GW3965 HCl

For research use only.

Catalog No.S2630

31 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.

Selleck's GW3965 HCl has been cited by 31 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 M2rSVFExKHWP M{nuXFIxKGi{cx?= NVTSeWdqSWO2aY\heIlwdiCxZjDoeY1idiCOWGLhcJBp[SCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGOxLXX4dJJme3OrbnegbJVu[W5iUmjSZYxxcGFiYYSgNVAhfU1iYX\0[ZIhOjBiaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= M1LxOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEC2PVA6Lz5{OECwOlkxQTxxYU6=
HEK293 NFTBcFQyOCC3TR?= MWSyNEBpenN? M2[1WmFkfGm4YYTpc44hd2ZicnH0JGxZWmKndHGg[ZhxemW|c3XkJIlvKEiHS{K5N{Bk\WyuczDjc{1mgHC{ZYPzbY5oKGi3bXHuJHJZWmGucHjhJIF1KDFyIIXNJIFnfGW{IEKwJIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> MnT1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhyME[5NFkoRjJ6MEC2PVA6RC:jPh?=
THP1 MnLCSpVv[3Srb36gZZN{[Xl? Ml\nTY5lfWO2aX;uJI9nKGOqb3zld5Rmem:uIHXm[ox2gCCrbjDUTHAyKGOnbHzzMEBGSzVyIE2gNE4xOSEQvF2u MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzV6N{W3N{c,OTd3OEe1O|M9N2F-
THP1 NFPXfolHfW6ldHnvckBie3OjeR?= MX6xPEBpenN? MkHsTY5lfWO2aX;uJI9nKGOqb3zld5Rmem:uIHXm[ox2gCCrbjDUTHAyKGOnbHzzJIFnfGW{IEG4JIhzeyxiRVO1NEA:KDBwMEGg{txONg>? NWPMR484RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NVY2OjFpPkG3OFE3PTJzPD;hQi=>
COS7 NH3BWJhHfW6ldHnvckBie3OjeR?= M4TXeVE3KGi{cx?= M37wfGFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gUHhT[mW2YTDy[YNmeHSxcjD0doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiC2cnHud4FkfGm4YYTpc44h[XO|YYmsJGVEPTBiPTCwMlAyPSEQvF2u M2TQVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUi3OVc{Lz5zN{W4O|U4OzxxYU6=
COS7 MX;GeY5kfGmxbjDhd5NigQ>? MX3BZ5RqfmG2aX;uJI9nKEy[UnLleIEh[29vdILhcpNn\WO2ZXSgbY4hS0:VNzDj[YxteyC5aYToJHJZWmGucHjhJIJ6KHKncH;yeIVzKHS{YX7zZYN1cX[jdHnvckBie3OjeTygSWM2OCB;IECuNFE2KM7:TT6= NIK0b2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{SxOlUzOSd-MUe0NVY2OjF:L3G+
THP1 MoKwRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? MmnXOkBpenN? NYnEWXBpSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDMVHMue3SrbYXsZZRm\CCLTE[gdJJw\HWldHnvckBi\nSncjC2JIhzeyCkeTDFUGlUSSxiSVO1NEA:KDBwMEKg{txONg>? NWC3cmhLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
THP1 Mny4SpVv[3Srb36gZZN{[Xl? M3nrTmFod26rc4SgZYN1cX[rdImgZZQhT0GOLXzpcotm\CCqdX3hckBNYFKkZYThJIV5eHKnc4Pl[EBqdiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzJJN1cW23bHH0bY9vKG:oIHPvMYFkfGm4YYTvdkBz\WO{dXn0cYVvfCCkeTDGVmVVKGG|c3H5MEBGSzVyIE2gNE4xOjdizszNMi=> NWTiNHk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe2OlU5QTdpPkG3OlY2QDl5PD;hQi=>
RAW264.7 MVLGeY5kfGmxbjDhd5NigQ>? MYqyOEBpenN? Mn;uTY5lfWO2aX;uJI9nKFt|SG3jbI9t\XO2ZYLvcEBm\m[udYigbY4hdW:3c3WgVmFYOjZ2LkegZ4VtdHNibH;h[IVlKHerdHigZYNmfHmuYYTl[E1NTExiYX\0[ZIhOjRiaILzMEBGSzVyIE2gNE4xOjlizszNMi=> Mn7jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5MUezNFQoRjF7N{G3N|A1RC:jPh?=
THP1 NVjrUIRGTnWwY4Tpc44h[XO|YYm= NUDNUIdRW3SrbYXsZZRqd25ib3[gX|NJZWOqb3zld5Rmem:uIHXm[ox2gCCrbjDoeY1idiCWSGCxJIZw[W1iY3XscJMhdG:jZHXkJJdqfGhiYXOtUGRNNCCHQ{WwJF0hOC5yM{Gg{txONg>? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
CV1 MXHGeY5kfGmxbjDhd5NigQ>? MYrBcpRi\2:waYP0JIFkfGm4aYT5JIF1KEy[UnLleIEhdGmpYX7kJIJqdmSrbneg[I9u[WmwIHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiVEGzNVcucW6mdXPl[EB1emGwc3PybZB1cW:wYXygZYN1cX[rdImgbY4h[W[{aXPhckBoemWnbjDtc45s\XliQ2[xJINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHigS4FtPC2VUlOxJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUCgQUAxNjB|OUixJO69VS5? NEHaeXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
THP1 M4Dz[WZ2dmO2aX;uJIF{e2G7 MXPB[49vcXO2IHHjeIl3cXS7IHH0JGdCVC2uaX7r[YQhcHWvYX6gUHhT[WyyaHGg[ZhxemW|c3XkJIlvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgd5RqdXWuYYTpc44hd2ZiY3;hZ5RqfmG2b4KgdoVkenWrdH3lcpQh[nliRmLFWEBie3OjeTygSWM2OCB;IECuNFk4KM7:TT6= MnzXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd4NkW4PVcoRjF5Nk[1PFk4RC:jPh?=
CV1 NIS4b|JHfW6ldHnvckBie3OjeR?= NILpc3pCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IFzYVoFteGijIHzp[4Fv\CCkaX7kbY5oKGSxbXHpckBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHQyOzF5LXnu[JVk\WRidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHHmdolk[W5iZ4Ll[Y4hdW:wa3X5JGNXOSClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKEejbEStV3JEOSCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7LDDJR|UxKD1iMD6xJO69VS5? Ml23QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB|NEWxNFIoRjJyM{S1NVAzRC:jPh?=
SH-SY5Y NWrhe|g{TnWwY4Tpc44h[XO|YYm= M{\kPVI1KGi{cx?= MXzB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVoJmfGFiZYjwdoV{e2WmIHnuJIh2dWGwIGPIMXN[PVliY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MWxDTCCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMD6xN{DPxE1w M{\2PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7Mk[0OFgyLz5zOUK2OFQ5OTxxYU6=
HepG2 NEPJdIlHfW6ldHnvckBie3OjeR?= NGnq[4dG\m[nY4Sgc44hW1KHQmCxZ{Bo\W6nIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMtKEWFNUCgQUAxNjJzIN88UU4> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
HuH7 MWfGeY5kfGmxbjDhd5NigQ>? MkPBRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDy[YNwdWKrbnHueEBNYFKkZYThJIxq\2GwZDDibY5lcW6pIHTvcYFqdiCrbjDoeY1idiCKdVi3JINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHig[pV{\WRiR3HsOE1FSkRiYomgeJJidnOjY4TpeoF1cW:wIHHzd4F6NCCHQ{WwJF0hOC5|MTFOwG0v NVXERnY4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
SH-SY5Y MmKySpVv[3Srb36gZZN{[Xl? M4TFb|I1KGi{cx?= NXrlPXY3SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFKjbIDoZUBmgHC{ZYPz[YQhcW5iaIXtZY4hW0hvU2m1XUBk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJGdidDRvTFLEJIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUCgQUAxNjNzIN88UU4> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTJ4NES4NUc,OTl{NkS0PFE9N2F-
CHO NIn3bI9HfW6ldHnvckBie3OjeR?= MUTB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVkBj\XSjIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nlicnXwc5J1\XJiYYPzZZktKEWFNUCgQUAxNjRzIN88UU4> NVnOcJYyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUewN|QyOTlpPkG3NFM1OTF7PD;hQi=>
CHOK1 NYDVdoV6TnWwY4Tpc44h[XO|YYm= M1XaVVI1KGi{cx?= M4X5[GFod26rc4SgZYN1cX[rdImgZZQhT2GuND30ZYdo\WRiTGjSZoV1[SBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDDTG9MOSClZXzsd{Bi\nSncjCyOEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwJF0hOC52MjFOwG0v MmOxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV4N{e2OlQoRjJ3Nke3OlY1RC:jPh?=
THP1 NHvXXFhHfW6ldHnvckBie3OjeR?= M3Xh[2Vn\mWldDDvckBCSkODMTDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5iZHnm[oVz\W62aXH0[YQhXEiSMTDj[YxteyxiRVO1NEA:KDBwNEO0JO69VS5? NFfoVGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
CV1 MmHHSpVv[3Srb36gZZN{[Xl? NF;YOYRC\2:waYP0JIFkfGm4aYT5JIF1KEy[UnLleIEhdGmpYX7kJIJqdmSrbneg[I9u[WmwLX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXjFiY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MXNTSzFiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygSWM2OCB;IECuOVAyOTlizszNMi=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN2NUGwNkc,OjB|NEWxNFI9N2F-
HuH7 NEXKR3dHfW6ldHnvckBie3OjeR?= M3vmc2Fod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gdoVkd22kaX7hcpQhVFiUYXzwbIEhdGmpYX7kJIJqdmSrbneg[I9u[WmwIHnuJIh2dWGwIFj1TFch[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBnfXOnZDDHZYw1NUSERDDifUB1emGwc3HjeIl3[XSrb36gZZN{[XluIFXDOVAhRSByLk[2JO69VS5? NETmT2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEm3N|I5QCd-MUi5O|MzQDh:L3G+
CV1 MY\GeY5kfGmxbjDhd5NigQ>? NETPZ25C\2:waYP0JIFkfGm4aYT5JIF1KEy[UnHsdIhiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbj3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gZYZzcWOjbjDndoVmdiCvb37r[ZkhS1ZzIHPlcIx{KGOxLYTyZY5{\mWldHXkJJdqfGhiR3HsOE1UWkNzIHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGVEPTBiPTCwMlc6PDN|IN88UU4> M1v0[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{S1NVAzLz5{MEO0OVExOjxxYU6=
CHOK1 NGfJbVZHfW6ldHnvckBie3OjeR?= M{nZNVI1KGi{cx?= NXzmWph3SWexbnnzeEBi[3Srdnn0fUBifCCJYXy0MZRi\2enZDDMXHJidHCqYTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBEUE:NMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMT6zJO69VS5? NH\zcpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[3O|Y3PCd-MkW2O|c3PjR:L3G+
HepG2 NI\vbWtHfW6ldHnvckBie3OjeR?= MV\F[oZm[3Rib36geJJq\2y7Y3XybYRmKGGlY4XteYxifGmxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{whTUN3MDC9JFIvODB{IN88UU4> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDl5M{K4PEc,OTh7N{OyPFg9N2F-
HepG2 MYrGeY5kfGmxbjDhd5NigQ>? NFzER4c2ODBibl2= M2DYWWlvcGmkaYTpc44hd2ZiMj2oN{0pOy1qKEKtZ4htd3KxLUOtLJRzcW[udX;yc41mfGi7bDni[Y57gWxrKEKsNk1lcXCqZX75cIV1cHmuKXHtbY5wMXC{b4DvfJkqeGinbonsLYFk\XSrYzDhZ4llNWmwZIXj[YQhe3KnYoCxZ{BuWk6DIHX4dJJme3Orb36gbY4hcHWvYX6gTIVxTzJiY3XscJMh[XRiNUCwJI5O M2Pt[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y4Lz5zOEiwNFc3PzxxYU6=
HepG2 MXvGeY5kfGmxbjDhd5NigQ>? M13yelUxOCCwTR?= MkTsTY5pcWKrdHnvckBw\iB{LTizMUg{NShqMj3jbIxwem9vMz2oeJJq\my3b4LvcYV1cHmuKXLlcpp6dClqMjyyMYRqeGinbons[ZRpgWxrYX3pco8qeHKxcH;4fUlxcGWweXypZYNmfGmlIHHjbYQucW6mdXPl[EBn[XNibWLORUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEincFeyJINmdGy|IHH0JFUxOCCwTR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
RAW264.7 M37POWZ2dmO2aX;uJIF{e2G7 NYrtfYwyOSC3TR?= M1L1eXJm\HWldHnvckBw\iCOUGOtd5RqdXWuYYTl[EBqVk:VIHflcoUh\XiycnXzd4lwdiCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{BmgHC{ZYPzbY5oKEy[UnHsdIhiKGG2IEGgeW0h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhyMEe2O{c,OTh6MEC3Olc9N2F-
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A673 MlTLdWhVWyCjc4PhfS=> MVXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NWLm[4xXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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NB-EBc1 NH;WPWlyUFSVIHHzd4F6 Mke3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= MoXFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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OHS-50 MVnxTHRUKGG|c3H5 MljNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NX;kd3VVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD M4nOXJFJXFNiYYPzZZk> MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NELXeZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NVnvSIZDeUiWUzDhd5NigQ>? MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 M2DDbpFJXFNiYYPzZZk> MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh|MDDj[Yxtew>? MnTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MVHxTHRUKGG|c3H5 MnzSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? M3LlVVxiKHSjcnfleF0oZ2KuYX7rK{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)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
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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 SDS / 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 SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

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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)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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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