NU[4RZZkSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjC3PFYuOCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5|ODFOwG0> MV[yNVYzOTh6Mx?=
A498 cells M3nVbnBzd2yrZnXyZZRqd25iYYPzZZk> MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF2OUigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNVEh|ryP NEfwVIIzOTZ{MUi4Ny=>
ACHN cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NWXIPVhTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBR2hPKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFizszN NXv0XWp5OjF4MkG4PFM>
Caki1 cells MXLQdo9tcW[ncnH0bY9vKGG|c3H5 NF:1O5lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPhb4kyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjZzOTFOwG0> NYjJc2ZXOjF4MkG4PFM>
SN12C cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQMULDJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2zMlkzKM7:TR?= NGixNnUzOTZ{MUi4Ny=>
TK10 cells NHXRPXdRem:uaX\ldoF1cW:wIHHzd4F6 NYnzbY8{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> MUCyNVYzOTh6Mx?=
UO31 cells NV3Ib2U1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWRM{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFUzKM7:TR?= MV[yNVYzOTh6Mx?=
PC3 cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 MUDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MkCg{txO NFPrSmgzOTZ{MUi4Ny=>
DU145 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 M3POWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI6NjlizszN M4LhWFIyPjJzOEiz
MCF7 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 NUDP[WxmSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF03NjlzIN88US=> MYSyNVYzOTh6Mx?=
MDA-MB-231 cells M171[3Bzd2yrZnXyZZRqd25iYYPzZZk> MoTIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1|MT63JO69VQ>? MYWyNVYzOTh6Mx?=
Hs 578T cells M2G2OnBzd2yrZnXyZZRqd25iYYPzZZk> NWGwVGxKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDId{A2PziWIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13LkiyJO69VQ>? M3;Wd|IyPjJzOEiz
BT549 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 Mm\FRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEVEW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok4xPCEQvF2= MYOyNVYzOTh6Mx?=
T47D cells MoDtVJJwdGmoZYLheIlwdiCjc4PhfS=> MYXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUK4Mlgh|ryP NHPVWmczOTZ{MUi4Ny=>
MDA-MB-468 cells NIfWUmVRem:uaX\ldoF1cW:wIHHzd4F6 NVnico43SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= MYSyNVYzOTh6Mx?=
NCI-H226 cells M2\CVGN6fG:2b4jpZ4l1gSCjc4PhfS=> NIHEb4lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> NHixNIQzOTZ{MUi4Ny=>
KM12 cells NEf4VXhEgXSxdH;4bYNqfHliYYPzZZk> Mn7BR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT20yOiClZXzsd{whVEN3ME2yPU46KM7:TR?= MVGyNVYzOTh6Mx?=
SF295 cells MXvDfZRwfG:6aXPpeJkh[XO|YYm= Mn3JR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= NEHSPVIzOTZ{MUi4Ny=>
SNB19 cells MlzyR5l1d3SxeHnjbZR6KGG|c3H5 NHfY[JpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUVkJzOTDj[YxteyxiTFO1NF0{OS55IN88US=> Mkf5NlE3OjF6OEO=
U251 cells NYPNVG8yS3m2b4TvfIlkcXS7IHHzd4F6 NFjEXpBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWOjVzIHPlcIx{NCCOQ{WwQVUvQDJizszN MUWyNVYzOTh6Mx?=
LOXIMVI cells M3[wZWN6fG:2b4jpZ4l1gSCjc4PhfS=> NWPqZXR5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVE:[SV3WTUBk\WyuczygUGM2OD14LkC0JO69VQ>? MmfaNlE3OjF6OEO=
MDA-MB-435 cells NFrTSVFEgXSxdH;4bYNqfHliYYPzZZk> M3zpU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20N|Uh[2WubIOsJGxEPTB;MkiuPEDPxE1? M4nwe|IyPjJzOEiz
SK-MEL-28 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= M1nF[2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU2HTD2yPEBk\WyuczygUGM2OD1|MT65JO69VQ>? M1j1UFIyPjJzOEiz
SK-MEL-5 cells MYrDfZRwfG:6aXPpeJkh[XO|YYm= NIHqboZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2PRVytOUBk\WyuczygUGM2OD12LkCyJO69VQ>? M4rsXVIyPjJzOEiz
UACC257 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= NWDDVFhMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{K1O{Bk\WyuczygUGM2OD12ND64JO69VQ>? MVeyNVYzOTh6Mx?=
UACC62 cells M{n0N2N6fG:2b4jpZ4l1gSCjc4PhfS=> NUe3TnNIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hXUGFQ{[yJINmdGy|LDDMR|UxRTZwM{mg{txO MkL4NlE3OjF6OEO=
IGROV1 cells M1TjS2N6fG:2b4jpZ4l1gSCjc4PhfS=> MXjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= MYWyNVYzOTh6Mx?=
OVCAR5 cells NFTsZZFEgXSxdH;4bYNqfHliYYPzZZk> M37XNWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUNTDj[YxteyxiTFO1NF0{QC57IN88US=> Mo[zNlE3OjF6OEO=
SKOV3 cells NFP2OndEgXSxdH;4bYNqfHliYYPzZZk> MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT29XOyClZXzsd{whVEN3ME2yPE42KM7:TR?= MUeyNVYzOTh6Mx?=
A498 cells Mn7tR5l1d3SxeHnjbZR6KGG|c3H5 M1TPXWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE1QThiY3XscJMtKEyFNUC9OU45QCEQvF2= NXricFFNOjF4MkG4PFM>
Caki1 cells Mn\kR5l1d3SxeHnjbZR6KGG|c3H5 M4XtUmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNic2lzIHPlcIx{NCCOQ{WwQVUvPzlizszN M4PjNFIyPjJzOEiz
HCT116 cells MoC3VJJwdGmoZYLheIlwdiCjc4PhfS=> MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczygTWM2OD1yLkCxPUDPxE1? NYjaSJk5OjF5NEK0PVY>
HCT116 cells MWPQdo9tcW[ncnH0bY9vKGG|c3H5 M4D1d2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> M{H4OlIyPjVyMkKx
H1299 cells MWDQdo9tcW[ncnH0bY9vKGG|c3H5 MlLiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczygTWM2OD1yLkGg{txO NGjF[FczOTZ3MEKyNS=>
HCT116 cells MnjrVJJwdGmoZYLheIlwdiCjc4PhfS=> MnPhTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> MXKxOFYyOzNzMh?=
RPMI8226 cells NYrCSG5JWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4TVV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? MYKyNVYzOTh6Mx?=
CHO cells NHrvXG5HfW6ldHnvckBie3OjeR?= NX[xVoh3UW6qaXLpeIlwdiCxZjDoeY1idiCHUleg[ZhxemW|c3XkJIlvKEOKTzDj[YxteyCkeTDheZRwdWG2ZXSgdIF1[2hiY3zhcZAh\WynY4Tyc5BpgXOrb3zv[5kh[XO|YYmsJGlEPTB;MUKuNkDPxE1? Ml3vNlAzODV|OUS=
HL-60(TB) cells MnHYVJJwdGmoZYLheIlwdiCjc4PhfS=> MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiOLU[wLHRDMSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NEmg{txO NV\xS|RmOjF4MkG4PFM>
RXF393 cells M37LbHBzd2yrZnXyZZRqd25iYYPzZZk> NH:3SYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLYSlM6OyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5yMTFOwG0> NYfwNll2OjF4MkG4PFM>
RXF393 cells MlP4R5l1d3SxeHnjbZR6KGG|c3H5 NH\KZnJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBTYEZ|OUOgZ4VtdHNuIFzDOVA:OTVwMzFOwG0> MkjDNlE3OjF6OEO=

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

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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大阪市内で「G20サミット」が開催されることに伴い、大阪府内で大規模な交通規制が行われる影響で、6月26日(水)から7月1日(月)までの間、下記地域へ出荷が行えなくなります。
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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