(+)-JQ1

Catalog No.S7110

For research use only.

(+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.

(+)-JQ1 Chemical Structure

CAS No. 1268524-70-4

Selleck's (+)-JQ1 has been cited by 321 publications

Purity & Quality Control

Choose Selective Target Protein Ligand Inhibitors

Biological Activity

Description (+)-JQ1 is a BET bromodomain inhibitor, with IC50 of 77 nM/33 nM for BRD4(1/2) in cell-free assays, binding to all bromodomains of the BET family, but not to bromodomains outside the BET family. (+)-JQ1 suppresses cell proliferation via inducing autophagy. (+)-JQ1 inhibits the expression of Nuclear receptor binding SET domain protein 3 (NSD3) target genes.
Features (+)-JQ1 is more effective than (-)-JQ1.
Targets
BRD4 (2) [1]
(Cell-free assay)
BRD4 (1) [1]
(Cell-free assay)
33 nM 77 nM
In vitro

(+)-JQ1 enantiomer binds directly into the Kac binding site of BET bromodomains. (+)-JQ1 (500 nM) binds BRD4 competitively with chromatin resulting in differentiation and growth arrest of NMC cells. (+)-JQ1 (500 nM) attenuates rapid proliferation of NMC 797 and Per403 cell lines as demonstrated by reduced Ki67 staining. (+)-JQ1 (500 nM) potently decreases expression of both BRD4 target genes in NMC 797 cells. (+)-JQ1 inhibits cellular viability with IC50 of 4 nM in NMC 11060 cells. [1] (+)-JQ1 results in robust inhibition of MYC expression in MM cell lines. (+)-JQ1 inhibits proliferating of KMS-34 and LR5 with IC50 of 68 nM and 98 nM, respectively. (+)-JQ1 (500 nM)-treated MM.1S cells results in a pronounced decrease in the proportion of cells in S-phase, with a concomitant increase in cells arrested in G0/G1. (+)-JQ1 (500 nM) results in pronounced cellular senescence by beta-galactosidase staining. (+)-JQ1 (800 nM) exposure leads to a significant reduction in cell viability among the majority of CD138+ patient-derived MM samples tested. [2] (+)-JQ1 inhibits growth of LP-1 cells with GI50 of 98 nM. (+)-JQ1 (625 nM) results in an increase in the percentage of LP-1 cells in G0/G1. (+)-JQ1 (500 nM) suppresses the expression of MYC, BRD4 and CDK9 in LP-1 cells. [3] (+)-JQ1 (1 μM) activates HIV transcription in latently infected Jurkat T cells. (+)-JQ1 (50 μM) stimulates predominantly Tat-dependent HIV transcription in both Jurkat and HeLa cells. (+)-JQ1 (5 μM) induces Brd4 dissociation enables Tat to recruit SEC to HIV promoter and induce Pol II CTD phosphorylation and viral transcription in J-Lat A2 cells. JQ1 enables Tat to increase CDK9 T-loop phosphorylation and partially dissociates P-TEFb from 7SK snRNP in Jurkat T cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
K1  NUHxSlZZS2WubDDWbYFjcWyrdImgRZN{[Xl? MXuyOVAwPTByL{GwNFAhdk1? NWX3[oZOOjRxNEivO|IhcA>? M3\RbGROW09? NEPIVo5qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDpckBjd3SqIHTvd4UuKGGwZDD0bY1mNSCmZYDlcoRmdnRibXHucoVz NF;0e|A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkewO|g5OSd-Mk[3NFc5QDF:L3G+
BCPAP MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NW[5OVd2OjVyL{WwNE8yODByIH7N MX2yOE81QC95MjDo MV7EUXNQ MU\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCrbjDic5RpKGSxc3WtJIFv\CC2aX3lMUBl\XCnbnTlcpQhdWGwbnXy NYSyWnZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3NFc5QDFpPkK2O|A4QDhzPD;hQi=>
K1  M4HUNGNmdGxiQ4njcIUhSXO|YYm= MoCwNlUxNzVyMD:xNFAxKG6P MXm3NkBp NVLFVppkTE2VTx?= NY\LTotw[XK{ZYP0d{Bk\WyuIHP5Z4xmKGG2IFewM2cyKHCqYYPl MmjvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5MEe4PFEoRjJ4N{C3PFgyRC:jPh?=
BCPAP M3jnNmNmdGxiQ4njcIUhSXO|YYm= NE\aPWozPTBxNUCwM|ExODBibl2= M3v1[|czKGh? NGDteYRFVVOR MlfSZZJz\XO2czDj[YxtKGO7Y3zlJIF1KEdyL1exJJBp[XOn NGPNO2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkewO|g5OSd-Mk[3NFc5QDF:L3G+
Hep3B Ml31S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmTONE0yOCEQvF2= MYm1JIQ> M1vROGROW09? MX\JR|UxRTBwMEig{txO MmD3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3N{WxOlcoRjJ4NUe1NVY4RC:jPh?=
HCCLM3 NHnO[41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMVExKM7:TR?= MXu1JIQ> NFLGOHpFVVOR MWHJR|UxRTBwMUSg{txO NX;qOpFzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1O|UyPjdpPkK2OVc2OTZ5PD;hQi=>
HuH7 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMVExKM7:TR?= NWHpSJhoPSCm M1HncGROW09? NF[3WnBKSzVyPUCuNlEh|ryP MnLpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3N{WxOlcoRjJ4NUe1NVY4RC:jPh?=
HepG2 Ml3XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[wSVAuOTBizszN NYLSPZpzPSCm M3HENWROW09? NFHlc5ZKSzVyPUCuN|Qh|ryP M{[5XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUe1NVY4Lz5{NkW3OVE3PzxxYU6=
SMMC7721 M1;TZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XKSFAuOTBizszN MXW1JIQ> NWjaSWROTE2VTx?= MlTHTWM2OD1yLkSxJO69VQ>? M3fPfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUe1NVY4Lz5{NkW3OVE3PzxxYU6=
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MHCC97H M{jXUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfvTJR2OC1zMDFOwG0> MlHtOUBl M1jhN2ROW09? MXrJR|UxRTBwNEGg{txO MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjV5NUG2O{c,OjZ3N{WxOlc9N2F-
Hep3B NGDyXIJE\WyuIFP5Z4xmKEG|c3H5 M3TaWFAvOS9yLkWvNk42KM7:TR?= M{nzS|Q5KGh? NHzZNJRFVVOR NVTn[It3dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZiSFPDJINmdGy|IHnuJJN2[i2JMTDwbIF{\cLi M3\VWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NUe1NVY4Lz5{NkW3OVE3PzxxYU6=
HCCLM3 NU\wS|RES2WubDDDfYNt\SCDc4PhfS=> NWjDdm5YOC5zL{CuOU8zNjVizszN M3TPSlQ5KGh? M4[1UGROW09? M3jnPIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKEiFQzDj[YxteyCrbjDzeYIuTzFicHjhd4XDqA>? Mn7MQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ3N{WxOlcoRjJ4NUe1NVY4RC:jPh?=
Hep3B NUi4WWlJSXCxcITvd4l{KEG|c3H5 NWPLRoVJOC5zL{CuOU8zNjVizszN M4XHV|Q5KGh? NX\2eIp[TE2VTx?= M3jkU4FkfGm4YYTld{Bk[XOyYYPlMVMh[W6mIHPhd5Bie2VvOTDlfJBz\XO|aX;uJIFv\CCrbnT1Z4VlKFCDUmCgZ4xm[X[jZ3WgZZMhf2WubDDhd{BkgXSxY3jyc41mKGNicnXs[YF{\SCrboTvJJRp\SCleYTvdIxie21iZoLvcUBucXSxY3jvcoRzcWF? NEfCUGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkW3OVE3Pyd-Mk[1O|UyPjd:L3G+
HCCLM3 MYrBdI9xfG:|aYOgRZN{[Xl? NIP6VIUxNjFxMD61M|IvPSEQvF2= NGDXOXU1QCCq NHexfllFVVOR Mki3ZYN1cX[jdHXzJINie3Cjc3WtN{BidmRiY3HzdIF{\S17IHX4dJJme3Orb36gZY5lKGmwZIXj[YQhWEGUUDDjcIVifmGpZTDhd{B4\WyuIHHzJIN6fG:laILvcYUh[yC{ZXzlZZNmKGmwdH:geIhmKGO7dH;wcIF{dSCocn;tJI1qfG:laH;u[JJq[Q>? NVvEeXRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[1O|UyPjdpPkK2OVc2OTZ5PD;hQi=>
A549 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7TeFZZOC5zLUGwJO69VQ>? MXq3NkBp NF3KZlNqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MofsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2MUWyNlUoRjJ4NEG1NlI2RC:jPh?=
H157 NEjkUGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHnlNGkxNjFvMUCg{txO NYnNTIl[PzJiaB?= M4jJe4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVrCRnhMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NVUzOjVpPkK2OFE2OjJ3PD;hQi=>
H1299 NX7JT5UyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1O0NVAvOS1zMDFOwG0> NYPXTXllPzJiaB?= NXLZPFRscW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWTFXYx6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NVUzOjVpPkK2OFE2OjJ3PD;hQi=>
A549 NFnWUFZHfW6ldHnvckBCe3OjeR?= MVexM|IvPS93IN88US=> NWHHfZN[OTJiaB?= NGr5T5PDqHenYXvsfUBl\WO{ZXHz[YQhSmOuLUKgcIV3\Wy| MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjRzNUKyOUc,OjZ2MUWyNlU9N2F-
H1299 NWD6b21sTnWwY4Tpc44hSXO|YYm= MmL6NU8zNjVxNTFOwG0> M2fNbVEzKGh? NEf4NFHDqHenYXvsfUBl\WO{ZXHz[YQhSmOuLUKgcIV3\Wy| NEnuVmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSxOVIzPSd-Mk[0NVUzOjV:L3G+
H157 NEDaPFVHfW6ldHnvckBCe3OjeR?= NInVNG0yNzJwNT:1JO69VQ>? MXqxNkBp NUn1dGRR\GWlcnXhd4VlKESUNDDlfJBz\XO|aX;u MlHPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2MUWyNlUoRjJ4NEG1NlI2RC:jPh?=
H1299 M13TfmZ2dmO2aX;uJGF{e2G7 MnvyNU8zNjVxNTFOwG0> MXWxNkBp M1nCXIRm[3KnYYPl[EBFWjRiZYjwdoV{e2mxbh?= NEPXT3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSxOVIzPSd-Mk[0NVUzOjV:L3G+
C8161 NVLjZpJKS2WubDDWbYFjcWyrdImgRZN{[Xl? Ml7BNE0zKM7:TR?= NXKxOHJQPCCm NFPkdpNFVVOR NWPxVW9C\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUeyNlMoRjJ4M{m3NlI{RC:jPh?=
Mel285 M2\GcGNmdGxiVnnhZoltcXS7IFHzd4F6 M1rzNVAuOiEQvF2= NHvhUHk1KGR? NULGOZloTE2VTx?= MVPk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7N{KyN{c,OjZ|OUeyNlM9N2F-
Mel290 MU\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmfUNE0zKM7:TR?= NIHEWVQ1KGR? NY\rOoZoTE2VTx?= NULORnVG\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7N{KyN{c,OjZ|OUeyNlM9N2F-
92.1 MkfBR4VtdCCYaXHibYxqfHliQYPzZZk> MWWwMVIh|ryP M{Wwc|Qh\A>? MVjEUXNQ Mnf1[IVkemWjc3XzJINmdGxidnnhZoltcXS7IHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NVP0b45xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVczOjNpPkK2N|k4OjJ|PD;hQi=>
Omm1.3 MULD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MV6wMVIh|ryP MXG0JIQ> MlrWSG1UVw>? M2jvZ4Rm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NVLIZWZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVczOjNpPkK2N|k4OjJ|PD;hQi=>
Mel202 M{PDT2NmdGxiVnnhZoltcXS7IFHzd4F6 NFnJ[W0xNTJizszN MYW0JIQ> NV7TVXBDTE2VTx?= MUDk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7N{KyN{c,OjZ|OUeyNlM9N2F-
Mel270 M1zHVWNmdGxiVnnhZoltcXS7IFHzd4F6 M3z5c|AuOiEQvF2= NVXNUpR{PCCm NHnTVW5FVVOR MXrk[YNz\WG|ZYOgZ4VtdCC4aXHibYxqfHliaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NEXkeYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5O|IzOyd-Mk[zPVczOjN:L3G+
Omm1 MlqxR4VtdCCYaXHibYxqfHliQYPzZZk> Mkm3NE0zKM7:TR?= M{T4VVQh\A>? NYG5VItxTE2VTx?= NV7VdodZ\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M2fWT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{m3NlI{Lz5{NkO5O|IzOzxxYU6=
92.1 NETPUYJCeG:ydH;zbZMhSXO|YYm= MlHXOVAxKG6P NIjL[og1QCCq MlvnSG1UVw>? M3ezcolv\HWlZYOgZZBweHSxc3nz MmW4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OUeyNlMoRjJ4M{m3NlI{RC:jPh?=
Omm1.3 NF\vZnFCeG:ydH;zbZMhSXO|YYm= M2LPblUxOCCwTR?= MX60PEBp M1XUSGROW09? M1niWYlv\HWlZYOgZZBweHSxc3nz NHzFZYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5O|IzOyd-Mk[zPVczOjN:L3G+
92.1 MVHD[YxtKEO7Y3zlJGF{e2G7 M37QRVUxOCCwTR?= M3\Yd|I1NzR6L{eyJIg> MXfEUXNQ Mk\ibY5lfWOnczD0bIUh[2WubDDhZ4N2dXWuYYTpc44h[XRic4XiMWcyyqB? M3O2[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{m3NlI{Lz5{NkO5O|IzOzxxYU6=
Omm1.3 NWTmeoxLS2WubDDDfYNt\SCDc4PhfS=> MWK1NFAhdk1? MkW5NlQwPDhxN{KgbC=> NU\oTFVMTE2VTx?= MYrpcoR2[2W|IITo[UBk\WyuIHHjZ5VufWyjdHnvckBifCC|dXKtS|HDqA>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7N{KyN{c,OjZ|OUeyNlM9N2F-
A549 MVvGeY5kfGmxbjDBd5NigQ>? M{O5RlExOC92MECvNVAxOCCwTR?= MXiyOEBp NH3HeG92eHKnZ4XsZZRmeyCjbnSgZYN1cX[jdHXzJHNKWlRz NFjz[oY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkKxNlE6QSd-Mk[yNVIyQTl:L3G+
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Rosetta2 DE3 M2n3e2Z2dmO2aX;uJIF{e2G7 NFLlT2hM\CB;IECuNFA3OiEQvF2= NXTJSFNXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[wPFAxPjRpPkK2NFgxODZ2PD;hQi=>
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Rosetta2 DE3 MY\GeY5kfGmxbjDhd5NigQ>? MX7L[EA:KDBwMEC2O{DPxE1? MoK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
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Rosetta2 DE3 M2jUPWZ2dmO2aX;uJIF{e2G7 MonGT4QhRSByLkCxNlgh|ryP MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
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Rosetta2 DE3 MYXGeY5kfGmxbjDhd5NigQ>? MVrL[EA:KDBwMEG0O{DPxE1? M3jOTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
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MV4-11 MmXFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYK3NkBp MULJR|UxKD1iMD6wNlMh|ryP MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV3OUSyPEc,OjV3NUm0Nlg9N2F-
MV4-11 NF;PTGlEgXSxdH;4bYNqfHliYYPzZZk> NXLqbG0zPCCmYYnz Mn3OTWM2OCB;IECuNFI1KM7:TR?= MkLTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2NkO0PFcoRjJ6NE[zOFg4RC:jPh?=
MV4-11 NUSwRoQ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUG0JIRigXN? NF\zUoZKSzVyIE2gNE4xOjRizszN NFnEPZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkC4NFA3PCd-Mk[wPFAxPjR:L3G+
Rosetta2 DE3 M1;WNGZ2dmO2aX;uJIF{e2G7 M3rwelMxKG2rboO= NX\FNWpQUUN3MDC9JFAvODJ6NzFOwG0> MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjB6MEC2OEc,OjZyOECwOlQ9N2F-
NALM16 MV;DfZRwfG:6aXPpeJkh[XO|YYm= MV:1JIRigXN? NV3TWWZITUN3MDC9JFAvODNizszN NGDWbpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUG3NFAzPCd-MkmxO|AxOjR:L3G+
BL21(DE3)-R3-pRARE2 MlXCSpVv[3Srb36gZZN{[Xl? MU[zNEBucW6| M1faXWlEPTBiPTCwMlA{OyEQvF2= NH;kTIk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5OVczOyd-MkixPVU4OjN:L3G+
BL21(DE3) NFv3TodHfW6ldHnvckBie3OjeR?= NHjDWFVM\CB;IECuNFM1KM7:TR?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd|MUS5NEc,OjZ5M{G0PVA9N2F-
Rosetta2 DE3 MlzsSox2d3Knc3PlcoNmKHCxbHHybZpifGmxbjDhd5NigQ>? NVK1ZZB1OzBibXnudy=> NF2yeXdKSzVyIE2gNE4xOzV5IN88US=> MoiwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZyOECwOlQoRjJ4MEiwNFY1RC:jPh?=
Rosetta2 DE3 NH32fmpHdHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 NXu5THBKOzBibXnudy=> MUDJR|UxKD1iMD6wOFIzKM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDR4M{S4O{c,Ojh2NkO0PFc9N2F-
Rosetta2 DE3 M4HyOGZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gZZN{[Xl? MUGzNEBucW6| MXHJR|UxKD1iMD6wOFY4KM7:TR?= M2HQb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NE[zOFg4Lz5{OES2N|Q5PzxxYU6=
MOLM13 NFjDeJdEgXSxdH;4bYNqfHliYYPzZZk> MlzwOEBl[Xm| MVHJR|UxKD1iMD6wOVYh|ryP MnmwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh2NkO0PFcoRjJ6NE[zOFg4RC:jPh?=
MOLM13 MoK3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYCyUmZDPCCmYYnz NVP2[nFrUUN3MDC9JFAvODV4IN88US=> M2PrfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MEiwNFY1Lz5{NkC4NFA3PDxxYU6=
HL60 NGXOfHRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= Mnz1O|IhcA>? MoTNTWM2OCB;IECuNFYh|ryP MlH5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzN{CwNlQoRjJ7MUewNFI1RC:jPh?=
HL60 MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLnN{Bl[Xm| NFvFZllISzVyIE2gNE4xPiEQvF2= NYrMZlF[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm2OVcxQTlpPkK5OlU4ODl7PD;hQi=>
NALM6 MWHDfZRwfG:6aXPpeJkh[XO|YYm= NEW3XmM2KGSjeYO= NIe3SJVGSzVyIE2gNE4xPiEQvF2= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV2OUi4PUc,Ojh3NEm4PFk9N2F-
Raji MknkSpVv[3Srb36gZZN{[Xl? MVjJR|UxKD1iMD6wOkDPxE1? NV\KNFlxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3N|E1QTBpPkK2O|MyPDlyPD;hQi=>
Raji MlzRSpVv[3Srb36gZZN{[Xl? MUW0JIg> M1u4cmlEPTBiPTCwMlA3QSEQvF2= NWnZ[nd[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA4PThpPkK0PVAxPzV6PD;hQi=>
MM1S NED5eYlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MkLJO|IhcA>? NU\PenlCUUN3MDC9JFAvODZ7MTFOwG0> NXfaO4RQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
BL21 (DE3)-codon plus-RIL NIK5SFdHdHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 MWfifUBndHWxcnXzZ4Vv[2ViYX7pd491em:yeTDhd5NigQ>? NYjE[VdTUUN3MDC9JFAvODdizszN MojvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3OE[3NVgoRjJ6NUi2O|E5RC:jPh?=
22Rv1 M4X0WmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NF;tSlE6PiCq NFjRT2ZKSzVyIE2gNE4xPzFizszN NWXlTXlYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
22Rv1 MmS4RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? M4jxVFEzKGh? NUO2U4c{UUN3MDC9JFAvODdzIN88US=> M{P2N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUSxN|cyLz5{OUW0NVM4OTxxYU6=
MV4-11 NFjtWI1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MWHJR|UxKD1iMD6wO|Ih|ryP NFjrVI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEG5OVczOyd-MkixPVU4OjN:L3G+
BL21(DE3)-R3-pRARE2 Mn[0SpVv[3Srb36gZZN{[Xl? MlrpN|AhdWmwcx?= MkPyTWM2OCB;IECuNFc4KM7:TR?= NV3aPJFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[3N|E1QTBpPkK2O|MyPDlyPD;hQi=>
BL21(DE3)-R3-pRARE2 MV;GeY5kfGmxbjDhd5NigQ>? NGHIRZM{OCCvaX7z M1iycWlEPTBiPTCwMlA4PyEQvF2= M2jFN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUm1O|I{Lz5{OEG5OVczOzxxYU6=
BL21(DE3)-R3-pRARE2 M1T1VmZ2dmO2aX;uJIF{e2G7 NFroRlY{OCCvaX7z MnjFTWM2OCB;IECuNFc4KM7:TR?= NHu0OI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe3Olg{PCd-Mkm3O|Y5OzR:L3G+
MV4-11 NEK2eVBEgXSxdH;4bYNqfHliYYPzZZk> NYi5Zll6OjRiaB?= MVvHTVUxKD1iMD6wPEDPxE1? MmH6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzOUGzOlMoRjJ4MUmxN|Y{RC:jPh?=
MV411 NFnzbHJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= MkHvO|IhcA>? MYLJR|UxKD1iMD6wPEDPxE1? NVTLd4F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizNVQ2OTNpPkK4N|E1PTF|PD;hQi=>
TY82 NH;GPXZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= Mn3UO|IhcA>? MoOxTWM2OCB;IECuNFgxQCEQvF2= NUW0SFE6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1NlU1OzVpPkK5OVI2PDN3PD;hQi=>
HL60 NFi3WHNHfW6ldHnvckBie3OjeR?= M175VFI1KGh? NFrSU4pKSzVyIE2gNE4xQDZizszN MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDV2OUi4PUc,Ojh3NEm4PFk9N2F-
697 M4jVeGN6fG:2b4jpZ4l1gSCjc4PhfS=> NV3aO2oxPSCmYYnz MUDFR|UxKD1iMD6wPUDPxE1? NY\KPHFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxO|AxOjRpPkK5NVcxODJ2PD;hQi=>
Loucy NHPFOlZEgXSxdH;4bYNqfHliYYPzZZk> NULQb|RTPSCmYYnz NUW4NGliTUN3MDC9JFAvODlizszN NWTmVpRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxO|AxOjRpPkK5NVcxODJ2PD;hQi=>
BL21(DE3) M{nvPGZ2dmO2aX;uJIF{e2G7 MmeyT4QhRSByLkC5NkDPxE1? NXrVcWVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm1OFE{PzFpPkK5OVQyOzdzPD;hQi=>
BL21(DE3)-R3-pRARE2 M{HPdWZ2dmO2aX;uJIF{e2G7 NYm5dlBsU2RiPTCwMlEh|ryP M{mweFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NUm1NFA4Lz5{OEW5OVAxPzxxYU6=
HT-29 NVrK[|BKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HYSVczKGh? MlvOTWM2OCB;IECuNVA1KM7:TR?= M4\LcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NUW5OFI5Lz5{NUW1PVQzQDxxYU6=
MM1S Mnq4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYe3NkBp Mn\4TWM2OCB;IECuNVA6KM7:TR?= NHqyTYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW1PVQzQCd-MkW1OVk1Ojh:L3G+
LNCAP cells Mn\sRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MXrJR|UxKD1iMD6xNFk3KM7:TR?= MknaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
T cells NHnjZ|dHfW6ldHnvckBie3OjeR?= NIHJcXkzPCCq M1LTW2lEPTBiPTCwMlEyKM7:TR?= M2f1[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{G0OVE{Lz5{OEOxOFUyOzxxYU6=
HL60 NIO5[lRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NUPWToRFPzJiaB?= M3TyVGlEPTBiPTCwMlEyKM7:TR?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjh4OUG5OEc,OjZ6NkmxPVQ9N2F-
BL21(DE3) NYj3OYVJTnWwY4Tpc44h[XO|YYm= MnrlTWM2OCB;IECuNVIh|ryP M2GwXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{OxOFkxLz5{NkezNVQ6ODxxYU6=
BL21(DE3) NWC4[IxpTnWwY4Tpc44h[XO|YYm= NUPZR3N5Oi53IHi= NFr2VoxKSzVyIE2gNE4yOiEQvF2= M{XMOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NUSxN|cyLz5{OUW0NVM4OTxxYU6=
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HD-MB03 M33ic2N6fG:2b4jpZ4l1gSCjc4PhfS=> NF;TWGw2KGSjeYO= MVzFR|UxKD1iMD6xOkDPxE1? MkLQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
LNCAP Mn\wRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MoLsPVYhcA>? MmXyTWM2OCB;IECuNVYh|ryP NGTP[mU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe1PFUyQCd-Mkm3OVg2OTh:L3G+
Hs578T MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? MYSxNkBp MkTaTWM2OCB;IECuNVYh|ryP NEfaSow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe1PFUyQCd-Mkm3OVg2OTh:L3G+
MV4-11 M{HQNmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIF{e2G7 NXjVb493OTJiaB?= NH33bVFKSzVyIE2gNE4yPiEQvF2= NVPaclBYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkmxO|AxOjRpPkK5NVcxODJ2PD;hQi=>
LNCAP MUTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDhd5NigQ>? NUTtSVdNOTJiaB?= NEfIZ5lKSzVyIE2gNE4yPiEQvF2= MkOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl3NEGzO|EoRjJ7NUSxN|cyRC:jPh?=
C4-2B MkH6RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZZN{[Xl? MUS5OkBp MWHJR|UxKD1iMD6xPUDPxE1? Ml7YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NUi1NVgoRjJ7N{W4OVE5RC:jPh?=
C4-2B NFH3VYFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBie3OjeR?= NGPq[XgyOiCq MU\JR|UxKD1iMD6xPUDPxE1? NFPoOZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUW0NVM4OSd-Mkm1OFE{PzF:L3G+
Vero E6 M4fIVWFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= MXK0PEBp MYDJR|UxKD1iMD6xPVI4PSEQvF2= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjN3M{i1PUc,OzJ|NUO4OVk9N2F-
MCF7 NWPUcHhZSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= MkThNVIhcA>? MnPXTWM2OCB;IECuNkDPxE1? NUfh[VB3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm3OVg2OThpPkK5O|U5PTF6PD;hQi=>
MV4-11 NVPYUFFiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[XO|YYm= NGHJ[2pKSzVyIE2gNE4zPCEQvF2= NHWwU|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G0Nlc2OSd-MkexOFI4PTF:L3G+
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Assay
Methods Test Index PMID
Western blot pDNA-PKcs / γH2AX / Ub-γH2AX / p-c-Jun S63 / Bax ; c-Myc ; p27 26119999 23792448
Growth inhibition assay Cell viability 23792448
Immunofluorescence GM130 ; MHC / EdU 29074567 28733670
In vivo (+)-JQ1 (50 mg/kg) inhibits tumors growth in mice with NMC 797 xenografts. (+)-JQ1 (50 mg/kg) results in effacement of NUT nuclear speckles in mice with NMC 797 xenografts, consistent with competitive binding to nuclear chromatin. (+)-JQ1 (50 mg/kg) induces strong (grade 31) keratin expression in NMC 797 xenografts. (+)-JQ1 (50 mg/kg) promotes differentiation, tumor regression and prolonged survival in mice models of NMC xenografts. [1] (+)-JQ1 (50 mg/kg) results in a significant prolongation in overall survival of SCID-beige mice orthotopically xenografted after intravenous injection with MM.1S-luc+ cells compared to vehicle-treated animals. [2] (+)-JQ1 (50 mg/kg i.p.) leads to a highly significant increase in survival of mice bearing Raji xenografts. [3]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MC 11060 cells
  • Concentrations: ~500 nM
  • Incubation Time: 48 hours
  • Method:

    Cells are seeded into white, 384-well microtiter plates at 500 cells per well in a total volume of 50 μL media. The 797, TT and TE10 cells are grown in DMEM containing 1% penicillin/streptomycin and 10% FBS. The Per403 cells are grown in DMEM containing 1 % penicillin/streptomycin and 20% FBS. Patient-derived NMC 11060 cells are grown in RPMI with 10% FBS and 1% penicillin/streptomycin. (+)-JQ1 is delivered to microtiter assay plates by robotic pin transfer. Following a 48 hours incubation at 37℃, cells are lysed and wells are assessed for total ATP content using a commercial proliferation assay. Replicate measurements are analyzed with respect to dose and estimates of IC50 are calculated by logistic regression (GraphPad Prism).

Animal Research:

[1]

  • Animal Models: Mice bearing NMC 797 xenografts
  • Dosages: 50 mg/kg
  • Administration: intraperitoneal injection

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 456.99
Formula

C23H25ClN4O2S

CAS No. 1268524-70-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C

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

Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions

Question 1:
How can I reconstitute the compound for in vivo injection?

Answer:
JQ1 does not dissolve in water/PBS. The vehicle we recommend is 2% DMSO+30% PEG 300+5% Tween 80+ddH2O. The compound can be dissolved in the vehicle at 5mg/ml and you can use it for IV injection.

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