Nutlin-3

For research use only.

Catalog No.S1061

36 publications

Nutlin-3 Chemical Structure

Molecular Weight(MW): 581.5

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 36 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 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXpOJBQPcLizszN NXmwPZZmPDkEoHi= MlToZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ NXzUVHpzOjZ|NUC1OlU>
NP69 M2PtZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTNzLk[5xtEzNjV2IN88US=> M4KwTlI3OjV{NUe1
NP460 NHrKNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTJ{Lki1xtEyNjF6IN88US=> MWiyOlI2OjV5NR?=
C666-1 NUG2[HBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\0TWM2OD1zOT65OeKyQC57MzFOwG0> NV3jWlJ7OjZ{NUK1O|U>
C666-1 MnvTR4VtdCCYaXHibYxqfHliQYPzZZk> MoXHNVAhyrWP NVK2cHJ7PDhiaB?= MlfZSG1UVw>? NInkZ2d{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDjbZNxdGG2aX6= NYH1WWI4OjZ{NUK1O|U>
C666-1  M3nFb2Z2dmO2aX;uJGF{e2G7 NIHmenUyOCEEtV2= NYDIVXduOjRiaB?= M3vRbmROW09? M13GeYFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? NVTTXXpmOjZ{NUK1O|U>
C666-1 MX3BdI9xfG:|aYOgRZN{[Xl? NVjCcXV3OTBiwsXN MlWxOFgwPzJiaB?= M13RTmROW09? NXy4TZFFe2Wwc3n0bZpmeyCFNk[2MVEh[2WubIOgeI8h[2m|cHzheIlvNWmwZIXj[YQh[XCxcITvd4l{ M{TGXFI3OjV{NUe1
A549 NIHoZlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7wXJQzPCCq MXXJR|UxRTF5Lk[4JOKyKDRwNUKg{txO NVTrUXBsOjZzMkWyN|A>
A549-NTC MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHvkb4szPCCq NIHyZm5KSzVyPUG5MlQzKMLzIEGuPVYh|ryP NU\TfXN5OjZzMkWyN|A>
A549-920 M{P6R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFv2UlIzPCCq M1XiVGlEPTB;M{OuPFUhyrFiND64OEDPxE1? NETSZWozPjF{NUKzNC=>
CRL-5908 NFO1O2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHWTI5JOjRiaB?= MYPJR|UxRTN6LkexJOKyKDJwNEOg{txO MluzNlYyOjV{M{C=
L6 NVXLUWdbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnThNVDDqM7:TdMg NGP5PFYzPC92OD:3NkBp Mme3SG1UVw>? MmrqbY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v NG\2dogzPTh5MUe5OC=>
C2C12 M33lRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHkNJR6OTEEoN88UeKh NI\0d3gzPC92OD:3NkBp MUHEUXNQ NISwcmFqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? NWL4UoY{OjV6N{G3PVQ>
MCF-7  NWjqWXV5TnWwY4Tpc44hSXO|YYm= MUKxNOKh|ryP MkTxSG1UVw>? MlXkbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh MYeyOVcxOjdyMx?=
DU4475  Mo\3SpVv[3Srb36gRZN{[Xl? M1HqSFUwOTBxMkCg{txO M2\QVFI1yqCq MUDkc5dvemWpdXzheIV{KFSxY3GtNUBld3OnIHTldIVv\GWwdHz5 M1LYdVI2PTR5MUe0
SMMC-7721 MVzGeY5kfGmxbjDBd5NigQ>? MnX6NVAh|ryP M1XTeVQ5KGh? MUHEUXNQ NHPZZ|Vk[XW|ZYOgSG5CKESVQjDkZY1i\2V? MX:yOVU1PDN4MR?=
SMMC-7721 M4X0TWZ2dmO2aX;uJGF{e2G7 NEfO[JEyOCEQvF2= M3vxWVQ5KGh? M4fwWmROW09? MWTpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg MoLYNlU2PDR|NkG=
SMMC-7721 M4K5O2Z2dmO2aX;uJGF{e2G7 MkjDNVAh|ryP NXTVc5RsPDhiaB?= NH3LOI5FVVOR MnyzbY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:owrDJSm5DOcLibWLORS=> NHPuUXkzPTV2NEO2NS=>
SMMC-7721 NEO5W5pHfW6ldHnvckBCe3OjeR?= MUWxNEDPxE1? NWfiO|ZIOzZiaB?= NGfzO45FVVOR M2XTcYNifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 Mlf3NlU2PDR|NkG=
MCF-7 MmDCSpVv[3Srb36gRZN{[Xl? MlXBNVDDqM7:TR?= Mn[5NE0zPCCq NYficXVXcW6mdXPld{BxPTNiYX7kJJAzOS:FaYCx MnTENlU1QDJ|N{O=
OVCAR10 NXXqUZduTnWwY4Tpc44hSXO|YYm= MUKxNOKh|ryP MnznNlFpyqB? MlT1SG1UVw>? MWnpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NGjFO|kzPTR{NkW0PC=>
NCI-H23 NWjSOlhTTnWwY4Tpc44hSXO|YYm= NYDpeVlROTEEoN88US=> MmT6NlFpyqB? MY\EUXNQ M3yyRYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> NEjSUVczPTR{NkW0PC=>
A2780 MW\GeY5kfGmxbjDBd5NigQ>? NUTtRmZwOTEEoN88US=> MorGNlFpyqB? NFr0NJdFVVOR M37IcYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> MoPQNlU1OjZ3NEi=
NCI-H23 NXTPSZl7TnWwY4Tpc44hSXO|YYm= M2G1V|ExyqEQvF2= NFPmWYczOWkEoB?= MYrEUXNQ NXHaelN7\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> NYXsNXRmOjV2Mk[1OFg>
A2780 MXrGeY5kfGmxbjDBd5NigQ>? M4X5R|ExyqEQvF2= MoruNlFpyqB? M{jX[2ROW09? MonK[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= MXeyOVQzPjV2OB?=
HCT116  MW\GeY5kfGmxbjDBd5NigQ>? NG[yW3EyOCEEtV2= Mm\NNlQhcA>? NYD3OXp7[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 M4TJXlI2OzhyMEW1
MCF-10CA1a NIDNeFNHfW6ldHnvckBCe3OjeR?= MVyxNOKh|ryP M2\KPFQ5KGh? MnTFSG1UVw>? NWrIfmNOcW6qaXLpeJMh[mG|YXygbY53[XOrb36gZY5lKHKnZIXj[YQhXEeILd8yN{1qdmS3Y3XkJIlvfmG|aX;uJJRwKGKjc3HsJIxmfmWucx?= MViyOVI2Pzd{OR?=
MCF-10A1  NIK1WGRHfW6ldHnvckBCe3OjeR?= Ml7qNVDDqM7:TR?= NF3rXZIzPC92ODDo MXjEUXNQ Moi5bY5pcWKrdIOgcYloemG2aX;uJI9nKG6xcn3hcEBjemWjc4Sg[ZBqfGinbHnhcOKh MlrNNlUzPTd5Mkm=
MCF-10CA1a MUnGeY5kfGmxbjDBd5NigQ>? MlHqNVDDqM7:TR?= NFO4OIUzPCCq NF3oOZVFVVOR NEnq[IRl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= MUKyOVI2Pzd{OR?=
MCF-10CA1a MmXnSpVv[3Srb36gRZN{[Xl? M2XhdFExyqEQvF2= Ml[5NlQhcA>? MnG3SG1UVw>? NF;MXWZqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NFTCTnQzPTJ3N{eyPS=>
SK-BR-7 MoDFSpVv[3Srb36gRZN{[Xl? NGfrU4oyOMLizszN MVuyOEBp MmOwSG1UVw>? MXLpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? M4nDOFI2OjV5N{K5
SUM102PT NYD3OmhrTnWwY4Tpc44hSXO|YYm= Mm[1NVDDqM7:TR?= M2rWXlI1KGh? NU\KOo9rTE2VTx?= NVPwV|JVcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MnHCNlUzPTd5Mkm=
RAW 264.7 MkLkSpVv[3Srb36gRZN{[Xl? NWDwUmQxOTEEoN88US=> NFXsUVg{OCCvaX6= MVTwdoV3\W62czD0bIUheDV|IILl[JVkfGmxbjDpckBz\XOyb37z[UB1dyCOUGO= MVGyOVE4OjV2Nx?=
RAW 264.7 MXvGeY5kfGmxbjDBd5NigQ>? Mnn3NVDDqM7:TR?= NH;MUXA{OCCvaX6= MkTndoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= MlXGNlUyPzJ3NEe=
RAW 264.7 NUHMW|dDTnWwY4Tpc44hSXO|YYm= M4HXflExyqEQvF2= MnTWN|AhdWmw MUXpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= M1HpPFI2OTd{NUS3
MCF7  M1q4U2NmdGxiVnnhZoltcXS7IFHzd4F6 NIjRV4szNjViwsXN M2S1UFUh\A>? NYPRRVNYTE2VTx?= NHWyZY1{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u NHu5NnozPTB6NUmwNi=>
MCF7  NWW5NXRFTnWwY4Tpc44hSXO|YYm= MljmNk42KML3TR?= MVO0PEBp M3PZPGROW09? MVvk[YNz\WG|ZYOgeIhmKGixbX;sc4dwfXNiRGPCJJJmeGGrcjDmdoVyfWWwY3nldy=> NH;MVXozPTB6NUmwNi=>
ACHN MkC2R4VtdCCYaXHibYxqfHliQYPzZZk> MWGwMlUuOTBizszN M3nnUVAuPiCm NEfPdGRFVVOR NGrSOYxqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M2jEOlI2ODZ5N{i3
Caki-2 NX7yXpFvS2WubDDWbYFjcWyrdImgRZN{[Xl? M3\F[|AvPS1zMDFOwG0> M1XI[FAuPiCm M3jQUGROW09? MnL5bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1\3clI2ODZ5N{i3
A498 Mo[xR4VtdCCYaXHibYxqfHliQYPzZZk> NGjuUosxNjVvMUCg{txO NGrEXIkxNTZiZB?= MWTEUXNQ NGqxOo1qdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHO4W2YzPTB4N{e4Oy=>
115 MmS5R4VtdCCYaXHibYxqfHliQYPzZZk> MVywMlUuOTBizszN MVqwMVYh\A>? NVyyWXZzTE2VTx?= MWLpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2r4fVI2ODZ5N{i3
117 NVy4WZFGS2WubDDWbYFjcWyrdImgRZN{[Xl? MWKwMlUuOTBizszN NHTE[5QxNTZiZB?= NF;qO4lFVVOR NV\E[IQ1cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NF\lZnAzPTB4N{e4Oy=>
ACHN M1TVPWZ2dmO2aX;uJGF{e2G7 M{CxbFAvPS9zL{Wg{txO NUHNUHY2PDhiaB?= M2DWU2ROW09? NVn3fG5kdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NFzXRXQzPTB4N{e4Oy=>
Caki-2 MoTXSpVv[3Srb36gRZN{[Xl? NVrG[mJlOC53L{GvOUDPxE1? MWO0PEBp MlvkSG1UVw>? Ml31cIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MnTqNlUxPjd5OEe=
A498 NEfaU4ZHfW6ldHnvckBCe3OjeR?= MnjnNE42NzFxNTFOwG0> MWO0PEBp MVPEUXNQ M1TMSoxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NGPxXngzPTB4N{e4Oy=>
115 NIrFelRHfW6ldHnvckBCe3OjeR?= MmGyNE42NzFxNTFOwG0> MlzxOFghcA>? MXPEUXNQ MUns[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NH7DR|UzPTB4N{e4Oy=>
ACHN M4nNcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzoSYZyPSEQvF2= M2PqOlQ5KGh? M4TVZ2ROW09? M4WyV4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MmLuNlUxPjd5OEe=
Caki-2 M4rBXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1JO69VQ>? MUm0PEBp M2nnTWROW09? NF7JR|JqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> M3\zSVI2ODZ5N{i3
A498 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe1JO69VQ>? MVu0PEBp NVPu[o9CTE2VTx?= MXrpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MXGyOVA3Pzd6Nx?=
115 NUHTdFIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml6yOUDPxE1? MoTyOFghcA>? NILYWnRFVVOR NXPROm81cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh M2\JWlI2ODZ5N{i3
ACHN NXPRNYJJTnWwY4Tpc44hSXO|YYm= MYi1JO69VQ>? NWHaNY5HPDhiaB?= MlPiSG1UVw>? MYTpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MnHVNlUxPjd5OEe=
Caki-2 Ml;0SpVv[3Srb36gRZN{[Xl? MXy1JO69VQ>? NEXUPI81QCCq NYPmZWxlTE2VTx?= M3exNIlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NFvKc4ozPTB4N{e4Oy=>
A498 NXnnWGN2TnWwY4Tpc44hSXO|YYm= MorOOUDPxE1? M1nU[FQ5KGh? NYXUUJlFTE2VTx?= MX7pcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NVG3[GFUOjVyNke3PFc>
115 MlrhSpVv[3Srb36gRZN{[Xl? MWi1JO69VQ>? MlTHOFghcA>? NICyNVBFVVOR M1vXbYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NVj3fJE3OjVyNke3PFc>
MOLM-13 M4SxVWZ2dmO2aX;uJGF{e2G7 M3XSPFbDqM7:TR?= Mn3TNE05KGh? MWLEUXNQ MVHpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> MYiyOFg5PTB6Mh?=
MOLM-13 NHnKS2hHfW6ldHnvckBCe3OjeR?= MV:2xsDPxE1? MkjkOkBp MX;EUXNQ NX3PXGpz\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> MnzTNlQ5QDVyOEK=
HepG2 NXHueVVZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T6TFczKGh? NHq0cIpFVVOR MYXJR|UxRTN3Lki2JOKyKDJwOTFOwG0> MoPoNlQ5QDR6MEm=
HepG2/As NGrZOYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfTfnJMPzJiaB?= MlnXSG1UVw>? MYjJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> M3H2WVI1QDh2OEC5
SMMC7721 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEP0WVQ4OiCq M1zaVmROW09? MXLJR|UxRTNzLkK4JOKyKDRwMjFOwG0> NXj2dJBSOjR6OES4NFk>
SMMC7721/Ac MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX63NkBp M4f2eGROW09? Mlq1TWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MWmyOFg5PDhyOR?=
Huh-7 NE\YcWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXQO|IhcA>? MUXEUXNQ NXL2Npo4UUN3ME2zN{46PiEEsTCzMlkh|ryP M17NdFI1QDh2OEC5
Hep3B M2\jW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTNO|IhcA>? MUHEUXNQ NHnJXGNKSzVyPUKwMlE5KMLzIEGuPFQh|ryP MWSyOFg5PDhyOR?=
HepG2 M17XUmFxd3C2b4Ppd{BCe3OjeR?= MmTJbY5lfWOnczDhdI9xfG:|aYO= Mn\xNlQ5QDR6MEm=
SMMC7721 MUDBdI9xfG:|aYOgRZN{[Xl? NIj1RW5qdmS3Y3XzJIFxd3C2b4Ppdy=> M4nIW|I1QDh2OEC5
Huh-7 NHri[5pCeG:ydH;zbZMhSXO|YYm= NUjCZnZocW6mdXPld{BieG:ydH;zbZM> MlfoNlQ5QDR6MEm=
Hep3B M{fy[2Fxd3C2b4Ppd{BCe3OjeR?= NHHrSVBqdmS3Y3XzJIFxd3C2b4Ppdy=> NYHz[mhVOjR6OES4NFk>
U2OS  NHq2PIFHfW6ldHnvckBCe3OjeR?= NXHqfoJ[OjBizszN MXWyOEBp M33tTIlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= NXHkcndxOjR6NkeyOVk>
AML2 NXfMcVYzSXCxcITvd4l{KEG|c3H5 NGTrNGYzNzFyIN88US=> NUHoXGFSOjRxNEigbC=> M2DSTolv\HWlZYOgZZBweHSxc3nz NITsdokzPDZ3OUe0PS=>
MOML13 NXLQTWlzSXCxcITvd4l{KEG|c3H5 NF7rOXgzNzFyIN88US=> NXntO5p[OjRxNEigbC=> NILkZ3pqdmS3Y3XzJIFxd3C2b4Ppdy=> NFzQdIczPDZ3OUe0PS=>
AML2 NXvpc2hyTnWwY4Tpc44hSXO|YYm= M1;K[lEx|ryP MkXINk81KGh? NVezRWpHcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> M{TTU|I1PjV7N{S5
AML3 M1i4[mZ2dmO2aX;uJGF{e2G7 MVuxNO69VQ>? M3TSSlIwPCCq MU\pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= NUXJfoI1OjR4NUm3OFk>
MOML13 NHnN[I5HfW6ldHnvckBCe3OjeR?= Mnv3NVDPxE1? M2XSV|IwPCCq M1HrZolv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NIjzVGozPDZ3OUe0PS=>
BeWo M1S2TGZ2dmO2aX;uJGF{e2G7 NF3GTG0{OCEEtV2= NV;1eZB{OjRiaB?= MoLMbY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs MUmyOFQ6QDF3NB?=
BeWo NEnIeJNCeG:ydH;zbZMhSXO|YYm= NVLkbXptOzBiwsXN NUXMRoxGOjRiaB?= NETkSHVqdmO{ZXHz[ZMh[XCxcITvd4l{ M1flVlI1PDl6MUW0
OCI NVzaWpdFTnWwY4Tpc44hSXO|YYm= MYSxNEDPxE1? M1fjOFI1KGh? M2C2eJVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NGLhWYczPDR5M{W2Ni=>
MOLM MmHBSpVv[3Srb36gRZN{[Xl? MonONVAh|ryP NInveFIzPCCq M4\HPZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NVrpOGQzOjR2N{O1OlI>
U2OS  MVrGeY5kfGmxbjDBd5NigQ>? MVuyNEDPxE1? MWSyOEBp NG\nVWlqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NFrJ[|gzPDN4NkCwOy=>
RKO NHHJeI5HfW6ldHnvckBCe3OjeR?= NH3OWnUzOCEQvF2= NUHMc3hWOjRiaB?= NYf0Z4FUcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= MkT2NlQ{PjZyMEe=
U2OS  MVrGeY5kfGmxbjDBd5NigQ>? M1;mblIxKM7:TR?= MnPzNlQhcA>? NEmwWlVqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MXiyOFM3PjByNx?=
RKO NHToXlhHfW6ldHnvckBCe3OjeR?= M{PYRVIxKM7:TR?= NYjO[Y8yOjRiaB?= MoPIbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MUiyOFM3PjByNx?=
SMMC-7721  M{T5cmNmdGxiVnnhZoltcXS7IFHzd4F6 MVGxMlI2NTJyIN88US=> M4r4VFI1NzR6L{eyJIg> M1rYSmROW09? MYDpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MnfDNlQzQDZ|MUK=
HuH-7 MkDaR4VtdCCYaXHibYxqfHliQYPzZZk> NIrUV2gyNjJ3LUKwJO69VQ>? M1nTbVI1NzR6L{eyJIg> MYHEUXNQ NXvuVplIcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MorYNlQzQDZ|MUK=
SMMC-7721  MnL1RZBweHSxc3nzJGF{e2G7 NVz3VlYxOjBizszN NVK0[HhoPDhiaB?= M4XLe2ROW09? NGjFR2FqdmS3Y3XzJIFxd3C2b4Ppdy=> Mm\zNlQzQDZ|MUK=
HuH-7 NFnzPGJCeG:ydH;zbZMhSXO|YYm= M37wflIxKM7:TR?= MUO0PEBp MV;EUXNQ M4H1[4lv\HWlZYOgZZBweHSxc3nz NXq4dpRROjR{OE[zNVI>
SMMC-7721  NY\UOHcxTnWwY4Tpc44hSXO|YYm= NX;PZVFMOTBizszN MXuzOkBp NGPpVohFVVOR NGPUOIJld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? NXv0b|d[OjR{OE[zNVI>
HuH-7 M1rVVmZ2dmO2aX;uJGF{e2G7 M3nqZlExKM7:TR?= NUXQSlV2OzZiaB?= M{W3b2ROW09? NXvnZ3Fx\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NVnQbmdOOjR{OE[zNVI>
AT2 M1TKNGZ2dmO2aX;uJGF{e2G7 NWPtZpBXPS9zMDFOwG0> MYPs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? M1rx[lI1OjRyMkCz
REH NHXEWotHfW6ldHnvckBCe3OjeR?= MkfmOU8yOCEQvF2= NHrSfGxt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= NH3BZXUzPDJ2MEKwNy=>
UoCB6 M{fNW2Z2dmO2aX;uJGF{e2G7 NEPQUJA2NzFyIN88US=> MmjRcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? MoC0NlQzPDB{MEO=
AT2 MWPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3mxNVAuOjVizszN NInadWJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MnHuNlQzPDB{MEO=
REH NXWwb2ltS2WubDDWbYFjcWyrdImgRZN{[Xl? NGPJeYcxNTJ3IN88US=> M1fkfolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MnvhNlQzPDB{MEO=
UoCB6 MXHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUSwMVI2KM7:TR?= MXTpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NHn0ZoMzPDJ2MEKwNy=>
A2780 MY\GeY5kfGmxbjDBd5NigQ>? MVq1M|ExNzJyIN88US=> M{nSdVI1KGh? NIr0VW12eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= NF;EVVYzPDF|NkG0Oy=>
H460 NU\hVGtzTnWwY4Tpc44hSXO|YYm= MmfzOU8yOC9{MDFOwG0> NGSzeW0zPCCq MXz1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? Mke5NlQyOzZzNEe=
Lovo  NIW1TlZHfW6ldHnvckBCe3OjeR?= MVm1M|ExNzJyIN88US=> MVKyOEBp MU\1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? M4rvTVI1OTN4MUS3
A2780 MYjBdI9xfG:|aYOgRZN{[Xl? NEn3OIc2NzFyL{KwJO69VQ>? MkHUNlQhcA>? NXL6XYdi\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MXiyOFE{PjF2Nx?=
H460 NHe0O2lCeG:ydH;zbZMhSXO|YYm= M{DBRlUwOTBxMkCg{txO M2fGdFI1KGh? MWrlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> M3npb|I1OTN4MUS3
Lovo  NF:yW2xCeG:ydH;zbZMhSXO|YYm= NXHYfoZKPS9zMD:yNEDPxE1? MkTMNlQhcA>? MkLQ[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MVeyOFE{PjF2Nx?=

... 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 COC1=CC(=C(C=C1)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)OC(C)C

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% 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