GW3965 HCl

For research use only.

Catalog No.S2630

30 publications

GW3965 HCl Chemical Structure

CAS No. 405911-17-3

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

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Selleck's GW3965 HCl has been cited by 30 publications

Purity & Quality Control

Choose Selective Liver X Receptor Inhibitors

Biological Activity

Description GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
Targets
hLXRβ [1]
(Cell-free assay)
LXRα/SRC1 LiSA [1]
(Cell-free assay)
hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
In vitro

GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1] GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1] In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 NVLFcndxOTBidV2= MmHaNlAhcHK| NV21fmh[SWO2aY\heIlwdiCxZjDoeY1idiCOWGLhcJBp[SCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGOxLXX4dJJme3OrbnegbJVu[W5iUmjSZYxxcGFiYYSgNVAhfU1iYX\0[ZIhOjBiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NFXsRmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OECwOlkxQSd-MkiwNFY6ODl:L3G+
HEK293 MUKxNEB2VQ>? NEK1UZQzOCCqcoO= M120fGFkfGm4YYTpc44hd2ZicnH0JGxZWmKndHGg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{1mgHC{ZYPzbY5oKGi3bXHuJHJZWmGucHjhJIF1KDFyIIXNJIFnfGW{IEKwJIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> MmLXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyME[5NFkoRjJ6MEC2PVA6RC:jPh?=
THP1 MnXaSpVv[3Srb36gZZN{[Xl? MYnJcoR2[3Srb36gc4Yh[2ixbHXzeIVzd2xiZX\mcJV5KGmwIGTIVFEh[2WubIOsJGVEPTBiPTCwMlAyKM7:TT6= Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd3OEe1O|MoRjF5NUi3OVc{RC:jPh?=
THP1 NEDzeW5HfW6ldHnvckBie3OjeR?= M1Lq[|E5KGi{cx?= NFfIT3JKdmS3Y4Tpc44hd2ZiY3jvcIV{fGW{b3yg[YZndHW6IHnuJHRJWDFiY3XscJMh[W[2ZYKgNVghcHK|LDDFR|UxKD1iMD6wNUDPxE1w NX;ZNItbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NVY2OjFpPkG3OFE3PTJzPD;hQi=>
COS7 NIj1eHRHfW6ldHnvckBie3OjeR?= MV:xOkBpenN? NY\1PZpISWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFKkZYThJJJm[2WydH;yJJRz[W6|ZnXjeIVlKGmwIFPPV|ch[2WubIOgZYZ1\XJiMU[gbJJ{KGK7IILldI9zfGW{IITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3MDC9JFAvODF3IN88UU4> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6N{W3N{c,OTd3OEe1O|M9N2F-
COS7 NIf0TnFHfW6ldHnvckBie3OjeR?= NF\Jdm1C[3SrdnH0bY9vKG:oIFzYVoJmfGFiY3:teJJidnOoZXP0[YQhcW5iQ1;TO{Bk\WyuczD3bZRpKFK[UnHsdIhiKGK7IILldI9zfGW{IITyZY5{[WO2aY\heIlwdiCjc4PhfUwhTUN3MDC9JFAvODF3IN88UU4> MnXEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd2MU[1NlEoRjF5NEG2OVIyRC:jPh?=
THP1 NV:ybXRbSW62aXnu[oxidW2jdH;yfUBie3OjeR?= MWm2JIhzew>? MnL1RY51cWmwZnzhcY1ifG:{eTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCOUGOtd5RqdXWuYYTl[EBKVDZicILv[JVkfGmxbjDh[pRmeiB4IHjyd{BjgSCHTFnTRUwhUUN3MDC9JFAvODJizszNMi=> M2LX[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y4Lz5zOEiwNFc3PzxxYU6=
THP1 NWXuc4ZYTnWwY4Tpc44h[XO|YYm= MVPB[49vcXO2IHHjeIl3cXS7IHH0JGdCVC2uaX7r[YQhcHWvYX6gUHhT[mW2YTDlfJBz\XO|ZXSgbY4hXEiSMTDj[YxteyCjc4Pld5Nm\CCjczDzeIlufWyjdHnvckBw\iClbz3hZ5RqfmG2b4KgdoVkenWrdH3lcpQh[nliRmLFWEBie3OjeTygSWM2OCB;IECuNFI4KM7:TT6= MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi5O{c,OTd4NkW4PVc9N2F-
RAW264.7 NF63[2pHfW6ldHnvckBie3OjeR?= M{[xRlI1KGi{cx?= NXXye2hmUW6mdXP0bY9vKG:oIGuzTH1kcG:uZYP0[ZJwdCCnZn\seZghcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOgcI9i\GWmIIfpeIgh[WOndInsZZRm\C2ORFygZYZ1\XJiMkSgbJJ{NCCHQ{WwJF0hOC5yMkmg{txONg>? MlnEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5MUezNFQoRjF7N{G3N|A1RC:jPh?=
THP1 NF;XVHZHfW6ldHnvckBie3OjeR?= Ml3UV5RqdXWuYYTpc44hd2ZiW{PIYYNpd2ync4Tldo9tKGWoZnz1fEBqdiCqdX3hckBVUFBzIH\vZY0h[2WubIOgcI9i\GWmIIfpeIgh[WNvTFTMMEBGSzVyIE2gNE4xOzFizszNMi=> NVXwV3RXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
CV1 NIDWTXpHfW6ldHnvckBie3OjeR?= M3X4NGFvfGGpb37pd5Qh[WO2aY\peJkh[XRiTGjSZoV1[SCuaXfhcoQh[mmwZHnu[{Bld22jaX6gZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDUNVMyPy2rbnT1Z4VlKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDWlEh[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBI[Wx2LWPSR|Eh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDhd5NigSxiSVO1NEA:KDBwMEO5PFEh|ryPLh?= NFTPeIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
THP1 NXnpRoZ6TnWwY4Tpc44h[XO|YYm= MVvB[49vcXO2IHHjeIl3cXS7IHH0JGdCVC2uaX7r[YQhcHWvYX6gUHhT[WyyaHGg[ZhxemW|c3XkJIlvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgd5RqdXWuYYTpc44hd2ZiY3;hZ5RqfmG2b4KgdoVkenWrdH3lcpQh[nliRmLFWEBie3OjeTygSWM2OCB;IECuNFk4KM7:TT6= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzZ4NUi5O{c,OTd4NkW4PVc9N2F-
CV1 M3vtSmZ2dmO2aX;uJIF{e2G7 MYLBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEy[UnHsdIhiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGSxN|E4NWmwZIXj[YQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPWNUBk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJGdidDRvU2LDNUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwJF0hOC5zIN88UU4> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN2NUGwNkc,OjB|NEWxNFI9N2F-
SH-SY5Y MmW1SpVv[3Srb36gZZN{[Xl? NEexbWszPCCqcoO= M2HtRWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDlfJBz\XO|ZXSgbY4hcHWvYX6gV2guW1l3WTDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIFfhcFQuVEKGIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlE{KM7:TT6= M1\xSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[0OFgyLz5zOUK2OFQ5OTxxYU6=
HepG2 MmTkSpVv[3Srb36gZZN{[Xl? MoPnSYZn\WO2IH;uJHNTTUKSMXOg[4Vv\SCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzMEBGSzVyIE2gNE4zOSEQvF2u NXPhe4k{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
HuH7 NHfJ[ZRHfW6ldHnvckBie3OjeR?= M1HIXWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gdoVkd22kaX7hcpQhVFiUYnX0ZUBtcWejbnSgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iSIXIO{Bk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJIZ2e2WmIFfhcFQuTEKGIHL5JJRz[W6|YXP0bZZifGmxbjDhd5NigSxiRVO1NEA:KDBwM{Gg{txONg>? NFPuTpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
SH-SY5Y M4HMS2Z2dmO2aX;uJIF{e2G7 NW\QWZUzOjRiaILz MYjB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVoFteGijIHX4dJJme3OnZDDpckBpfW2jbjDTTE1UYTW\IHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1NSkRiYX\0[ZIhOjRiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OCB;IECuN|Eh|ryPLh?= NYHkVVRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlQ1QDFpPkG5NlY1PDhzPD;hQi=>
CHO M3frS2Z2dmO2aX;uJIF{e2G7 MkD0RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHIh[mW2YTDy[YNmeHSxcjDlfJBz\XO|ZXSgbY4hS0iRIHPlcIx{KGK7IILldI9zfGW{IHHzd4F6NCCHQ{WwJF0hOC52MTFOwG0v M1jvTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5MEO0NVE6Lz5zN{CzOFEyQTxxYU6=
CHOK1 NVe3eFVmTnWwY4Tpc44h[XO|YYm= M{WzflI1KGi{cx?= MVjB[49vcXO2IHHjeIl3cXS7IHH0JGdidDRvdHHn[4VlKEy[UnLleIEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvPDJizszNMi=> M4rvblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke3OlY1Lz5{NU[3O|Y3PDxxYU6=
THP1 NHjqZYtHfW6ldHnvckBie3OjeR?= MofPSYZn\WO2IH;uJGFDS0FzIHflcoUh\XiycnXzd4lwdiCrbjDoeY1idiCmaX\m[ZJmdnSrYYTl[EBVUFBzIHPlcIx{NCCHQ{WwJF0hOC52M{Sg{txONg>? MmWxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
CV1 M17tTGZ2dmO2aX;uJIF{e2G7 NYTuVpN1SWexbnnzeEBi[3Srdnn0fUBifCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbj3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gZYZzcWOjbjDndoVmdiCvb37r[ZkhS1ZzIHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1UWkNzIHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGVEPTBiPTCwMlUxOTF7IN88UU4> MmrFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NEWxNFIoRjJyM{S1NVAzRC:jPh?=
HuH7 M{HD[2Z2dmO2aX;uJIF{e2G7 NWPGfZJWSWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBz\WOxbXLpcoFvfCCOWGLhcJBp[SCuaXfhcoQh[mmwZHnu[{Bld22jaX6gbY4hcHWvYX6gTJVJPyClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKG[3c3XkJGdidDRvRFLEJIJ6KHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OCB;IECuOlYh|ryPLh?= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
CV1 MWfGeY5kfGmxbjDhd5NigQ>? MYXB[49vcXO2IHHjeIl3cXS7IHH0JGxZWmGucHjhJIxq\2GwZDDibY5lcW6pIHTvcYFqdi2vZXTpZZRm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIghT2GuND3TVmMyKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFXDOVAhRSByLke5OFM{KM7:TT6= NHXSS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
CHOK1 NX:ycol5TnWwY4Tpc44h[XO|YYm= MVKyOEBpenN? M1GyOGFod26rc4SgZYN1cX[rdImgZZQhT2GuND30ZYdo\WRiTGjSZYxxcGFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gR2hQUzFiY3XscJMh[W[2ZYKgNlQhcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NEA:KDFwMzFOwG0v M{HTW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke3OlY1Lz5{NU[3O|Y3PDxxYU6=
HepG2 MULGeY5kfGmxbjDhd5NigQ>? MnPYSYZn\WO2IH;uJJRzcWeueXPldoll\SCjY3P1cZVt[XSrb36gbY4hcHWvYX6gTIVxTzJiY3XscJMtKEWFNUCgQUAzNjByMjFOwG0v M331S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUezNlg5Lz5zOEm3N|I5QDxxYU6=
HepG2 NIfVc|lHfW6ldHnvckBie3OjeR?= NWjZXHVUPTByIH7N MWXJcohq[mm2aX;uJI9nKDJvKEOtLFMuMCh{LXPocI9zdy1|LTj0dolndHWxcn;t[ZRpgWxrYnXufpltMSh{LEKt[IlxcGWweXzleIh6dCmjbXnuc{lxem:yb4j5LZBp\W67bDnhZ4V1cWNiYXPp[E1qdmS3Y3XkJJNz\WKyMXOgcXJPSSCneIDy[ZN{cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJIF1KDVyMDDuUS=> NWizRVZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
HepG2 NXjzc4dxTnWwY4Tpc44h[XO|YYm= NE\iWIQ2ODBibl2= MX3Jcohq[mm2aX;uJI9nKDJvKEOtLFMuMCh{LXPocI9zdy1|LTj0dolndHWxcn;t[ZRpgWxrYnXufpltMSh{LEKt[IlxcGWweXzleIh6dCmjbXnuc{lxem:yb4j5LZBp\W67bDnhZ4V1cWNiYXPp[E1qdmS3Y3XkJIZieyCvUl7BJIV5eHKnc4Ppc44hcW5iaIXtZY4hUGWyR{KgZ4VtdHNiYYSgOVAxKG6P MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
RAW264.7 M1XYUmZ2dmO2aX;uJIF{e2G7 MVOxJJVO MWLS[YR2[3Srb36gc4YhVFCVLYP0bY12dGG2ZXSgbW5QWyCpZX7lJIV5eHKnc4Ppc44hcW5ibX;1d4UhWkGZMk[0Mlch[2WubIOg[ZhxemW|c3nu[{BNYFKjbIDoZUBifCBzIIXNJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= NULVbWlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
RAW264.7 MVjGeY5kfGmxbjDhd5NigQ>? M{D0PVEhfU1? M2TvVWlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhdnWlbHXhdkBkdy2{ZYDy[ZN{d3JicnXs[YF{\SCocn;tJIlPV1NicILvcY91\XJiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XRiMTD1UUBjgSCUVD3QR3I> M1PYNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y4Lz5zOEiwNFc3PzxxYU6=
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SJ-GBM2 M3PaS5FJXFNiYYPzZZk> MnrJdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NGLLPGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 NHnhcYlyUFSVIHHzd4F6 MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NEXRRmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC M{\sUZFJXFNiYYPzZZk> MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M1W1dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 M{THepFJXFNiYYPzZZk> NFjHNXFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= M1X5O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 Mn7LdWhVWyCjc4PhfS=> NEK4XmxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH NGXmVGRyUFSVIHHzd4F6 MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NVrpR|d5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 M4LP[5FJXFNiYYPzZZk> M33NTpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= NUXoSoNwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NYTLZYZMeUiWUzDhd5NigQ>? MYPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| NVTyVnNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD Mn\KdWhVWyCjc4PhfS=> M1rK[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? Mk\SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) M2nJU5FJXFNiYYPzZZk> MnTpdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE2JIE[zJEg3NVSJIGKpJINmdGy| NHXkelI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 MVPxTHRUKGG|c3H5 MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh|MDDj[Yxtew>? M13rcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 NEX3dIJyUFSVIHHzd4F6 MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? M1PpPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Skp2 / pEGFR / EGFR / pERK / ERK ; 

PubMed: 25184494     


GW3965 treatment downregulates SKP2 and EGFR protein levels in BxPC-3 and MIA-PaCa-2 cells. Downregulation of EGFR was concomitant with a downregulation of its own phosphorylation in BxPC-3 and MIA-PaCa-2 at 5 uM GW 3965. ERK1/2 and its phosphorylation were not statistically different in any of the cell lines.

LXRα / LXRβ / ABCA1 / ABCG1; 

PubMed: 11604492     


Differentiated THP-1 macrophages were incubated for 48 h in RPMI medium plus 10% LPDS, Oxysterols [20(S)HC, 22(R)HC, or 22(S)HC, 2.0 μg/ml], synthetic LXR ligand (GW3965 or T1317, 0.1 to 10.0 μM), or RXR ligand (LG268, 50 nM).

25184494 11604492
Immunofluorescence
LAMP-1 / LDLR; 

PubMed: 23382078     


HeLa cells were cultured in 10% LPDS medium for 8 h and then treated with GW3965 (1 μM) for the indicated times. Cells were immunostained with LDLR and LAMP-1 antibodies. Nuclei were counterstained with DAPI (blue). Representative confocal images are shown. T, time; O/N, overnight.

pRelA ; 

PubMed: 26635040     


Freshly isolated PDC (plasmacytoid dendritic cells) were treated for 24 h with 1 mM of GW3965 (GW), followed by TLR7 ligand, R848 (1 mg/mL) for 45 min. Phosphorylation of the NF-κB p65 (pRelA) subunit and its cellular localization were evaluated by confocal microscopy analysis. Results from a representative experiment out of 3 using PDC from 3 different donors.

23382078 26635040
Growth inhibition assay
Cell viability; 

PubMed: 25184494     


A, B, C, PDAC cells (BxPC-3, Mia-PaCa-2, and PANC-1 cell lines, respectively) show dose-dependent decreases in cell proliferation upon treatment with increasing GW3965 concentrations. EC50 calculations indicate that BxPC-3 and Mia-PaCa-2 cells are more sensitive to ligand treatment than PANC-1 cells. 

25184494
In vivo In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1] GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. [2] In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3] In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: C57BL/6 mice
  • Dosages: ≤10 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL warmed (25.86 mM)
Water Insoluble
Ethanol Insoluble

* 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 618.51
Formula

C33H31ClF3NO3.HCl

CAS No. 405911-17-3
Storage powder
in solvent
Synonyms N/A
Smiles C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl

In vivo Formulation Calculator (Clear solution)

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

Molarity Calculator

Molarity Calculator

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

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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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).

Dilution Calculator

Dilution Calculator

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

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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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.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    How to formulate the compound for mouse in vivo experiment?

  • Answer:

    S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID