GW3965 HCl

Name: GW3965 HCl
Brand: Selleck Chemicals
SKU: S2630
Rating: 5 (31 reviews)

For research use only.

Catalog No.S2630

31 publications

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

Science, 2018, 359(6376):684-688

PubMed: 29301957 ( click the link to review the publication )

Nature, 2016, 14;535(7611):303-7.

PubMed: 27383786 ( click the link to review the publication )

J Med Chem, 2021, 64(14):9943-9959

PubMed: 34251816 ( click the link to review the publication )

ACS Chem Biol, 2021, 16(1):136-149

PubMed: 33378170 ( click the link to review the publication )

Life Sci, 2021, 276:119434

PubMed: 33785343 ( click the link to review the publication )

Infect Immun, 2021, IAI.00788-20

PubMed: 33593888 ( click the link to review the publication )

Front Cell Dev Biol, 2020, 8:609090

PubMed: 33490072 ( click the link to review the publication )

Front Pharmacol, 2020, 27;11:375

PubMed: 32292349 ( click the link to review the publication )

Int Immunopharmacol, 2020, 90:107240

PubMed: 33310663 ( click the link to review the publication )

Clin Sci (Lond), 2020, 134(2):273-287

PubMed: 31957803 ( click the link to review the publication )

Neurotherapeutics, 2020, Apr 15

PubMed: 32297184 ( click the link to review the publication )

Nat Commun, 2019, 11;10(1):4621

PubMed: 31604910 ( click the link to review the publication )

EMBO Mol Med, 2019, 11(10):e10769

PubMed: 31468706 ( click the link to review the publication )

Cells, 2019, 8(12)E1601

PubMed: 31835444 ( click the link to review the publication )

J Neuroinflammation, 2019, 16(1):132

PubMed: 31255170 ( click the link to review the publication )

Neoplasia, 2019, 22(1):1-9

PubMed: 31751859 ( click the link to review the publication )

Am J Transl Res, 2019, 11(3):1498-1509

PubMed: 30972177 ( click the link to review the publication )

Redox Biol, 2019, 21:101069

PubMed: 30576926 ( click the link to review the publication )

Exp Neurol, 2018, 304:21-29

PubMed: 29447944 ( click the link to review the publication )

Immunol Cell Biol, 2018, 96(3):298-315

PubMed: 29345385 ( click the link to review the publication )

Mol Cell Endocrinol, 2018, 474:48-56

PubMed: 29454584 ( click the link to review the publication )

Biochem Cell Biol, 2018, 96(1):11-18

PubMed: 29024600 ( click the link to review the publication )

Exp Ther Med, 2018, 16(3):1814-1824

PubMed: 30186406 ( click the link to review the publication )

J Clin Invest, 2017, 127(2):583-592

PubMed: 28094767 ( click the link to review the publication )
Arch Toxicol, 2017, 91(1):271-287

PubMed: 27052460 ( click the link to review the publication )

Sci Rep, 2017, 7(1):2303

PubMed: 28536436 ( click the link to review the publication )

Cytokine, 2017, 91:30-37

PubMed: 27987394 ( click the link to review the publication )

Arch Virol, 2016, 161(9):2491-501

PubMed: 27357231 ( click the link to review the publication )

J Cell Biochem, 2016, 117(10):2272-80

PubMed: 26917453 ( click the link to review the publication )

FEBS Lett, 2015, 589(1):52-8

PubMed: 25436422 ( click the link to review the publication )

FEBS Lett, 2015, 589(1):52-8

PubMed: ( click the link to review the publication )

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	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-
RAW264.7	NYLMc2NmTnWwY4Tpc44h[XO\|YYm=	M2C1UlEhfU1?		MmPQTY5pcWKrdHnvckBw\iCOUGOtd5RqdXWuYYTl[EBvfWOuZXHyJINwNXKncILld5NweiC{ZXzlZZNmKG[{b32gbW5QWyCycn;tc5RmeiCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{BifCBzIIXNJIJ6KFKWLWDDVi=>	NUL6T4VNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NFA4PjdpPkG4PFAxPzZ5PD;hQi=>
HeLa	MUfGeY5kfGmxbjDhd5NigQ>?	M4\lSlEhfU1?		MluxTY5lfWO2aX;uJI9nKEy[UnLleIEhW1WPT4nsZZRqd25iYomgV3VOVzJiaX6gbJVu[W5iSHXMZUBk\WyuczDheEAyKHWPIHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	NF[0N2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
HeLa	MWTGeY5kfGmxbjDhd5NigQ>?	M2[xXVEhfU1?		MkHPTY5lfWO2aX;uJI9nKEy[UnLleIEhW1WPT4nsZZRqd25iYomgV3VOVzNiaX6gbJVu[W5iSHXMZUBk\WyuczDheEAyKHWPIHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>?	NEfkeGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
HeLa	Mln4SpVv[3Srb36gZZN{[Xl?	NIOy[lYyKHWP		NEfjRldKdmS3Y4Tpc44hd2ZiTGjSZYxxcGFiU2XNU5lt[XSrb36gZpkhW1WPT{OgbY4hcHWvYX6gTIVN[SClZXzsd{BifCBzIIXNJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?=	NGL0N5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEiwNFc3Pyd-MUi4NFA4Pjd:L3G+
DAOY	NF:3TY5yUFSVIHHzd4F6			NF7xXmlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?=	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SJ-GBM2	MmHHdWhVWyCjc4PhfS=>			MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?=	M3XDWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673	MlTLdWhVWyCjc4PhfS=>			MVXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>?	NWLm[4xXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC	NX\EfFlXeUiWUzDhd5NigQ>?			MkXrdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	MmLuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	M2D1PZFJXFNiYYPzZZk>			M4XRXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
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?=
SK-N-SH	M1X3NpFJXFNiYYPzZZk>			NYjiR4pPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-12	M1XEXJFJXFNiYYPzZZk>			MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	Mnf2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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 PLoS One 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 Mol Cell Biol 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 Mol Cell Biol 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 Haematologica 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 PLoS One 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 C_max of 12.7 μg/mL and t_1/2 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)

References

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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 Download GW3965 HCl SDF

Molecular Weight	618.51
Formula	C₃₃H₃₁ClF₃NO₃.HCl
CAS No.	405911-17-3
Storage	3 years-20°C powder 2 years-80°C 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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mg/kg

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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

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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.

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.

Bio Calculators

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)

*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

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 )

* 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
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
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Molecular Weight Calculator

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

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Molarity Calculator

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.

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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GW3965 HCl