Nutlin-3

For research use only.

Catalog No.S1061

41 publications

Nutlin-3 Chemical Structure

CAS No. 890090-75-2

Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.

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Selleck's Nutlin-3 has been cited by 41 publications

Purity & Quality Control

Choose Selective Mdm2 Inhibitors

Biological Activity

Description Nutlin-3 is a potent and selective Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.
Targets
Mdm2 [5]
(Cell-free assay)
180 nM
In vitro

Nutlin-3 potently inhibits the MDM2-p53 interaction, leading to the activation of the p53 pathway. Nutlin-3 treatment induces the expression of MDM2 and p21, and displays potent antiproliferative activity with IC50 of ~1.5 μM, only in cells with wild-type p53 such as HCT116, RKO and SJSA-1, but not in the mutant p53 cell lines SW480 and MDA-MB-435. In SJSA-1 cells, Nutlin-3 treatment at 10 μM for 48 hours significantly induces caspase-dependent cell apoptosis by ~45%. Although Nutlin-3 also inhibits the growth and viability of human skin (1043SK) and mouse embryo (NIH/3T3) with IC50 of 2.2 μM and 1.3 μM, respectively, cells remain viable 1 week post-treatment even at 10 μM of Nutlin-3, in contrast with the SJSA-1 cells with viability lost at 3 μM of Nutlin-3 treatment. [1] Nutlin-3 does not induce the phosphorylation of p53 on key serine residues and reveals no difference in their sequence-specific DNA binding and ability to transactivate p53 target genes compared with phosphorylated p53 induced by the genotoxic drugs doxorubicin and etoposide, demonstrating that phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis. [2] Although binding less efficiently to MDMX than to MDM2, Nutlin-3 can block the MDMX–p53 interaction and induce the p53 pathway in retinoblastoma cells (Weri1) with IC50 of 0.7 μM. [3] Nutlin-3 at 30 μM also disrupts endogenous p73-HDM2 interaction and enhances the stability and proapoptotic activities of p73, leading to the dose-dependent cell growth inhibition and apoptosis induction in cells without wild-type p53. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzMVZpxPcLizszN MW[0POKhcA>? MmexZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ NI[5bnYzPjN3MEW2OS=>
NP69 NUHzfWZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zUO2lEPTB;M{GuOlnDuTJwNUSg{txO MkjRNlYzPTJ3N{W=
NP460 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTibnY6UUN3ME2yNk45PcLzMT6xPEDPxE1? Mm\lNlYzPTJ3N{W=
C666-1 NHXMdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTF7Lkm1xtE5Njl|IN88US=> NVHNd3pJOjZ{NUK1O|U>
C666-1 MYLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYHUR3RMOTBiwsXN MoXzOFghcA>? MXjEUXNQ MnHqd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw M3PwdlI3OjV{NUe1
C666-1  M{fEZ2Z2dmO2aX;uJGF{e2G7 M3fIR|ExKML3TR?= NVK3PY5jOjRiaB?= M1K2emROW09? NXvteWtF[WO2aY\heIV{KHSqZTDwOVMheGG2aIfhfUwhfXC{ZXf1cIF1cW6pIIC1N{wheDJzIHHu[EBO\G1{ NIeyO3gzPjJ3MkW3OS=>
C666-1 M1TuW2Fxd3C2b4Ppd{BCe3OjeR?= MVixNEDDvU1? MUC0PE84OiCq NXfreI1jTE2VTx?= MWHz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= MVqyOlI2OjV5NR?=
A549 NYrKSpdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrsfJMzPCCq NEXSO3ZKSzVyPUG3MlY5KMLzIESuOVIh|ryP MV[yOlEzPTJ|MB?=
A549-NTC MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDEbHAzPCCq NG\vVZBKSzVyPUG5MlQzKMLzIEGuPVYh|ryP MWOyOlEzPTJ|MB?=
A549-920 NVXUVmJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTrNlQhcA>? MVHJR|UxRTN|Lki1JOKyKDRwOESg{txO MkLINlYyOjV{M{C=
CRL-5908 NWDCZYRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjVe3J{OjRiaB?= M3v5OmlEPTB;M{iuO|EhyrFiMj60N{DPxE1? NUDubGhrOjZzMkWyN|A>
L6 NYnGSm1IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2juTFExyqEQvF5CpC=> MXOyOE81QC95MjDo MVnEUXNQ MXPpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> MmLsNlU5PzF5OUS=
C2C12 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LFO|ExyqEQvF5CpC=> NIq2NVEzPC92OD:3NkBp NVfWOI1mTE2VTx?= NGn0VHpqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MnHVNlU5PzF5OUS=
MCF-7  NGK0PW1HfW6ldHnvckBCe3OjeR?= MnXENVDDqM7:TR?= MlKySG1UVw>? NUn1dZhIcW6qaXLpeJMh[3mlbHnuJGQyKGGwZDDEbYNmesLi NIe1V40zPTdyMkewNy=>
DU4475  MWHGeY5kfGmxbjDBd5NigQ>? NVvNVJZwPS9zMD:yNEDPxE1? MVKyOOKhcA>? NWLaPYE{\G:5boLl[5Vt[XSnczDUc4NiNTFiZH;z[UBl\XCnbnTlcpRtgQ>? NYLJXohjOjV3NEexO|Q>
SMMC-7721 MWHGeY5kfGmxbjDBd5NigQ>? NYLNdWJ1OTBizszN M{HK[lQ5KGh? MV7EUXNQ NFnycGZk[XW|ZYOgSG5CKESVQjDkZY1i\2V? MlHTNlU2PDR|NkG=
SMMC-7721 M2PUWmZ2dmO2aX;uJGF{e2G7 NHLLeXkyOCEQvF2= NWjnR3NqPDhiaB?= MljuSG1UVw>? MkTIbY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> NWPNUXBTOjV3NESzOlE>
SMMC-7721 NX7WNI5tTnWwY4Tpc44hSXO|YYm= MkXvNVAh|ryP Moj4OFghcA>? MkDOSG1UVw>? NXq2dIlWcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NGLGc|czPTV2NEO2NS=>
SMMC-7721 NUXKRohZTnWwY4Tpc44hSXO|YYm= MkXwNVAh|ryP MkLlN|YhcA>? MVnEUXNQ NHztW29k[XW|ZYOgeIhmKGWldH;wbYMh\XiycnXzd4lwdiCxZjDJSmkyPg>? NXzZdYNKOjV3NESzOlE>
MCF-7 NEPUO2ZHfW6ldHnvckBCe3OjeR?= MmHtNVDDqM7:TR?= NWjhSItHOC1{NDDo MknHbY5lfWOnczDwOVMh[W6mIICyNU9EcXBz MlOzNlU1QDJ|N{O=
OVCAR10 MWXGeY5kfGmxbjDBd5NigQ>? MojkNVDDqM7:TR?= MmTuNlFpyqB? NHfRPZNFVVOR MojqbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NWnLS3JrOjV2Mk[1OFg>
NCI-H23 M3XOb2Z2dmO2aX;uJGF{e2G7 MVexNOKh|ryP NFe4N|kzOWkEoB?= MoTPSG1UVw>? Mk\KbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NV\zcGg1OjV2Mk[1OFg>
A2780 MkP6SpVv[3Srb36gRZN{[Xl? NHfvblkyOMLizszN NUDRNFlIOjGqwrC= NHG4TYlFVVOR MmHibY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MYWyOVQzPjV2OB?=
NCI-H23 M2fIOmZ2dmO2aX;uJGF{e2G7 NXn5WYNpOTEEoN88US=> M3rBWFIycMLi NIKwS4tFVVOR NGKz[JBl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> NXX6THhlOjV2Mk[1OFg>
A2780 NIPhNJJHfW6ldHnvckBCe3OjeR?= MX2xNOKh|ryP MYeyNYjDqA>? MmDlSG1UVw>? MVnk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= M{j5dVI2PDJ4NUS4
HCT116  MVrGeY5kfGmxbjDBd5NigQ>? M4HIfVExKML3TR?= NUXwVmpYOjRiaB?= MWHjZZV{\XNiYTDwOVMu\GWyZX7k[Y51KHSndILhdIxwcWRiR{GtZZJz\XO2IHnuJIRqeGyxaXSgTGNVOTF4IHPsc45meyCGMzDhcoQhTDh? M1TtcVI2OzhyMEW1
MCF-10CA1a M3qwcmZ2dmO2aX;uJGF{e2G7 M3z3c|ExyqEQvF2= MUm0PEBp NX\UbW9sTE2VTx?= MlXTbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? M{LrT|I2OjV5N{K5
MCF-10A1  NYf0WmNFTnWwY4Tpc44hSXO|YYm= MYGxNOKh|ryP MWCyOE81QCCq M1XKWGROW09? MW\pcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> NWq1NIcxOjV{NUe3Nlk>
MCF-10CA1a MoDoSpVv[3Srb36gRZN{[Xl? MX[xNOKh|ryP NGHtNVUzPCCq M1LXfGROW09? MXfk[YNz\WG|ZYOgeIhmKFSJRj5OtlMucW6mdXPl[EBuWk6DIHzleoVteyCxZl3NVFItyqCPTWC5MEBidmUEoHnueIVoemmwwrFOtuKhOw>? NGC3V5UzPTJ3N{eyPS=>
MCF-10CA1a NXraUnpiTnWwY4Tpc44hSXO|YYm= MXmxNOKh|ryP MXmyOEBp MnXPSG1UVw>? NX3YeoJbcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u M{jjbVI2OjV5N{K5
SK-BR-7 NIHDOGhHfW6ldHnvckBCe3OjeR?= NV;qcVZTOTEEoN88US=> MWqyOEBp MlrSSG1UVw>? M3;Be4lvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= MUCyOVI2Pzd{OR?=
SUM102PT NGPPd2ZHfW6ldHnvckBCe3OjeR?= NFn4VIIyOMLizszN MoWwNlQhcA>? M1P2PWROW09? MXfpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NETMTlczPTJ3N{eyPS=>
RAW 264.7 NXS1XG9XTnWwY4Tpc44hSXO|YYm= MUKxNOKh|ryP NIP0blI{OCCvaX6= NEDt[3NxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> NY[0PItCOjVzN{K1OFc>
RAW 264.7 MX;GeY5kfGmxbjDBd5NigQ>? NUTkR|ZWOTEEoN88US=> M{DXeVMxKG2rbh?= MUXy[YR2[2W|IITo[UBNWFNvYYXncYVvfGWmIITo[UBPTi4QulKgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHjeIl3cXS7 MkfkNlUyPzJ3NEe=
RAW 264.7 NY\GPG9VTnWwY4Tpc44hSXO|YYm= Ml\JNVDDqM7:TR?= Mn;wN|AhdWmw NW\LUHhycW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh NIDKTWkzPTF5MkW0Oy=>
MCF7  MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NEfwTVkzNjViwsXN MV21JIQ> Ml;DSG1UVw>? NXjBSYw{e2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> M{HBZ|I2ODh3OUCy
MCF7  NXv2T21ETnWwY4Tpc44hSXO|YYm= NIfnNXAzNjViwsXN NY\oeGdjPDhiaB?= MVzEUXNQ NHK5VIxl\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? M2PnflI2ODh3OUCy
ACHN NWPYTHhiS2WubDDWbYFjcWyrdImgRZN{[Xl? M3T5SlAvPS1zMDFOwG0> MmixNE03KGR? M3TPfWROW09? NGTs[HNqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MoThNlUxPjd5OEe=
Caki-2 NWLGcpljS2WubDDWbYFjcWyrdImgRZN{[Xl? NHzDdFQxNjVvMUCg{txO MXSwMVYh\A>? MXHEUXNQ MlvZbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NYPr[mZUOjVyNke3PFc>
A498 MoP1R4VtdCCYaXHibYxqfHliQYPzZZk> NHfnNooxNjVvMUCg{txO MXOwMVYh\A>? MlTOSG1UVw>? M{joPYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUDvUY5MOjVyNke3PFc>
115 NXK2WHF5S2WubDDWbYFjcWyrdImgRZN{[Xl? NF3EPJgxNjVvMUCg{txO NXPDdYpMOC14IHS= MoXGSG1UVw>? M1fwbYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mk\YNlUxPjd5OEe=
117 NUXJd|ROS2WubDDWbYFjcWyrdImgRZN{[Xl? NGLYXWsxNjVvMUCg{txO MYOwMVYh\A>? NXPZR2MxTE2VTx?= MWHpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXnaZ2RbOjVyNke3PFc>
ACHN MYHGeY5kfGmxbjDBd5NigQ>? MlOwNE42NzFxNTFOwG0> M2XhWFQ5KGh? M{jWd2ROW09? NFLTSWJt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MmPGNlUxPjd5OEe=
Caki-2 NW[wWFF4TnWwY4Tpc44hSXO|YYm= NHXpUGExNjVxMT:1JO69VQ>? M2\GRlQ5KGh? Ml\qSG1UVw>? Mly0cIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? Mk[yNlUxPjd5OEe=
A498 NF7PfFVHfW6ldHnvckBCe3OjeR?= MlHONE42NzFxNTFOwG0> M3zZeVQ5KGh? NF3YWVZFVVOR NFO1bopt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MmHmNlUxPjd5OEe=
115 MWjGeY5kfGmxbjDBd5NigQ>? NXvTXIxlOC53L{GvOUDPxE1? NVzYeJVWPDhiaB?= NXO3[FZGTE2VTx?= MX3s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NUW3XXFyOjVyNke3PFc>
ACHN NWDucHlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDuOUDPxE1? NHPBN5M1QCCq NYTYUVNXTE2VTx?= MVjpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MYSyOVA3Pzd6Nx?=
Caki-2 NWTacpY5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn1WoNpPSEQvF2= NX71RWtvPDhiaB?= NGfMU2JFVVOR MXrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= M3;PRVI2ODZ5N{i3
A498 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmG4OUDPxE1? MkL3OFghcA>? NXXYfI1MTE2VTx?= NUP5XXFYcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MXuyOVA3Pzd6Nx?=
115 M1P6[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVK1JO69VQ>? M2PwOlQ5KGh? MlO1SG1UVw>? M3Ox[4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MlOyNlUxPjd5OEe=
ACHN MWjGeY5kfGmxbjDBd5NigQ>? NXjhfI92PSEQvF2= NEHwdJA1QCCq NInoSolFVVOR NIXFOnNqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg Mmf4NlUxPjd5OEe=
Caki-2 MWrGeY5kfGmxbjDBd5NigQ>? NVnNS|ZzPSEQvF2= MX60PEBp MXXEUXNQ NUX6V5oycW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> NEL0W2YzPTB4N{e4Oy=>
A498 MlLtSpVv[3Srb36gRZN{[Xl? M{n6OFUh|ryP M2nGTVQ5KGh? MkHsSG1UVw>? NHrJbpJqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg NG\5VWczPTB4N{e4Oy=>
115 MW\GeY5kfGmxbjDBd5NigQ>? M2e2b|Uh|ryP NUi1bVRzPDhiaB?= M1zZbWROW09? MoXIbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MWKyOVA3Pzd6Nx?=
MOLM-13 NYC0WI0yTnWwY4Tpc44hSXO|YYm= MWW2xsDPxE1? NUHiTnJ4OC16IHi= MoDnSG1UVw>? NV60S4JtcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| MlO1NlQ5QDVyOEK=
MOLM-13 Ml3QSpVv[3Srb36gRZN{[Xl? NYLJ[YxUPsLizszN M4DzO|YhcA>? M3rTdmROW09? MVXlcohidmOnczD0bIUh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINmIh[W6mIHjlZZQhe2ixY3ugdJJwfGWrboOgTJNxOjdiYX7kJGh{eDly MorENlQ5QDVyOEK=
HepG2 M1XhRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoS0O|IhcA>? M1v2NWROW09? MXvJR|UxRTN3Lki2JOKyKDJwOTFOwG0> MkP4NlQ5QDR6MEm=
HepG2/As NIOybphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVK3NkBp NWfQ[ZNuTE2VTx?= MoLzTWM2OD14OD6xN{DDuSB7Lk[g{txO NVrCVYRXOjR6OES4NFk>
SMMC7721 M1TTd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\5c2tHPzJiaB?= MonUSG1UVw>? NHrCS5dKSzVyPUOxMlI5KMLzIESuNkDPxE1? NFnNdpAzPDh6NEiwPS=>
SMMC7721/Ac NYHRRmFuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XpflczKGh? NIOwfolFVVOR NX;a[4N[UUN3ME21OU4zOSEEsTC1MlA{KM7:TR?= NU\QTmtwOjR6OES4NFk>
Huh-7 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfkc444OiCq MkfmSG1UVw>? NFLGXGpKSzVyPUOzMlk3KMLzIEOuPUDPxE1? M2fXclI1QDh2OEC5
Hep3B M3HTVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK3NkBp M4jkXGROW09? NELFSm1KSzVyPUKwMlE5KMLzIEGuPFQh|ryP M1fyOlI1QDh2OEC5
HepG2 NG\SRm1CeG:ydH;zbZMhSXO|YYm= M{Xk[olv\HWlZYOgZZBweHSxc3nz NYHqVpBmOjR6OES4NFk>
SMMC7721 NWmxXJdLSXCxcITvd4l{KEG|c3H5 M4nDT4lv\HWlZYOgZZBweHSxc3nz MUGyOFg5PDhyOR?=
Huh-7 M1rD[mFxd3C2b4Ppd{BCe3OjeR?= MljRbY5lfWOnczDhdI9xfG:|aYO= NX;5O3M3OjR6OES4NFk>
Hep3B M1TaZmFxd3C2b4Ppd{BCe3OjeR?= MXvpcoR2[2W|IHHwc5B1d3Orcx?= MnrZNlQ5QDR6MEm=
U2OS  NF7UWJZHfW6ldHnvckBCe3OjeR?= M{Gxc|IxKM7:TR?= NUfEeGFEOjRiaB?= NGHtNI5qdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX Mmr0NlQ5Pjd{NUm=
AML2 MkPERZBweHSxc3nzJGF{e2G7 NHnLPFYzNzFyIN88US=> MVeyOE81QCCq NEnGXJhqdmS3Y3XzJIFxd3C2b4Ppdy=> MXGyOFY2QTd2OR?=
MOML13 M3m2WWFxd3C2b4Ppd{BCe3OjeR?= M1HiWVIwOTBizszN NYTldFY3OjRxNEigbC=> MVnpcoR2[2W|IHHwc5B1d3Orcx?= M161bFI1PjV7N{S5
AML2 MWrGeY5kfGmxbjDBd5NigQ>? M4XM[VEx|ryP NFvv[oozNzRiaB?= M3r4UYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz M3jIc|I1PjV7N{S5
AML3 Mm[2SpVv[3Srb36gRZN{[Xl? Mm\VNVDPxE1? MXKyM|QhcA>? MWTpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= MnLaNlQ3PTl5NEm=
MOML13 M2HLTmZ2dmO2aX;uJGF{e2G7 MYmxNO69VQ>? M4CwN|IwPCCq M4X4OYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz MYiyOFY2QTd2OR?=
BeWo NXH2NFBzTnWwY4Tpc44hSXO|YYm= MWOzNEDDvU1? MXOyOEBp NELPcHlqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> NHL6cmMzPDR7OEG1OC=>
BeWo NETqVGRCeG:ydH;zbZMhSXO|YYm= MXyzNEDDvU1? MWCyOEBp NWnYXIUxcW6lcnXhd4V{KGGyb4D0c5Nqew>? NUT3cIJHOjR2OUixOVQ>
OCI M4HZPGZ2dmO2aX;uJGF{e2G7 MW[xNEDPxE1? NVT4TGFJOjRiaB?= NXnzPYd3fXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u MnXoNlQ1PzN3NkK=
MOLM NFrXb2VHfW6ldHnvckBCe3OjeR?= MUexNEDPxE1? MXeyOEBp NXTBU|c{fXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NETZXXIzPDR5M{W2Ni=>
U2OS  MnnRSpVv[3Srb36gRZN{[Xl? MmjKNlAh|ryP MW[yOEBp MmPsbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? MXGyOFM3PjByNx?=
RKO NX\zUmR{TnWwY4Tpc44hSXO|YYm= NV:yflUyOjBizszN M{XIS|I1KGh? MlPBbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? NVvM[5VKOjR|Nk[wNFc>
U2OS  MYjGeY5kfGmxbjDBd5NigQ>? MlzNNlAh|ryP NHm5O2MzPCCq NGX2WWZqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> NYL0XGJ2OjR|Nk[wNFc>
RKO MXXGeY5kfGmxbjDBd5NigQ>? MlzyNlAh|ryP NILJ[XIzPCCq NU[5ZXFCcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MVWyOFM3PjByNx?=
SMMC-7721  NInm[lZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NH:yNGsyNjJ3LUKwJO69VQ>? Ml3JNlQwPDhxN{KgbC=> NX6xTphqTE2VTx?= MXLpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M4PJ[lI1Ojh4M{Gy
HuH-7 MVTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnKyNU4zPS1{MDFOwG0> NXrxSIE1OjRxNEivO|IhcA>? M1e0[2ROW09? NWLENWdscW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> Ml3xNlQzQDZ|MUK=
SMMC-7721  NUTsW3BoSXCxcITvd4l{KEG|c3H5 MVmyNEDPxE1? NVLwOGlHPDhiaB?= MXjEUXNQ NVzuS|hWcW6mdXPld{BieG:ydH;zbZM> MXiyOFI5PjNzMh?=
HuH-7 NFjaTHlCeG:ydH;zbZMhSXO|YYm= NF3pUYkzOCEQvF2= M37tUFQ5KGh? MYjEUXNQ MoDobY5lfWOnczDhdI9xfG:|aYO= NGHkclczPDJ6NkOxNi=>
SMMC-7721  NFPIRXRHfW6ldHnvckBCe3OjeR?= M4DXRVExKM7:TR?= NIfONJc{PiCq MoP6SG1UVw>? NIX4Wmdld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? NIi4S|kzPDJ6NkOxNi=>
HuH-7 MlfVSpVv[3Srb36gRZN{[Xl? MkjZNVAh|ryP MmrVN|YhcA>? NXThPZo{TE2VTx?= M2LkU4Rwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ MXyyOFI5PjNzMh?=
AT2 MnjoSpVv[3Srb36gRZN{[Xl? MVe1M|ExKM7:TR?= NVvIcZNRdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NYjJdo9LOjR{NECyNFM>
REH NX:2V2dXTnWwY4Tpc44hSXO|YYm= M1r4WVUwOTBizszN Mk\YcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? M4OxSlI1OjRyMkCz
UoCB6 MWHGeY5kfGmxbjDBd5NigQ>? MYC1M|ExKM7:TR?= M3fTVoxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MYeyOFI1ODJyMx?=
AT2 NXTiVolkS2WubDDWbYFjcWyrdImgRZN{[Xl? NVKzV|BoOC1{NTFOwG0> NHviXHFqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MVWyOFI1ODJyMx?=
REH MnPJR4VtdCCYaXHibYxqfHliQYPzZZk> NHHZcoExNTJ3IN88US=> NVXv[G5UcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MYmyOFI1ODJyMx?=
UoCB6 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4njdFAuOjVizszN M1v1TolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnHwNlQzPDB{MEO=
A2780 MXLGeY5kfGmxbjDBd5NigQ>? MonrOU8yOC9{MDFOwG0> M1zqdVI1KGh? M3fYZZVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NH\HepMzPDF|NkG0Oy=>
H460 MWTGeY5kfGmxbjDBd5NigQ>? NVXkTFBnPS9zMD:yNEDPxE1? MlX0NlQhcA>? M1z0cZVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi MYCyOFE{PjF2Nx?=
Lovo  M1XwZWZ2dmO2aX;uJGF{e2G7 M4\RS|UwOTBxMkCg{txO M4HBdlI1KGh? MWX1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? MlPYNlQyOzZzNEe=
A2780 MX3BdI9xfG:|aYOgRZN{[Xl? NFTXOGw2NzFyL{KwJO69VQ>? MmnvNlQhcA>? MWnlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> NGHydm4zPDF|NkG0Oy=>
H460 MmW1RZBweHSxc3nzJGF{e2G7 NGTKSlE2NzFyL{KwJO69VQ>? NYHPcItsOjRiaB?= NUn2OW5M\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? NUnWTJdSOjRzM{[xOFc>
Lovo  Mn;mRZBweHSxc3nzJGF{e2G7 NXS4TpRwPS9zMD:yNEDPxE1? M{nDNVI1KGh? NWrhZ4FU\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? M3W3VVI1OTN4MUS3

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MDM2 / p53 / ALKBH2 / p21 / PUMA; 

PubMed: 23258843     


CCF-STTG1 cells were treated with the MDM2 antagonist nutlin-3 (0–8 µM) for 24h before cell lysates were collected for western blotting.

RRM1 / RRM2 / p53R2 / p21 / p53 / pS6 / S6; 

PubMed: 28507282     


(A) Rh18 cells were treated with different concentrations of nutlin-3 as indicated for 24 hr. Total proteins were extracted for immunoblotting of RRM1, RRM2, γH2AX, p21, p53R2, p53, S6, pS6-235/6 and 4E-BP1. (B) Rh30 cells were treated with different concentrations of nutlin-3 as indicated for 24 hr. Total proteins were extracted for immunoblotting of RRM1, RRM2, γH2AX, p21, p53R2, p53, S6, pS6-235/6 and 4E-BP1. GAPDH and Actin served as loading controls.

23258843 28507282
Immunofluorescence
Lamin A / Lamin C / p16 / H3K9me3; 

PubMed: 30728349     


c Immunofluorescence images of nuclear deformation and p16 expression after Nutlin-3 treatment for different time period. HCT p53+/− cells were treated with Nutlin-3 (1 μM) for different time (24, 48 h). After treatment, cells were subjected to immunofluorescence staining for Lamin A/C (Red), p16 (Green), and counterstained with DAPI (Blue). dImmunofluorescence images of nuclear deformation and decreased expression of H3K9me3 in HCT p53+/− cells (left). Counting of histone H3K9me3-positive cells (middle) and signal intensities (right) on the basis of IF staining. HCT p53+/− cells were treated with Nutlin-3 (1 μM) for different time (24, 48 h). After treatment, cells were IF stained with Lamin A/C (Red), H3K9me3 (Green), and counterstained with DAPI (Blue). *P < 0.05. 

Merlin / cyclin D1 / p53 / MDM2; 

PubMed: 30274821     


The changes in the subcellular localization of proteins in response to Nutlin-3. Nuclear merlin was indicated with white arrows. Scale bar = 50 μm.

p53; 

PubMed: 24286312     


The subcellular localization of p53 was detected under immunofluorescence microscope (1,000×). The cells were treated as indicated and stained for p53 (red). Nuclei were counterstained with DAPI (blue).

30728349 30274821 24286312
Growth inhibition assay
Cell viability; 

PubMed: 29286113     


Inhibitory effect of nutlin-3 for the cell proliferation after cultivate cells at different concentration for three times (24, 48 and 72 h), respectively.

29286113
In vivo Oral administration of Nutlin-3 at 200 mg/kg twice daily for 3 weeks significantly inhibits the tumor growth of SJAS-1 xenografts by 90%, comparable with the effect of doxorubicin treatment with 81% inhibition of tumor growth. [1]

Protocol

Kinase Assay:

[1]

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Biacore study:

Competition assay is performed on a Biacore S51. A Series S Sensor chip CM5 is utilized for the immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~200 response units (1 response unit corresponds to 1 pg of protein per mm2). The concentration of MDM2 protein is kept constant at 300 nM. Nutlin-3 is dissolved in DMSO at 10 mM and further diluted to make a concentration series of Nutlin-3 in each MDM2 test sample. The assay is run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of Nutlin-3 is calculated as a percentage of binding in the absence of Nutlin-3 and IC50 is calculate
Cell Research:

[1]

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  • Cell lines: HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
  • Concentrations: Dissolved in DMSO, final concentrations ~ 30 μM
  • Incubation Time: 8, 24, and 48 hours
  • Method:

    Cells are exposed to various concentrations of Nutlin-3 for 8, 24 and 48 hours. The transcriptional levels of p21 and MDM2 genes are analyzed by real-time PCR, and protein levels by western blotting. Cell viability is measured by the MTT assay. Cell apoptosis is determined by terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling (TUNEL) staining with flow cytometry and fluorescence microscopy.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
  • Dosages: 200 mg/kg
  • Administration: Orally, twice a day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (171.96 mM)
Ethanol 30 mg/mL (51.59 mM)
Water 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 581.5
Formula

C30H30Cl2N4O4

CAS No. 890090-75-2
Storage powder
in solvent
Synonyms N/A
Smiles CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)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 ()
% DMSO % % Tween 80 % ddH2O
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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)

  • Mass
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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 )

  • C1
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    C2
    V2

* 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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

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

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    Is this a racemic mixture of Nutlin-3a and Nutlin-3b or just the Nutlin-3a enantiomer?

  • Answer:

    It is a racemate.

Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID