Dacinostat (LAQ824)

Catalog No.S1095 Synonyms: NVP-LAQ824

Dacinostat (LAQ824) Chemical Structure

Molecular Weight(MW): 379.459

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

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In DMSO USD 420 In stock
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Cited by 10 Publications

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  • 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.

  • 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.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Dacinostat (LAQ824) is a novel HDAC inhibitor with IC50 of 32 nM and is known to activate the p21 promoter.
Targets
HDAC [1]
(Cell-free assay)
32 nM
In vitro

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
H1299 NUOyRVNtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUjsdG5XUW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEhzMkm5JIh2dWGwIHz1coch[2G{Y3nuc41iKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMUWg{txO NYm0elY6OTR3MkG0NlI>
HCT116 NFrOdoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnjZTY5pcWKrdH;yfUBi[3Srdnn0fUBi\2GrboP0JGhEXDFzNjDoeY1idiClb3zvckBk\WyuIHfyc5d1cCxiSVO1NF0xNjBzIN88US=> MVexOFUzOTR{Mh?=
HCT116 NV3HXVlyS3m2b4TvfIlkcXS7IHHzd4F6 NV[4b|RbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlA2KM7:TR?= NWm1[ZJ3OTd7NEG2NlU>
human mammary epithelial cells NVHZO4x4S3m2b4TvfIlkcXS7IHHzd4F6 NILHbXNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBu[W2vYYL5JIVxcXSqZXzpZYwh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEh|ryP MonFNVc6PDF4MkW=
HEK293 cells MoHzSpVv[3Srb36gZZN{[Xl? MnvYTY5pcWKrdHnvckBw\iCKRFHDNUBqdiCKRVuyPVMh[2WubIOsJGlEPTB;MD6wNFI3KM7:TR?= MlG0NVg{ODh3NkO=
HeLa cells M131c2Z2dmO2aX;uJIF{e2G7 MlXpNE4{KM7:TR?= NHrZcYUyPiCq MoLsTY5pcWKrdHnvckBw\iCKRFHDOE1u\WSrYYTl[EBz\XC{ZYPzbY9vKG:oIF3FSlIu\GWyZX7k[Y51KHS{YX7zZ5JqeHSrb36gbY4hUGWOYTDj[YxteyCjdDCwMlMhfU1iYX\0[ZIhOTZiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NVXJToZjOTd7NU[5PFg>
HCT116 cells NHfhfYlRem:uaX\ldoF1cW:wIHHzd4F6 M{ThOGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjBzMzFOwG0> MkjsNlAzODV|OUS=
H1299 cells Mn;YVJJwdGmoZYLheIlwdiCjc4PhfS=> NHvYbFJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjF4MTFOwG0> MV:yNFIxPTN7NB?=
H460 cells MmK2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zzcVQ5KGh? MonXS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP NEjaUW4zOTB5M{G2NC=>
HCT116 cells MmrOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVTwT|BYPDhiaB?= NHvKd4xIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> M4L0NFIyODd|MU[w
CCRF-CEM cells M2ToTXBzd2yrZnXyZZRqd25iYYPzZZk> NGXIVW1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFPDVmYuS0WPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK1NUDPxE1? NVrDcZVTOjF4MkG4PFM>
K562 cells M2HUNHBzd2yrZnXyZZRqd25iYYPzZZk> NXzD[41zSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV3IN88US=> NWXHU4xmOjF4MkG4PFM>
MOLT4 cells NWLuc5M2WHKxbHnm[ZJifGmxbjDhd5NigQ>? MoH1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN M{fvTVIyPjJzOEiz
SR cells NXXoV|BFWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIHpUppCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPSJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlk6KM7:TR?= NEi4UoczOTZ{MUi4Ny=>
A549 cells M{PCUnBzd2yrZnXyZZRqd25iYYPzZZk> NVW2eZY6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB7IN88US=> MmiyNlE3OjF6OEO=
EKVX cells M2rxZXBzd2yrZnXyZZRqd25iYYPzZZk> MXvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEWNVmigZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUGuO|Uh|ryP NVjId2ZwOjF4MkG4PFM>
HOP62 cells NUOwdoNCWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoCwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN MWGyNVYzOTh6Mx?=
HOP92 cells M3TJO3Bzd2yrZnXyZZRqd25iYYPzZZk> NYWzXFBqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIU3A6OiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5zOUmg{txO MXWyNVYzOTh6Mx?=
NCI-H226 cells NWLUXGJOWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkTXRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> MoG5NlE3OjF6OEO=
NCI-H23 cells NVjCSFAyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGXPVZpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNTFOwG0> MVOyNVYzOTh6Mx?=
NCI-H322M cells M37Eb3Bzd2yrZnXyZZRqd25iYYPzZZk> NXrPRWtDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDN{Ml2gZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUKuNlYh|ryP MnPaNlE3OjF6OEO=
NCI-H460 cells M1\ud3Bzd2yrZnXyZZRqd25iYYPzZZk> NV6zOpJqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? NHTrRW8zOTZ{MUi4Ny=>
COLO205 cells Mmf3VJJwdGmoZYLheIlwdiCjc4PhfS=> MYfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN M3fhTlIyPjJzOEiz
HCT116 cells M1jl[HBzd2yrZnXyZZRqd25iYYPzZZk> MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN Mm\DNlE3OjF6OEO=
HCT15 cells NVnobW9PWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnvZRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxOUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk4xPyEQvF2= MmPVNlE3OjF6OEO=
HT-29 cells MmfIVJJwdGmoZYLheIlwdiCjc4PhfS=> NIft[ldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV4NjFOwG0> M1vCUFIyPjJzOEiz
KM12 cells NYrBcop4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkjIRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTUGyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlA1KM7:TR?= NHPmdG4zOTZ{MUi4Ny=>
SW620 cells M3zmbHBzd2yrZnXyZZRqd25iYYPzZZk> MkDiRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{[yNEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE41PzhizszN MX:yNVYzOTh6Mx?=
SF268 cells NVmxT|RFWHKxbHnm[ZJifGmxbjDhd5NigQ>? MWLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMk[4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlU{KM7:TR?= Mn3TNlE3OjF6OEO=
SF295 cells M3r4RnBzd2yrZnXyZZRqd25iYYPzZZk> MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOIMkm1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlc1OyEQvF2= MkjINlE3OjF6OEO=
SF539 cells NWLJV2Z1WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3q5RmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> NH;JWXgzOTZ{MUi4Ny=>
SNB19 cells NFnxbJlRem:uaX\ldoF1cW:wIHHzd4F6 M3H0V2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CNVkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN MYiyNVYzOTh6Mx?=
SNB75 cells NH;1PJpRem:uaX\ldoF1cW:wIHHzd4F6 NWr0d|l7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTUmI4PSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|MUig{txO NG\aTpgzOTZ{MUi4Ny=>
U251 cells NHL2eXRRem:uaX\ldoF1cW:wIHHzd4F6 NGHWZmJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWyOVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzd|IN88US=> NFnobnkzOTZ{MUi4Ny=>
LOXIMVI cells M4DVRXBzd2yrZnXyZZRqd25iYYPzZZk> NHPKOoJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO MYCyNVYzOTh6Mx?=
MALME-3M cells M37STXBzd2yrZnXyZZRqd25iYYPzZZk> M3PFc2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? NY\wbnFqOjF4MkG4PFM>
M14 cells NX3rbnF5WHKxbHnm[ZJifGmxbjDhd5NigQ>? MkXYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMUSgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPFQ6KM7:TR?= NYDyeHR4OjF4MkG4PFM>
MDA-MB-435 cells M2rncnBzd2yrZnXyZZRqd25iYYPzZZk> M4fCWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTR|NTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD61N|ch|ryP MlH1NlE3OjF6OEO=
SK-MEL-28 cells MkHSVJJwdGmoZYLheIlwdiCjc4PhfS=> MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE0zQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57OUOg{txO MnzINlE3OjF6OEO=
SK-MEL-5 cells M3zxZXBzd2yrZnXyZZRqd25iYYPzZZk> NEnMVFdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? NF65[|MzOTZ{MUi4Ny=>
UACC257 cells M3TUUXBzd2yrZnXyZZRqd25iYYPzZZk> NIO1dWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NVjzPXRVOjF4MkG4PFM>
UACC62 cells M{nNR3Bzd2yrZnXyZZRqd25iYYPzZZk> MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWDQ1O2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PzlizszN MX2yNVYzOTh6Mx?=
IGROV1 cells M1PMWXBzd2yrZnXyZZRqd25iYYPzZZk> NV7VN3plSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJS3JQXjFiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMUi3JO69VQ>? MWmyNVYzOTh6Mx?=
OVCAR3 cells MkfkVJJwdGmoZYLheIlwdiCjc4PhfS=> M2O2ZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjFzIN88US=> NF32ZoMzOTZ{MUi4Ny=>
OVCAR4 cells NFfP[WxRem:uaX\ldoF1cW:wIHHzd4F6 NF;yV5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Oy5{MTFOwG0> NVfTdYs2OjF4MkG4PFM>
OVCAR5 cells MmXTVJJwdGmoZYLheIlwdiCjc4PhfS=> NUjlc2NKSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwMk[g{txO M1\1UlIyPjJzOEiz
OVCAR8 cells NF\sSYxRem:uaX\ldoF1cW:wIHHzd4F6 NXnEVHJDSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO NGWxNWczOTZ{MUi4Ny=>
NCI/ADR-RES cells M2XZN3Bzd2yrZnXyZZRqd25iYYPzZZk> MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? M2fiOlIyPjJzOEiz
SKOV3 cells MkTyVJJwdGmoZYLheIlwdiCjc4PhfS=> MlLHRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1;WN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42OjRizszN NWPkUZZuOjF4MkG4PFM>
786-0 cells NWX6VplLWHKxbHnm[ZJifGmxbjDhd5NigQ>? NEHnVpFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEe4Ok0xKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjN6IN88US=> MU[yNVYzOTh6Mx?=
A498 cells NH3vZ2RRem:uaX\ldoF1cW:wIHHzd4F6 NHjRTphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG0PVgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvOTFizszN MV6yNVYzOTh6Mx?=
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... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[1]
+ Expand
  • Cell lines: H1299, HCT116, DU145, PC3 and MDA435 cells
  • Concentrations: 0-10 μM
  • Incubation Time: 48 hours
  • Method: 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
  • Formulation: LAQ824 is dissolved in DMSO.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 76 mg/mL (200.28 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 379.459
Formula

C22H25N3O3

CAS No. 404951-53-7
Storage powder
in solvent
Synonyms NVP-LAQ824

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID