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 18 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 NH;Od|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3fjbGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJOTJ7OTDoeY1idiCudX7nJINiemOrbn;tZUBk\WyuIHfyc5d1cCxiSVO1NF0xNjF3IN88US=> MY[xOFUzOTR{Mh?=
HCT116 NV;ySnI2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4DZVGlvcGmkaYTvdpkh[WO2aY\peJkh[WejaX7zeEBJS1RzMU[gbJVu[W5iY3;sc44h[2WubDDndo94fGhuIFnDOVA:OC5yMTFOwG0> M4X2T|E1PTJzNEKy
HCT116 Mlu5R5l1d3SxeHnjbZR6KGG|c3H5 NEjOO5ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYomgUXRVKGG|c3H5MEBKSzVyPUCuNFUh|ryP NXLoO4RqOTd7NEG2NlU>
human mammary epithelial cells MlvyR5l1d3SxeHnjbZR6KGG|c3H5 M1TkRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJI1idW2jcomg[ZBqfGinbHnhcEBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9NUDPxE1? NF;JPYoyPzl2MU[yOS=>
HEK293 cells NGDucnFHfW6ldHnvckBie3OjeR?= NWnXbmE6UW6qaXLpeIlwdiCxZjDISGFEOSCrbjDISWszQTNiY3XscJMtKEmFNUC9NE4xODJ4IN88US=> MVKxPFMxQDV4Mx?=
HeLa cells M4fr[WZ2dmO2aX;uJIF{e2G7 NEjYSWkxNjNizszN MmTFNVYhcA>? M4noemlvcGmkaYTpc44hd2ZiSFTBR|QudWWmaXH0[YQhemWycnXzd4lwdiCxZjDNSWYzNWSncHXu[IVvfCC2cnHud4NzcXC2aX;uJIlvKEinTHGgZ4VtdHNiYYSgNE4{KHWPIHHmeIVzKDF4IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= M1i1dlE4QTV4OUi4
HCT116 cells M4rueXBzd2yrZnXyZZRqd25iYYPzZZk> NVW4c|JuSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliTWTTJIF{e2G7LDDJR|UxRTBwMEGzJO69VQ>? NEf3UYIzODJyNUO5OC=>
H1299 cells MUfQdo9tcW[ncnH0bY9vKGG|c3H5 MnfxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKMUK5PUBk\WyuczDifUBOXFNiYYPzZZktKEmFNUC9NE4yPjFizszN MmXkNlAzODV|OUS=
H460 cells MlLMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWG0PEBp Ml\0S5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTFQ3OCClZXzsd{Bi\nSncjC0PEBpenNiYomgV3JDKGG|c3H5MEBKSzVyPUCuNFch|ryP NIPKeVMzOTB5M{G2NC=>
HCT116 cells MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLnfIQ1PDhiaB?= NInZO4xIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KFOUQjDhd5NigSxiSVO1NF0xNjBzODFOwG0> MmfhNlExPzNzNkC=
CCRF-CEM cells NFSyWo1Rem:uaX\ldoF1cW:wIHHzd4F6 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEOFUl[tR2VOKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ3MTFOwG0> M3LJcVIyPjJzOEiz
K562 cells M4XkSnBzd2yrZnXyZZRqd25iYYPzZZk> MmLoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU2KM7:TR?= MlrtNlE3OjF6OEO=
MOLT4 cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 MkLvRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zUOEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{OTFizszN MmrUNlE3OjF6OEO=
SR cells NWrUcGZWWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWjTbHF5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTVkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Nk46QSEQvF2= NFXwXmkzOTZ{MUi4Ny=>
A549 cells MnO2VJJwdGmoZYLheIlwdiCjc4PhfS=> M2\0W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4xQSEQvF2= M4jIcVIyPjJzOEiz
EKVX cells NGHWZWRRem:uaX\ldoF1cW:wIHHzd4F6 NHHoSoFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFXLWngh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPzVizszN MWiyNVYzOTh6Mx?=
HOP62 cells M1HYUnBzd2yrZnXyZZRqd25iYYPzZZk> NGjw[mNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjPVFYzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjVyMjFOwG0> M3TPOVIyPjJzOEiz
HOP92 cells NVPJZnVJWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nuOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSF;QPVIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOTl7IN88US=> NGnZSFAzOTZ{MUi4Ny=>
NCI-H226 cells M1LO[3Bzd2yrZnXyZZRqd25iYYPzZZk> MmO3RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzPiClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS52MTFOwG0> M{\D[|IyPjJzOEiz
NCI-H23 cells NUTSXXZ5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NX36dVd{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ|IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkWg{txO NGD4co0zOTZ{MUi4Ny=>
NCI-H322M cells NUn3d3gxWHKxbHnm[ZJifGmxbjDhd5NigQ>? MlzwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFMzOk1iY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTJwMk[g{txO MleyNlE3OjF6OEO=
NCI-H460 cells NE\re4JRem:uaX\ldoF1cW:wIHHzd4F6 Ml7xRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC55IN88US=> Mn3sNlE3OjF6OEO=
COLO205 cells NIjTV5lRem:uaX\ldoF1cW:wIHHzd4F6 NVK2XnBTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1zLkC4JO69VQ>? M{C5SFIyPjJzOEiz
HCT116 cells M4nTe3Bzd2yrZnXyZZRqd25iYYPzZZk> MV3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NE4{PDdizszN MVKyNVYzOTh6Mx?=
HCT15 cells NGDvepFRem:uaX\ldoF1cW:wIHHzd4F6 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2yMlA4KM7:TR?= M{Lt[VIyPjJzOEiz
HT-29 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 NVXXbFQ4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OC53Nk[g{txO NEW5SmQzOTZ{MUi4Ny=>
KM12 cells M3nBR3Bzd2yrZnXyZZRqd25iYYPzZZk> NWnR[GN1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUVEzKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjB2IN88US=> MWmyNVYzOTh6Mx?=
SW620 cells MXjQdo9tcW[ncnH0bY9vKGG|c3H5 M4fyVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e2NlAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPDd6IN88US=> NYLM[4xGOjF4MkG4PFM>
SF268 cells MkmxVJJwdGmoZYLheIlwdiCjc4PhfS=> M4KxZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yOlgh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVEvPTNizszN M1zSeFIyPjJzOEiz
SF295 cells NHP3NY5Rem:uaX\ldoF1cW:wIHHzd4F6 M3vrRWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[yPVUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPzR|IN88US=> NETI[GUzOTZ{MUi4Ny=>
SF539 cells NITzWnNRem:uaX\ldoF1cW:wIHHzd4F6 M1\qb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvQTZ3IN88US=> NHm0S3kzOTZ{MUi4Ny=>
SNB19 cells NW[0eVRMWHKxbHnm[ZJifGmxbjDhd5NigQ>? NI\ISYpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPORlE6KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0yNjV|IN88US=> NWLHW2p2OjF4MkG4PFM>
SNB75 cells NVP4cJBYWHKxbHnm[ZJifGmxbjDhd5NigQ>? M4jCWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU17CO|Uh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzF6IN88US=> MnX4NlE3OjF6OEO=
U251 cells NEPO[HlRem:uaX\ldoF1cW:wIHHzd4F6 NYPnW|I{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVNlUyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjd5MzFOwG0> MXGyNVYzOTh6Mx?=
LOXIMVI cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 NGr2VW5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzPXGlOXkliY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTFwMEig{txO MX[yNVYzOTh6Mx?=
MALME-3M cells NH7we45Rem:uaX\ldoF1cW:wIHHzd4F6 NHfoV2VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3BUG1GNTOPIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkS2NUDPxE1? NYW0SY9oOjF4MkG4PFM>
M14 cells Ml;SVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn7CRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPMUSgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuPFQ6KM7:TR?= NWjPRlhwOjF4MkG4PFM>
MDA-MB-435 cells M1uwVnBzd2yrZnXyZZRqd25iYYPzZZk> NXPPNWRqSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2wMlU{PyEQvF2= M2e5WlIyPjJzOEiz
SK-MEL-28 cells NFrwXJNRem:uaX\ldoF1cW:wIHHzd4F6 NHO0eGtCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW1GVC1{ODDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD65PVMh|ryP NUL2W|JPOjF4MkG4PFM>
SK-MEL-5 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 NYrD[npESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvNTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;MD6yO|Eh|ryP NVnSeHlNOjF4MkG4PFM>
UACC257 cells M4LTSnBzd2yrZnXyZZRqd25iYYPzZZk> NIDpPYlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGXBR2MzPTdiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwM{mzJO69VQ>? MXiyNVYzOTh6Mx?=
UACC62 cells MWLQdo9tcW[ncnH0bY9vKGG|c3H5 MmnMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXQVPDOlIh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvOzd7IN88US=> NXzvZ5lLOjF4MkG4PFM>
IGROV1 cells NHXmTlVRem:uaX\ldoF1cW:wIHHzd4F6 M1;1T2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSVfSU3YyKGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjF6NzFOwG0> NIPIeFczOTZ{MUi4Ny=>
OVCAR3 cells M1;D[HBzd2yrZnXyZZRqd25iYYPzZZk> NHfnTVlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;WR2FTOyClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OS5zMTFOwG0> NYOwcGt7OjF4MkG4PFM>
OVCAR4 cells MmLTVJJwdGmoZYLheIlwdiCjc4PhfS=> M3jWcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI1KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjJzIN88US=> NWDqRWoyOjF4MkG4PFM>
OVCAR5 cells NV\DfZcyWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{nrWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2\DRXI2KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjJ4IN88US=> MnvKNlE3OjF6OEO=
OVCAR8 cells NHi1RXlRem:uaX\ldoF1cW:wIHHzd4F6 NUnudGVISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPWmNCWjhiY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTBwNEWg{txO NGKxc44zOTZ{MUi4Ny=>
NCI/ADR-RES cells NIXCPI1Rem:uaX\ldoF1cW:wIHHzd4F6 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST;BSHIuWkWVIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1yLkG4JO69VQ>? NHnnVWEzOTZ{MUi4Ny=>
SKOV3 cells NYXuNnJGWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGLuclNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLU3Y{KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m1NF0xNjV{NDFOwG0> NHnsZWIzOTZ{MUi4Ny=>
786-0 cells MkfFVJJwdGmoZYLheIlwdiCjc4PhfS=> M4S3cmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iN{i2MVAh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVIvOzhizszN Mm\6NlE3OjF6OEO=
A498 cells MUPQdo9tcW[ncnH0bY9vKGG|c3H5 M4rObWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUS5PEBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NU4yOSEQvF2= NXHnc3pKOjF4MkG4PFM>
ACHN cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MnnyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDQ1jOJINmdGy|IHL5JHNTSiCjc4PhfUwhT0l3ME2xMlEh|ryP NFnKTG8zOTZ{MUi4Ny=>
Caki1 cells NWj0OWFFWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1zpemFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ3HrbVEh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVAvPjF7IN88US=> MoLPNlE3OjF6OEO=
SN12C cells M2\QeXBzd2yrZnXyZZRqd25iYYPzZZk> M2DFXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU16xNmMh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVMvQTJizszN MmPDNlE3OjF6OEO=
TK10 cells MlfmVJJwdGmoZYLheIlwdiCjc4PhfS=> MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSNMUCgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFQ1KM7:TR?= M3KzZ|IyPjJzOEiz
UO31 cells NE\4[5VRem:uaX\ldoF1cW:wIHHzd4F6 MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFWRM{GgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUCuOFUzKM7:TR?= NYrreXdyOjF4MkG4PFM>
PC3 cells M3;4WHBzd2yrZnXyZZRqd25iYYPzZZk> NGO2c3JCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGDDN{Bk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9NlAh|ryP NFzZdoszOTZ{MUi4Ny=>
DU145 cells MVXQdo9tcW[ncnH0bY9vKGG|c3H5 M3;rR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRGWxOFUh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVI6NjlizszN MmHWNlE3OjF6OEO=
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MDA-MB-231 cells NIfROI5Rem:uaX\ldoF1cW:wIHHzd4F6 MlvRRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1|MT63JO69VQ>? NVnSVXBSOjF4MkG4PFM>
Hs 578T cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NX[4S3ZOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDId{A2PziWIHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13LkiyJO69VQ>? NF2xNZMzOTZ{MUi4Ny=>
BT549 cells MlnZVJJwdGmoZYLheIlwdiCjc4PhfS=> M1rwdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQmS1OFkh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvODRizszN M3LyS|IyPjJzOEiz
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MDA-MB-468 cells MmPkVJJwdGmoZYLheIlwdiCjc4PhfS=> MmLVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDZ6IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD13Lki4JO69VQ>? NUjte|NqOjF4MkG4PFM>
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KM12 cells M2\sZ2N6fG:2b4jpZ4l1gSCjc4PhfS=> MmLoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gT20yOiClZXzsd{whVEN3ME2yPU46KM7:TR?= Mn;2NlE3OjF6OEO=
SF295 cells M3LBVWN6fG:2b4jpZ4l1gSCjc4PhfS=> MlqwR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2YzQTViY3XscJMtKEyFNUC9Ok46OSEQvF2= MYqyNVYzOTh6Mx?=
SNB19 cells MlHIR5l1d3SxeHnjbZR6KGG|c3H5 M2XGb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNPSjF7IHPlcIx{NCCOQ{WwQVMyNjdizszN MV[yNVYzOTh6Mx?=
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LOXIMVI cells MV;DfZRwfG:6aXPpeJkh[XO|YYm= M2T2fGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGxQYEmPVlmgZ4VtdHNuIFzDOVA:Pi5yNDFOwG0> NV;1e4djOjF4MkG4PFM>
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UACC257 cells M{XTZWN6fG:2b4jpZ4l1gSCjc4PhfS=> MlzvR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gWWFESzJ3NzDj[YxteyxiTFO1NF01PC56IN88US=> MnGyNlE3OjF6OEO=
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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.
  • (Only for Reference)
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.
  • (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 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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