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 在庫  
JPY 60474.96 あり
JPY 46076.16 あり
JPY 139668.35 あり

カスタマーフィードバック(4)

  • 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.

  • 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 MmjqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVfqTFVlUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEhzMkm5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMUWg{txO MWixOFUzOTR{Mh?=
HCT116 NF3tVnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2jsVWlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> M{fHblE1PTJzNEKy
HCT116 M4S0dmN6fG:2b4jpZ4l1gSCjc4PhfS=> M1z6V2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wOUDPxE1? NVfEVIJZOTd7NEG2NlU>
human mammary epithelial cells M{LlOmN6fG:2b4jpZ4l1gSCjc4PhfS=> MnP6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? M3PT[FE4QTRzNkK1
HEK293 cells MVHGeY5kfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKEiGQVOxJIlvKEiHS{K5N{Bk\WyuczygTWM2OD1yLkCwNlYh|ryP MWqxPFMxQDV4Mx?=
HeLa cells NUfQNVFnTnWwY4Tpc44h[XO|YYm= MXewMlMh|ryP NH;tTYMyPiCq NGnHR|hKdmirYnn0bY9vKG:oIFjERWM1NW2nZHnheIVlKHKncILld5Nqd25ib3[gUWVHOi2mZYDlcoRmdnRidILhcpNkemmydHnvckBqdiCKZVzhJINmdGy|IHH0JFAvOyC3TTDh[pRmeiBzNjDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NVi5S2pFOTd7NU[5PFg>
HCT116 cells MkPuVJJwdGmoZYLheIlwdiCjc4PhfS=> NGnGV2hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCPVGOgZZN{[XluIFnDOVA:OC5yMUOg{txO NWSzSHZWOjB{MEWzPVQ>
H1299 cells M{fidnBzd2yrZnXyZZRqd25iYYPzZZk> MkfmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN MV[yNFIxPTN7NB?=
H460 cells NX3xTZMyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;jVFk1QCCq Mof2S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP NV\vPW9SOjFyN{OxOlA>
HCT116 cells M2TUUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojMOFghcA>? NFzpVZpIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> NV3Z[YFNOjFyN{OxOlA>
CCRF-CEM cells NYLQ[ItzWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> Mo\rNlE3OjF6OEO=
K562 cells NXzaO241WHKxbHnm[ZJifGmxbjDhd5NigQ>? NXPDdVZpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> NHzIdZUzOTZ{MUi4Ny=>
MOLT4 cells MUDQdo9tcW[ncnH0bY9vKGG|c3H5 M{ixVmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTV;MWFQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzFzIN88US=> NUHMcoNtOjF4MkG4PFM>
SR cells NIrqU2VRem:uaX\ldoF1cW:wIHHzd4F6 Mkj1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVUjDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;Mj65PUDPxE1? MnXBNlE3OjF6OEO=
A549 cells NF3zO41Rem:uaX\ldoF1cW:wIHHzd4F6 NUnFW5dzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB7IN88US=> NHXnU|IzOTZ{MUi4Ny=>
EKVX cells M1zuPHBzd2yrZnXyZZRqd25iYYPzZZk> MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP Mn72NlE3OjF6OEO=
HOP62 cells NF3pRpVRem:uaX\ldoF1cW:wIHHzd4F6 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUE[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlUxOiEQvF2= M3H3WVIyPjJzOEiz
HOP92 cells Ml3mVJJwdGmoZYLheIlwdiCjc4PhfS=> MoO3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C5NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQTlizszN NUj2TnBwOjF4MkG4PFM>
NCI-H226 cells MUTQdo9tcW[ncnH0bY9vKGG|c3H5 M{XaWWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNEGg{txO MnPTNlE3OjF6OEO=
NCI-H23 cells M3uwPXBzd2yrZnXyZZRqd25iYYPzZZk> MmrDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjVizszN NWf0XZh{OjF4MkG4PFM>
NCI-H322M cells NWPJcZptWHKxbHnm[ZJifGmxbjDhd5NigQ>? M322TGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWg{OjKPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1{LkK2JO69VQ>? M3HuTlIyPjJzOEiz
NCI-H460 cells NInXZmlRem:uaX\ldoF1cW:wIHHzd4F6 Ml3iRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> NHq5d|EzOTZ{MUi4Ny=>
COLO205 cells M{\UUXBzd2yrZnXyZZRqd25iYYPzZZk> MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MWiyNVYzOTh6Mx?=
HCT116 cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 NWfGPYQ1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{S3JO69VQ>? MoDJNlE3OjF6OEO=
HCT15 cells NIPHS3ZRem:uaX\ldoF1cW:wIHHzd4F6 NV;GSlNRSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oi5yNzFOwG0> MmTYNlE3OjF6OEO=
HT-29 cells NFyy[41Rem:uaX\ldoF1cW:wIHHzd4F6 NV3nZ|hFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO MV[yNVYzOTh6Mx?=
KM12 cells NH3k[2lRem:uaX\ldoF1cW:wIHHzd4F6 Mn3SRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= MXyyNVYzOTh6Mx?=
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SF268 cells NVnT[WZZWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWm1[ocySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI3QCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> NFm5VFIzOTZ{MUi4Ny=>
SF295 cells NVfhO2tUWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVq2[|ZqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlI6PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55NEOg{txO M3vnS|IyPjJzOEiz
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SNB19 cells NW\3cGloWHKxbHnm[ZJifGmxbjDhd5NigQ>? NX\iT2hpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmIyQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS53MzFOwG0> MlXENlE3OjF6OEO=
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MALME-3M cells M1LJ[3Bzd2yrZnXyZZRqd25iYYPzZZk> MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR4MTFOwG0> MWWyNVYzOTh6Mx?=
M14 cells MoLaVJJwdGmoZYLheIlwdiCjc4PhfS=> NIKzd4hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF2xOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE45PDlizszN NFn1NYEzOTZ{MUi4Ny=>
MDA-MB-435 cells Ml;wVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn;XRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? NXzGe5hIOjF4MkG4PFM>
SK-MEL-28 cells MkfPVJJwdGmoZYLheIlwdiCjc4PhfS=> NWrFTWlbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPVk{KM7:TR?= M1TFVlIyPjJzOEiz
SK-MEL-5 cells NHj4bG5Rem:uaX\ldoF1cW:wIHHzd4F6 M3fXSGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMkexJO69VQ>? M{\SflIyPjJzOEiz
UACC257 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWDQ1OyOVch[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzl|IN88US=> MmXjNlE3OjF6OEO=
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IGROV1 cells NED1WmVRem:uaX\ldoF1cW:wIHHzd4F6 MYnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmJUl;WNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4yQDdizszN NGTJe2QzOTZ{MUi4Ny=>
OVCAR3 cells NFPuVIhRem:uaX\ldoF1cW:wIHHzd4F6 MmrSRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRVlPBVlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN M3;yZlIyPjJzOEiz
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OVCAR5 cells NXzXWFZNWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1XVWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> NXOzb2JZOjF4MkG4PFM>
OVCAR8 cells MVrQdo9tcW[ncnH0bY9vKGG|c3H5 NXTJOnBzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO M2TkcVIyPjJzOEiz
NCI/ADR-RES cells M1\KN3Bzd2yrZnXyZZRqd25iYYPzZZk> MXHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? M1POPFIyPjJzOEiz
SKOV3 cells MnPYVJJwdGmoZYLheIlwdiCjc4PhfS=> NGfFPJRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{NDFOwG0> NVfuNZhyOjF4MkG4PFM>
786-0 cells M{\MZXBzd2yrZnXyZZRqd25iYYPzZZk> MkC4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiB5OE[tNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4{QCEQvF2= MXuyNVYzOTh6Mx?=
A498 cells M2\1ZnBzd2yrZnXyZZRqd25iYYPzZZk> NEH2e2tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN MnvHNlE3OjF6OEO=
ACHN cells NHHLdVdRem:uaX\ldoF1cW:wIHHzd4F6 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEGFSF6gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuNUDPxE1? MYKyNVYzOTh6Mx?=
Caki1 cells MoT6VJJwdGmoZYLheIlwdiCjc4PhfS=> MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOja3mxJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlYyQSEQvF2= NX\MWGpwOjF4MkG4PFM>
SN12C cells MYnQdo9tcW[ncnH0bY9vKGG|c3H5 M4Lad2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU16xNmMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvQTJizszN NXXaeFVKOjF4MkG4PFM>
TK10 cells M2XybHBzd2yrZnXyZZRqd25iYYPzZZk> NIH1WpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTLNVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDR2IN88US=> MUCyNVYzOTh6Mx?=
UO31 cells NWLEb|hFWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWRM{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFUzKM7:TR?= Mn3XNlE3OjF6OEO=
PC3 cells MVzQdo9tcW[ncnH0bY9vKGG|c3H5 NVrzTI1ESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= NUi4[Vh4OjF4MkG4PFM>
DU145 cells NVXSeWJrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NI\admlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zQS57IN88US=> NY\PS2ZbOjF4MkG4PFM>
MCF7 cells NWTkV5dVWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlL3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME22MlkyKM7:TR?= NYfGOGpOOjF4MkG4PFM>
MDA-MB-231 cells MWrQdo9tcW[ncnH0bY9vKGG|c3H5 M13yUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{GuO{DPxE1? NIrYfW4zOTZ{MUi4Ny=>
Hs 578T cells MX7Qdo9tcW[ncnH0bY9vKGG|c3H5 NWXXPJQxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDId{A2PziWIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13LkiyJO69VQ>? M2X2NVIyPjJzOEiz
BT549 cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 M1[1O2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvODRizszN M4n5e|IyPjJzOEiz
T47D cells M2n3W3Bzd2yrZnXyZZRqd25iYYPzZZk> MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFR2N1SgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUK4Mlgh|ryP M4TqTFIyPjJzOEiz
MDA-MB-468 cells M33MNnBzd2yrZnXyZZRqd25iYYPzZZk> NYG1bFhvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME21Mlg5KM7:TR?= MVqyNVYzOTh6Mx?=
NCI-H226 cells MoTIR5l1d3SxeHnjbZR6KGG|c3H5 NETYPIlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBPS0lvSEKyOkBk\WyuczygUGM2OD1{MDFOwG0> M2ey[FIyPjJzOEiz
KM12 cells MXXDfZRwfG:6aXPpeJkh[XO|YYm= MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzMEBNSzVyPUK5Mlkh|ryP NEfwdnMzOTZ{MUi4Ny=>
SF295 cells M2Li[2N6fG:2b4jpZ4l1gSCjc4PhfS=> NFTFO3JEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUTjJ7NTDj[YxteyxiTFO1NF03NjlzIN88US=> NYLDcI5EOjF4MkG4PFM>
SNB19 cells NF\nfZpEgXSxdH;4bYNqfHliYYPzZZk> MoXuR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV25DOTliY3XscJMtKEyFNUC9N|EvPyEQvF2= M2LWZ|IyPjJzOEiz
U251 cells NYfNXmpMS3m2b4TvfIlkcXS7IHHzd4F6 MXfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzMEBNSzVyPUWuPFIh|ryP NY\lUnJPOjF4MkG4PFM>
LOXIMVI cells MULDfZRwfG:6aXPpeJkh[XO|YYm= MmnFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG9ZUU2YSTDj[YxteyxiTFO1NF03NjB2IN88US=> MVOyNVYzOTh6Mx?=
MDA-MB-435 cells NG\abWVEgXSxdH;4bYNqfHliYYPzZZk> NXLqOpRrS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ{PSClZXzsd{whVEN3ME2yPE45KM7:TR?= NUXxWIpiOjF4MkG4PFM>
SK-MEL-28 cells NYflNGNXS3m2b4TvfIlkcXS7IHHzd4F6 MmS3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2suVUWOLUK4JINmdGy|LDDMR|UxRTNzLkmg{txO NX:0Vo5LOjF4MkG4PFM>
SK-MEL-5 cells MVfDfZRwfG:6aXPpeJkh[XO|YYm= MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyxiTFO1NF01NjB{IN88US=> M1L2O|IyPjJzOEiz
UACC257 cells M2\C[GN6fG:2b4jpZ4l1gSCjc4PhfS=> NICwdlFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBWSUOFMkW3JINmdGy|LDDMR|UxRTR2Lkig{txO M{noT|IyPjJzOEiz
UACC62 cells M3f2VGN6fG:2b4jpZ4l1gSCjc4PhfS=> M2CxZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHVCS0N4MjDj[YxteyxiTFO1NF03NjN7IN88US=> NYr2W|V3OjF4MkG4PFM>
IGROV1 cells NVe4cnI5S3m2b4TvfIlkcXS7IHHzd4F6 MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMtKEyFNUC9OFgvQSEQvF2= MmXVNlE3OjF6OEO=
OVCAR5 cells MmHpR5l1d3SxeHnjbZR6KGG|c3H5 M333S2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG9XS0GUNTDj[YxteyxiTFO1NF0{QC57IN88US=> MkjhNlE3OjF6OEO=
SKOV3 cells NXLr[21KS3m2b4TvfIlkcXS7IHHzd4F6 NVfNNo41S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0uRVkOgZ4VtdHNuIFzDOVA:OjhwNTFOwG0> NYPmPINtOjF4MkG4PFM>
A498 cells NF\S[WZEgXSxdH;4bYNqfHliYYPzZZk> NX\0ZnpIS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTR7ODDj[YxteyxiTFO1NF02Njh6IN88US=> MlSzNlE3OjF6OEO=
Caki1 cells MWrDfZRwfG:6aXPpeJkh[XO|YYm= NUDMb2tUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS2GtaUGgZ4VtdHNuIFzDOVA:PS55OTFOwG0> MXqyNVYzOTh6Mx?=
HCT116 cells MnXtVJJwdGmoZYLheIlwdiCjc4PhfS=> M{WwdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzMEBKSzVyPUCuNFE6KM7:TR?= M1uxRlIyPzR{NEm2
HCT116 cells Mmq0VJJwdGmoZYLheIlwdiCjc4PhfS=> M1jSXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGe{b4f0bEBqdmirYnn0bY9vNCCLQ{WwQVAvODF7IN88US=> MkjCNlE3PTB{MkG=
H1299 cells Mk\oVJJwdGmoZYLheIlwdiCjc4PhfS=> NITt[lNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzMEBKSzVyPUCuNUDPxE1? MW[yNVY2ODJ{MR?=
HCT116 cells M{XidXBzd2yrZnXyZZRqd25iYYPzZZk> MonZTY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiSFPUNVE3KGOnbHzzJJBzd2yrZnXyZZRqd25uIFnDOVA:OC5yMTFOwG0> NV:xOY1SOTR4MUOzNVI>
RPMI8226 cells NEXFSJhRem:uaX\ldoF1cW:wIHHzd4F6 M2n4ZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUmDNTVgzOjZiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNUKzJO69VQ>? M4fxRlIyPjJzOEiz
CHO cells NFX2eVNHfW6ldHnvckBie3OjeR?= M4jSNmlvcGmkaYTpc44hd2ZiaIXtZY4hTVKJIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliYYX0c41ifGWmIIDheINpKGOuYX3wJIVt\WO2cn;wbJl{cW:ub3f5JIF{e2G7LDDJR|UxRTF{LkKg{txO M2i5dVIxOjB3M{m0
HL-60(TB) cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 M3r2SWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFytOlApXEJrIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK0PUDPxE1? MU[yNVYzOTh6Mx?=
RXF393 cells NFe0O3ZRem:uaX\ldoF1cW:wIHHzd4F6 MlK4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUWF[zPVMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvODFizszN M1[3NVIyPjJzOEiz
RXF393 cells NH61[XNEgXSxdH;4bYNqfHliYYPzZZk> M{H0dmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHJZTjN7MzDj[YxteyxiTFO1NF0yPS5|IN88US=> MX[yNVYzOTh6Mx?=

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
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

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

HDAC信号経路図

HDAC Inhibitors with Unique Features

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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