GW3965 HCl

For research use only.

Catalog No.S2630

29 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 29 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 NYXyRVRPOTBidV2= M4ize|IxKGi{cx?= MW\BZ5RqfmG2aX;uJI9nKGi3bXHuJGxZWmGucHjhJIV5eHKnc4Pl[EBqdiCKRVuyPVMh[2WubIOgZ48u\XiycnXzd4lv\yCqdX3hckBTYFKjbIDoZUBifCBzMDD1UUBi\nSncjCyNEBpenNiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6 M1H6T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEC2PVA6Lz5{OECwOlkxQTxxYU6=
HEK293 NILTXGIyOCC3TR?= M4HqV|IxKGi{cx?= MWPBZ5RqfmG2aX;uJI9nKHKjdDDMXHJj\XSjIHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiY3:t[ZhxemW|c3nu[{BpfW2jbjDSXHJidHCqYTDheEAyOCC3TTDh[pRmeiB{MDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 M2fnOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEC2PVA6Lz5{OECwOlkxQTxxYU6=
THP1 MoT6SpVv[3Srb36gZZN{[Xl? MmPOTY5lfWO2aX;uJI9nKGOqb3zld5Rmem:uIHXm[ox2gCCrbjDUTHAyKGOnbHzzMEBGSzVyIE2gNE4xOSEQvF2u M1jFRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUi3OVc{Lz5zN{W4O|U4OzxxYU6=
THP1 Mnn4SpVv[3Srb36gZZN{[Xl? MW[xPEBpenN? NYXqcldwUW6mdXP0bY9vKG:oIHPoc4xme3Sncn;sJIVn\my3eDDpckBVUFBzIHPlcIx{KGGodHXyJFE5KGi{czygSWM2OCB;IECuNFEh|ryPLh?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzRzNkWyNUc,OTd2MU[1NlE9N2F-
COS7 MXLGeY5kfGmxbjDhd5NigQ>? NVzoNXJIOTZiaILz MUPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIFzYVoJmfGFicnXj[ZB1d3JidILhcpNn\WO2ZXSgbY4hS0:VNzDj[YxteyCjZoTldkAyPiCqcoOgZpkhemWyb4L0[ZIhfHKjboPhZ5RqfmG2aX;uJIF{e2G7LDDFR|UxKD1iMD6wNVUh|ryPLh?= M2TBelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5NUi3OVc{Lz5zN{W4O|U4OzxxYU6=
COS7 M37pT2Z2dmO2aX;uJIF{e2G7 M{XQ[mFkfGm4YYTpc44hd2ZiTGjSZoV1[SClbz30doFve2[nY4Tl[EBqdiCFT2O3JINmdGy|IIfpeIghWliUYXzwbIEh[nlicnXwc5J1\XJidILhcpNi[3SrdnH0bY9vKGG|c3H5MEBGSzVyIE2gNE4xOTVizszNMi=> NVX6Om0{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUe0NVY2OjFpPkG3OFE3PTJzPD;hQi=>
THP1 NXLjNWJjSW62aXnu[oxidW2jdH;yfUBie3OjeR?= NXHUSYhkPiCqcoO= M4\XUWFvfGmrbn\sZY1u[XSxcomgZYN1cX[rdImgZYdicW6|dDDoeY1idiCWSGCxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhUUx4IIDyc4R2[3Srb36gZYZ1\XJiNjDodpMh[nliRVzJV2EtKEmFNUCgQUAxNjB{IN88UU4> NV\EdJFoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
THP1 MVTGeY5kfGmxbjDhd5NigQ>? MnXQRYdwdmm|dDDhZ5Rqfmm2eTDheEBISUxvbHnub4VlKGi3bXHuJGxZWmKndHGg[ZhxemW|c3XkJIlvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgd5RqdXWuYYTpc44hd2ZiY3:tZYN1cX[jdH;yJJJm[3K3aYTt[Y51KGK7IF\SSXQh[XO|YYmsJGVEPTBiPTCwMlAzPyEQvF2u NGfBN4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[2OVg6Pyd-MUe2OlU5QTd:L3G+
RAW264.7 M{LpSWZ2dmO2aX;uJIF{e2G7 MV6yOEBpenN? NGDwd25KdmS3Y4Tpc44hd2ZiW{PIYYNpd2ync4Tldo9tKGWoZnz1fEBqdiCvb4Xz[UBTSVd{NkSuO{Bk\WyuczDsc4Fl\WRid3n0bEBi[2W2eXzheIVlNUyGTDDh[pRmeiB{NDDodpMtKEWFNUCgQUAxNjB{OTFOwG0v M1nwfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{G3N|A1Lz5zOUexO|MxPDxxYU6=
THP1 MoTwSpVv[3Srb36gZZN{[Xl? NYTNeVRYW3SrbYXsZZRqd25ib3[gX|NJZWOqb3zld5Rmem:uIHXm[ox2gCCrbjDoeY1idiCWSGCxJIZw[W1iY3XscJMhdG:jZHXkJJdqfGhiYXOtUGRNNCCHQ{WwJF0hOC5yM{Gg{txONg>? Mm\3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
CV1 NVvCTpFSTnWwY4Tpc44h[XO|YYm= Mn7NRY51[WexbnnzeEBi[3Srdnn0fUBifCCOWGLi[ZRiKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIGSxN|E4NWmwZIXj[YQhfHKjboPjdolxfGmxbnHsJIFkfGm4aYT5JIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPWNUBk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJGdidDRvU2LDNUBjgSCudXPp[oVz[XOnIILldI9zfGW{IHHzd4F6NCCLQ{WwJF0hOC5yM{m4NUDPxE1w NUHncXJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFUyODJpPkKwN|Q2OTB{PD;hQi=>
THP1 MVnGeY5kfGmxbjDhd5NigQ>? MXHB[49vcXO2IHHjeIl3cXS7IHH0JGdCVC2uaX7r[YQhcHWvYX6gUHhT[WyyaHGg[ZhxemW|c3XkJIlvKFSKUEGgZ4VtdHNiYYPz[ZN{\WRiYYOgd5RqdXWuYYTpc44hd2ZiY3;hZ5RqfmG2b4KgdoVkenWrdH3lcpQh[nliRmLFWEBie3OjeTygSWM2OCB;IECuNFk4KM7:TT6= NGCzUVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{[2OVg6Pyd-MUe2OlU5QTd:L3G+
CV1 NV:5dGxKTnWwY4Tpc44h[XO|YYm= NUTqd406SW62YXfvcol{fCCjY4Tpeol1gSCjdDDMXHJidHCqYTDsbYdidmRiYnnu[Ilv\yCmb33hbY4h[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBVOTNzNz3pcoR2[2WmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXjFiY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MXNTSzFiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygTWM2OCB;IECuNUDPxE1w NWD4dI1zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzOFUyODJpPkKwN|Q2OTB{PD;hQi=>
SH-SY5Y NGXQV5VHfW6ldHnvckBie3OjeR?= NYLhVJliOjRiaILz NV\xc4c2SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBNYFKkZYThJIV5eHKnc4Pl[EBqdiCqdX3hckBUUC2VWUXZJINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHigS4FtPC2OQlSgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvOTNizszNMi=> NVy5eolIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlQ1QDFpPkG5NlY1PDhzPD;hQi=>
HepG2 NXzpVmtCTnWwY4Tpc44h[XO|YYm= M4HKNWVn\mWldDDvckBUWkWEUEHjJIdmdmViZYjwdoV{e2mxbjDpckBpfW2jbjDI[ZBIOiClZXzsd{whTUN3MDC9JFAvOjFizszNMi=> NWn3Zm17RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
HuH7 MY\GeY5kfGmxbjDhd5NigQ>? MXrB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIILlZ49u[mmwYX70JGxZWmKndHGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGmwIHj1cYFvKEi3SEegZ4VtdHNiY3:teJJidnOoZXP0[YQhf2m2aDDmeZNm\CCJYXy0MWRDTCCkeTD0doFve2GldHn2ZZRqd25iYYPzZZktKEWFNUCgQUAxNjNzIN88UU4> MlqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
SH-SY5Y MkLDSpVv[3Srb36gZZN{[Xl? MonrNlQhcHK| Mn;1RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDMXHJidHCqYTDlfJBz\XO|ZXSgbY4hcHWvYX6gV2guW1l3WTDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIFfhcFQuVEKGIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGVEPTBiPTCwMlMyKM7:TT6= NXXmbFFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmyOlQ1QDFpPkG5NlY1PDhzPD;hQi=>
CHO MlvSSpVv[3Srb36gZZN{[Xl? NFLSZ|BC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJGxZWiCkZYThJJJm[2WydH;yJIV5eHKnc4Pl[EBqdiCFSF:gZ4VtdHNiYomgdoVxd3K2ZYKgZZN{[XluIFXDOVAhRSByLkSxJO69VS5? Mm\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTdyM{SxNVkoRjF5MEO0NVE6RC:jPh?=
CHOK1 M{PsSWZ2dmO2aX;uJIF{e2G7 M4nx[FI1KGi{cx?= MWPB[49vcXO2IHHjeIl3cXS7IHH0JGdidDRvdHHn[4VlKEy[UnLleIEhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5iQ1jPT|Eh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfUwhTUN3MDC9JFAvPDJizszNMi=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ5N{[2OEc,OjV4N{e2OlQ9N2F-
THP1 NH3lfXdHfW6ldHnvckBie3OjeR?= M3XlRmVn\mWldDDvckBCSkODMTDn[Y5mKGW6cILld5Nqd25iaX6gbJVu[W5iZHnm[oVz\W62aXH0[YQhXEiSMTDj[YxteyxiRVO1NEA:KDBwNEO0JO69VS5? M2LTfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OUezNlg5Lz5zOEm3N|I5QDxxYU6=
CV1 NXnPc5R7TnWwY4Tpc44h[XO|YYm= MnfyRYdwdmm|dDDhZ5Rqfmm2eTDheEBNYFKkZYThJIxq\2GwZDDibY5lcW6pIHTvcYFqdi2vZXTpZZRm\CC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIghT2GuND3TVmMyKGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKgZZN{[XluIFXDOVAhRSByLkWwNVE6KM7:TT6= M4ixTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyM{S1NVAzLz5{MEO0OVExOjxxYU6=
HuH7 M2P5TGZ2dmO2aX;uJIF{e2G7 Ml3URYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDy[YNwdWKrbnHueEBNYFKjbIDoZUBtcWejbnSgZolv\GmwZzDkc41icW5iaX6gbJVu[W5iSIXIO{Bk\WyuczDjc{11emGwc3\lZ5Rm\CC5aYToJIZ2e2WmIFfhcFQuTEKGIHL5JJRz[W6|YXP0bZZifGmxbjDhd5NigSxiRVO1NEA:KDBwNk[g{txONg>? NYDpS3hVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi5O|MzQDhpPkG4PVc{Ojh6PD;hQi=>
CV1 NX3pRYxMTnWwY4Tpc44h[XO|YYm= M1rmdWFod26rc4SgZYN1cX[rdImgZZQhVFiUYXzwbIEhdGmpYX7kJIJqdmSrbneg[I9u[WmwLX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEXjFiY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MXNTSzFiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygSWM2OCB;IECuO|k1OzNizszNMi=> NHe5NlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEO0OVExOid-MkCzOFUyODJ:L3G+
CHOK1 NX3mOFYzTnWwY4Tpc44h[XO|YYm= MnrKNlQhcHK| NVLRdI5bSWexbnnzeEBi[3Srdnn0fUBifCCJYXy0MZRi\2enZDDMXHJidHCqYTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBEUE:NMTDj[YxteyCjZoTldkAzPCCqcoOgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxKD1iMT6zJO69VS5? M4rUbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Nke3OlY1Lz5{NU[3O|Y3PDxxYU6=
HepG2 MlTpSpVv[3Srb36gZZN{[Xl? NYTj[5Y5TW[oZXP0JI9vKHS{aXfsfYNmemmmZTDhZ4N2dXWuYYTpc44hcW5iaIXtZY4hUGWyR{KgZ4VtdHNuIFXDOVAhRSB{LkCwNkDPxE1w MkD6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh7N{OyPFgoRjF6OUezNlg5RC:jPh?=
HepG2 NIHGZplHfW6ldHnvckBie3OjeR?= MmW2OVAxKG6P NYrnOmh3UW6qaXLpeIlwdiCxZjCyMUg{NSh|LTioNk1kcGyxcn:tN{0pfHKrZnz1c5JwdWW2aInsLYJmdnq7bDmoNkwzNWSrcHjlcplt\XSqeXypZY1qdm9rcILvdI95gSmyaHXufYwq[WOndHnjJIFkcWRvaX7keYNm\CC|cnXidFFkKG2UTlGg[ZhxemW|c3nvckBqdiCqdX3hckBJ\XCJMjDj[YxteyCjdDC1NFAhdk1? NGrlNZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
HepG2 M3fZ[WZ2dmO2aX;uJIF{e2G7 MkDWOVAxKG6P M13hR2lvcGmkaYTpc44hd2ZiMj2oN{0pOy1qKEKtZ4htd3KxLUOtLJRzcW[udX;yc41mfGi7bDni[Y57gWxrKEKsNk1lcXCqZX75cIV1cHmuKXHtbY5wMXC{b4DvfJkqeGinbonsLYFk\XSrYzDhZ4llNWmwZIXj[YQh\mG|IH3SUmEh\XiycnXzd4lwdiCrbjDoeY1idiCKZYDHNkBk\WyuczDheEA2ODBibl2= M4LiSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6OECwO|Y4Lz5zOEiwNFc3PzxxYU6=
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RAW264.7 MorvSpVv[3Srb36gZZN{[Xl? NHG1XJIyKHWP M1rG[mlvcGmkaYTpc44hd2ZiTGDTMZN1cW23bHH0[YQhdnWlbHXhdkBkdy2{ZYDy[ZN{d3JicnXs[YF{\SCocn;tJIlPV1NicILvcY91\XJiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XRiMTD1UUBjgSCUVD3QR3I> NGTjPZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
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SJ-GBM2 MYLxTHRUKGG|c3H5 NIrtVotyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> M{HN[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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SK-N-MC M3ntR5FJXFNiYYPzZZk> NIm1V41yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> M{LvdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 Mm[3dWhVWyCjc4PhfS=> MoXwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| M3XNelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 Mkf6dWhVWyCjc4PhfS=> MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NUCzOFJZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MUPxTHRUKGG|c3H5 NIPsUGlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NHewcWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 M13mepFJXFNiYYPzZZk> MoDVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| Ml3mQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 Ml25dWhVWyCjc4PhfS=> MnLldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M33WV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD MYHxTHRUKGG|c3H5 MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NGO1S3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) NGC5dplyUFSVIHHzd4F6 NFS0RnlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= M1jve|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 MU\xTHRUKGG|c3H5 M2PLVZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| MkHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NXi1SFV2eUiWUzDhd5NigQ>? NHPMVVFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= M2rS[FxiKHSjcnfleF0oZ2KuYX7rK{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]
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  • 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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To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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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