Dacinostat (LAQ824)

Catalog No.S1095 Synonyms: NVP-LAQ824

For research use only.

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

Dacinostat (LAQ824) Chemical Structure

CAS No. 404951-53-7

Selleck's Dacinostat (LAQ824) has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description Dacinostat (LAQ824, NVP-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 M1rabWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWLJcohq[mm2b4L5JIFkfGm4aYT5JIFo[Wmwc4SgTFEzQTliaIXtZY4hdHWwZzDjZZJkcW6xbXGgZ4VtdCCpcn;3eIgtKEmFNUC9NE4yPSEQvF2= NWP3N|NFOTR3MkG0NlI>
HCT116 NIjKdmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnETVdKdmirYnn0c5J6KGGldHn2bZR6KGGpYXnud5QhUEOWMUG2JIh2dWGwIHPvcI9vKGOnbHyg[5Jwf3SqLDDJR|UxRTBwMEGg{txO NUfPc3hlOTR3MkG0NlI>
HCT116 NHr1dm1EgXSxdH;4bYNqfHliYYPzZZk> NHHWNmhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP NYLZeZBrOTd7NEG2NlU>
human mammary epithelial cells NF;rRo5EgXSxdH;4bYNqfHliYYPzZZk> MoPSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gcYFudWG{eTDldIl1cGWuaXHsJINmdGy|IHL5JG1VXCCjc4PhfUwhUUN3ME2xJO69VQ>? NUi3SWFGOTd7NEG2NlU>
HEK293 cells M1XqOWZ2dmO2aX;uJIF{e2G7 M4rHeGlvcGmkaYTpc44hd2ZiSFTBR|EhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUCuNFAzPiEQvF2= Mn\zNVg{ODh3NkO=
HeLa cells Mo[5SpVv[3Srb36gZZN{[Xl? NWXqZpN2OC5|IN88US=> M4\5bVE3KGh? NWPqToNjUW6qaXLpeIlwdiCxZjDISGFEPC2vZXTpZZRm\CC{ZYDy[ZN{cW:wIH;mJG1GTjJvZHXw[Y5l\W62IITyZY5{[3KrcITpc44hcW5iSHXMZUBk\WyuczDheEAxNjNidV2gZYZ1\XJiMU[gbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MX[xO|k2Pjl6OB?=
HCT116 cells NFXySGRRem:uaX\ldoF1cW:wIHHzd4F6 MlG2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZpkhVVSVIHHzd4F6NCCLQ{WwQVAvODF|IN88US=> NHG0RmgzODJyNUO5OC=>
H1299 cells MlPIVJJwdGmoZYLheIlwdiCjc4PhfS=> NHPhNG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFixNlk6KGOnbHzzJIJ6KE2WUzDhd5NigSxiSVO1NF0xNjF4MTFOwG0> NVTCSm9XOjB{MEWzPVQ>
H460 cells Mnf0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\OOFghcA>? MXnHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIOFYxKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDTVmIh[XO|YYmsJGlEPTB;MD6wO{DPxE1? NGjEO2YzOTB5M{G2NC=>
HCT116 cells NH7UOm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnP6OFghcA>? NX\RVYIxT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCVUlKgZZN{[XluIFnDOVA:OC5yMUig{txO MkDINlExPzNzNkC=
CCRF-CEM cells NUL3W5FlWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnXyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFQ2LGMWNGVSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NUGg{txO M3vZZVIyPjJzOEiz
K562 cells Mn7rVJJwdGmoZYLheIlwdiCjc4PhfS=> NIDaWZJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTVizszN Mmm3NlE3OjF6OEO=
MOLT4 cells NGLHRVBRem:uaX\ldoF1cW:wIHHzd4F6 MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2RTGS0JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyOSEQvF2= MmDINlE3OjF6OEO=
SR cells NXLoZpByWHKxbHnm[ZJifGmxbjDhd5NigQ>? NULwRlN1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTVkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk46QSEQvF2= MUGyNVYzOTh6Mx?=
A549 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 NFn0b5dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODlizszN NEH1SFAzOTZ{MUi4Ny=>
EKVX cells NW\uNnB5WHKxbHnm[ZJifGmxbjDhd5NigQ>? M2HLT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRVvWXEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU44PSEQvF2= M376W|IyPjJzOEiz
HOP62 cells NVfKUIhjWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlrjRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKT2C2NkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE42ODJizszN MojuNlE3OjF6OEO=
HOP92 cells M3rxO3Bzd2yrZnXyZZRqd25iYYPzZZk> MWrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiRUEmyJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlE6QSEQvF2= MXOyNVYzOTh6Mx?=
NCI-H226 cells NGHwVFFRem:uaX\ldoF1cW:wIHHzd4F6 NFnPZ4lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjJ4IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkSxJO69VQ>? MUSyNVYzOTh6Mx?=
NCI-H23 cells Mn7sVJJwdGmoZYLheIlwdiCjc4PhfS=> NEXiVZdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOjNiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwNTFOwG0> NUi1WYQ1OjF4MkG4PFM>
NCI-H322M cells NVHlS5RiWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn3IRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO NG[1eWEzOTZ{MUi4Ny=>
NCI-H460 cells MmjyVJJwdGmoZYLheIlwdiCjc4PhfS=> NVf6WWY4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDR4MDDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD63JO69VQ>? NUD5PJBJOjF4MkG4PFM>
COLO205 cells NH\XdoZRem:uaX\ldoF1cW:wIHHzd4F6 NUW5fHpCSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? NE\NNGgzOTZ{MUi4Ny=>
HCT116 cells NWPrS5Q2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NGfhU|BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5|NEeg{txO MonVNlE3OjF6OEO=
HCT15 cells MojoVJJwdGmoZYLheIlwdiCjc4PhfS=> M1yzeWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvODdizszN NXvwd28{OjF4MkG4PFM>
HT-29 cells M3HsSHBzd2yrZnXyZZRqd25iYYPzZZk> M2eze2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTZ4IN88US=> NF;LWGMzOTZ{MUi4Ny=>
KM12 cells NYrLepY5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NETVTmRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODRizszN MV6yNVYzOTh6Mx?=
SW620 cells NV;UWnBXWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1jBW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDd6IN88US=> Mn7hNlE3OjF6OEO=
SF268 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 Mkn2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkK2PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= MXuyNVYzOTh6Mx?=
SF295 cells NYXKUJprWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGO5bGZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGNlk2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd2MzFOwG0> NIPXVIwzOTZ{MUi4Ny=>
SF539 cells M1XSZXBzd2yrZnXyZZRqd25iYYPzZZk> NH\sfZVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPGOVM6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjl4NTFOwG0> MYmyNVYzOTh6Mx?=
SNB19 cells MnrnVJJwdGmoZYLheIlwdiCjc4PhfS=> MkXLRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVTlKxPUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU42OyEQvF2= M4TqOVIyPjJzOEiz
SNB75 cells Mo\qVJJwdGmoZYLheIlwdiCjc4PhfS=> MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOQQke1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlMyQCEQvF2= MYSyNVYzOTh6Mx?=
U251 cells M4D3VXBzd2yrZnXyZZRqd25iYYPzZZk> NXXXNIdSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> MljGNlE3OjF6OEO=
LOXIMVI cells MomwVJJwdGmoZYLheIlwdiCjc4PhfS=> MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyRWFnNWmkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvODhizszN MmrrNlE3OjF6OEO=
MALME-3M cells NXv2fI9XWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4rqd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVHMUWUuO01iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNE[xJO69VQ>? MX6yNVYzOTh6Mx?=
M14 cells MWLQdo9tcW[ncnH0bY9vKGG|c3H5 NWPFVVhWSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNNVQh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQDR7IN88US=> NIDNR2ozOTZ{MUi4Ny=>
MDA-MB-435 cells NHTifY5Rem:uaX\ldoF1cW:wIHHzd4F6 MkmyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDN3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkWzO{DPxE1? MoP4NlE3OjF6OEO=
SK-MEL-28 cells NU\zdHRyWHKxbHnm[ZJifGmxbjDhd5NigQ>? MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE0zQCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC57OUOg{txO M3S5[FIyPjJzOEiz
SK-MEL-5 cells MnzJVJJwdGmoZYLheIlwdiCjc4PhfS=> NIrQb4dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC13IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkK3NUDPxE1? MY[yNVYzOTh6Mx?=
UACC257 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 NF:wRWFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? NUjQVpBEOjF4MkG4PFM>
UACC62 cells NXj5[I4xWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnP0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> MY[yNVYzOTh6Mx?=
IGROV1 cells NFewT25Rem:uaX\ldoF1cW:wIHHzd4F6 M4n5fGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSVfSU3YyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF6NzFOwG0> Mn[5NlE3OjF6OEO=
OVCAR3 cells M3G4cHBzd2yrZnXyZZRqd25iYYPzZZk> NHrV[oZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> MkmxNlE3OjF6OEO=
OVCAR4 cells M2PYcnBzd2yrZnXyZZRqd25iYYPzZZk> MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:YQ1HSOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9N{4zOSEQvF2= NIPnboEzOTZ{MUi4Ny=>
OVCAR5 cells NIC0SFFRem:uaX\ldoF1cW:wIHHzd4F6 NFLoUVhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC5{NjFOwG0> NWnuXo5xOjF4MkG4PFM>
OVCAR8 cells M3HPRXBzd2yrZnXyZZRqd25iYYPzZZk> M2DodmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI5KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3IN88US=> NUO5PVJTOjF4MkG4PFM>
NCI/ADR-RES cells NUnifWEyWHKxbHnm[ZJifGmxbjDhd5NigQ>? M3eySmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJM2FFWi2URWOgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuNVgh|ryP Mk\WNlE3OjF6OEO=
SKOV3 cells M3SxTnBzd2yrZnXyZZRqd25iYYPzZZk> M2jDe2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1vPWlMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPTJ2IN88US=> MkLTNlE3OjF6OEO=
786-0 cells MkTjVJJwdGmoZYLheIlwdiCjc4PhfS=> NFjOSFRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIEe4Ok0xKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0zNjN6IN88US=> NXn5[2JqOjF4MkG4PFM>
A498 cells NWLlb41EWHKxbHnm[ZJifGmxbjDhd5NigQ>? MoLTRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNEm4JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEyKM7:TR?= MnvQNlE3OjF6OEO=
ACHN cells NX3IfIVqWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlvxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDQ1jOJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEh|ryP MmXrNlE3OjF6OEO=
Caki1 cells M2O0NnBzd2yrZnXyZZRqd25iYYPzZZk> MmjPRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFYXvpNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE43OTlizszN M{C3TVIyPjJzOEiz
SN12C cells MkHFVJJwdGmoZYLheIlwdiCjc4PhfS=> M4TDd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU16xNmMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvQTJizszN NVruWmVrOjF4MkG4PFM>
TK10 cells NVv6cFBlWHKxbHnm[ZJifGmxbjDhd5NigQ>? NY\YTJVJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDUT|ExKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR2NDFOwG0> MUKyNVYzOTh6Mx?=
UO31 cells NFvmd2hRem:uaX\ldoF1cW:wIHHzd4F6 NV\Tb2pQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVU|MyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjR3MjFOwG0> NFHBdZIzOTZ{MUi4Ny=>
PC3 cells Mk[wVJJwdGmoZYLheIlwdiCjc4PhfS=> NU[yVnFXSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIxKM7:TR?= M3S3PVIyPjJzOEiz
DU145 cells NYLYVJNsWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKESXMUS1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yPU46KM7:TR?= MXmyNVYzOTh6Mx?=
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MDA-MB-231 cells NE\IZXNRem:uaX\ldoF1cW:wIHHzd4F6 M{TGZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVTBMW1DNTJ|MTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{GuO{DPxE1? M4fPVlIyPjJzOEiz
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HCT116 cells NIPHVWVRem:uaX\ldoF1cW:wIHHzd4F6 MnLORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOsJGlEPTB;MD6wNVkh|ryP Mn:3NlE4PDJ2OU[=
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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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: HCT116 cells is injected s.c. into the right axillary (lateral) region of outbred athymic (nu/nu) female mice.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via i.v.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 379.459
Formula

C22H25N3O3

CAS No. 404951-53-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

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