Nutlin-3

Catalog No.S1061

For research use only.

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.

Nutlin-3 Chemical Structure

CAS No. 890090-75-2

Selleck's Nutlin-3 has been cited by 83 publications

Purity & Quality Control

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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
SMMC-7721  NUCwS4k2TnWwY4Tpc44hSXO|YYm= M{nSc|ExKM7:TR?= MUezOkBp M2HnWWROW09? MkSy[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 NVvPTWdqSXCxcITvd4l{KEG|c3H5 MoHjNlAh|ryP NXTwTGFGPDhiaB?= NIjjd5FFVVOR NV3HPIJ3cW6mdXPld{BieG:ydH;zbZM> NFnSbGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
SMMC-7721  NYn3SZFCSXCxcITvd4l{KEG|c3H5 M3na[|IxKM7:TR?= M2H6dlQ5KGh? MlXCSG1UVw>? MWXpcoR2[2W|IHHwc5B1d3Orcx?= NXnVO|dZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 NEDyTWJE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXuxMlI2NTJyIN88US=> NHLr[IQzPC92OD:3NkBp MkXySG1UVw>? NGHyRpRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
SMMC-7721  NIC1PWVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn;sNU4zPS1{MDFOwG0> Ml7pNlQwPDhxN{KgbC=> NWXjSVFxTE2VTx?= MmfWbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NGL5bnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
RKO NILCN|FHfW6ldHnvckBCe3OjeR?= MWOyNEDPxE1? MoTTNlQhcA>? NWTWS2RMcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MknBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
U2OS  M4DGd2Z2dmO2aX;uJGF{e2G7 MWKyNEDPxE1? NI\xfZMzPCCq MV;pcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= NUm0SGM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlYxODdpPkK0N|Y3ODB5PD;hQi=>
RKO MUjGeY5kfGmxbjDBd5NigQ>? NHWwVYEzOCEQvF2= MWeyOEBp NH3wV5dqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NkCwO{c,OjR|Nk[wNFc9N2F-
U2OS  MkfhSpVv[3Srb36gRZN{[Xl? NET6UWQzOCEQvF2= MXqyOEBp M3Xhc4lv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? MnXYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
MOLM NGfJ[lJHfW6ldHnvckBCe3OjeR?= MVixNEDPxE1? MUOyOEBp NHL4W4d2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MoXvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
OCI MnzQSpVv[3Srb36gRZN{[Xl? MV2xNEDPxE1? MXqyOEBp NXL2bldwfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u M3;H[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEezOVYzLz5{NES3N|U3OjxxYU6=
BeWo NUC5bXE4SXCxcITvd4l{KEG|c3H5 M3OwTVMxKML3TR?= NIDteHAzPCCq NVPxPGRLcW6lcnXhd4V{KGGyb4D0c5Nqew>? NIDQOYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5PFE2PCd-MkS0PVgyPTR:L3G+
BeWo MVnGeY5kfGmxbjDBd5NigQ>? NISzWZA{OCEEtV2= MorGNlQhcA>? NHrlVIhqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> NXzB[HBJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVgyPTRpPkK0OFk5OTV2PD;hQi=>
MOML13 MXvGeY5kfGmxbjDBd5NigQ>? MmO0NVDPxE1? M{[4blIwPCCq MmPxbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= M1jlZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
AML3 MYXGeY5kfGmxbjDBd5NigQ>? Mny0NVDPxE1? MnLXNk81KGh? NFnlVJBqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NGLoNZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 NYj1PJRuTnWwY4Tpc44hSXO|YYm= NFXhbI8yOM7:TR?= MVmyM|QhcA>? M3vNeolv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NHHQOos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
MOML13 NFH2Uo9CeG:ydH;zbZMhSXO|YYm= NETDeXMzNzFyIN88US=> MnrFNlQwPDhiaB?= NHTqeHdqdmS3Y3XzJIFxd3C2b4Ppdy=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OUe0PUc,OjR4NUm3OFk9N2F-
AML2 MnT0RZBweHSxc3nzJGF{e2G7 NVrx[HcxOi9zMDFOwG0> M3LL[VI1NzR6IHi= M2izU4lv\HWlZYOgZZBweHSxc3nz M4\WfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
U2OS  M3PQZmZ2dmO2aX;uJGF{e2G7 NGnMW5QzOCEQvF2= MmjzNlQhcA>? M33OUIlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K1PUc,OjR6NkeyOVk9N2F-
Hep3B MkfjRZBweHSxc3nzJGF{e2G7 M4XtTolv\HWlZYOgZZBweHSxc3nz NEH3eHE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
Huh-7 NWL2PY9KSXCxcITvd4l{KEG|c3H5 NWPIPJY2cW6mdXPld{BieG:ydH;zbZM> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721 M2qwcWFxd3C2b4Ppd{BCe3OjeR?= NGHRNnVqdmS3Y3XzJIFxd3C2b4Ppdy=> NFTaSmc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2 NF3Gc4FCeG:ydH;zbZMhSXO|YYm= M{jlW4lv\HWlZYOgZZBweHSxc3nz MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Hep3B NGXGVIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL3O3A4OiCq MknQSG1UVw>? NFzudppKSzVyPUKwMlE5KMLzIEGuPFQh|ryP NUDUblJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
Huh-7 NXjzb2t2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf6W|V6PzJiaB?= NFThRZRFVVOR MkTtTWM2OD1|Mz65OkDDuSB|Lkmg{txO NYjVUo1VRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
SMMC7721/Ac NVy4RY9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXaO|IhcA>? MoPQSG1UVw>? MmjkTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MkXaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
SMMC7721 NI\MN4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rOS|czKGh? NHTLTYtFVVOR NXnPZlJPUUN3ME2zNU4zQCEEsTC0MlIh|ryP M4TWZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2/As MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTFTYU4OiCq MX3EUXNQ MVXJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> M3LpTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[3NkBp MoLISG1UVw>? NUDoe3QyUUN3ME2zOU45PiEEsTCyMlkh|ryP NUH0bYZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
MOLM-13 NUG5bIpqTnWwY4Tpc44hSXO|YYm= MnnlOuKh|ryP Mm\EOkBp MVnEUXNQ M1T3[oVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= NUHXXY11RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFUxQDJpPkK0PFg2ODh{PD;hQi=>
MOLM-13 MYDGeY5kfGmxbjDBd5NigQ>? MkjmOuKh|ryP NEDldXoxNThiaB?= NV32PIlkTE2VTx?= M3vjNYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? NWD3eldCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFUxQDJpPkK0PFg2ODh{PD;hQi=>
115 Ml;6SpVv[3Srb36gRZN{[Xl? MnPWOUDPxE1? M2n6NFQ5KGh? M4nVd2ROW09? NFzkZWZqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M3vuVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 MVrGeY5kfGmxbjDBd5NigQ>? M160WVUh|ryP MXK0PEBp NUDmV4o6TE2VTx?= MYHpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi Mn7NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 NHTRcG5HfW6ldHnvckBCe3OjeR?= M2\2fVUh|ryP M1;CVFQ5KGh? NHq1NYVFVVOR MoPybY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MoDYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
ACHN MVrGeY5kfGmxbjDBd5NigQ>? M3HOXFUh|ryP NFi5V201QCCq MoDLSG1UVw>? M1HoUIlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
115 M1LFWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK1JO69VQ>? MVe0PEBp M4rlV2ROW09? MUjpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MnS2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
A498 M2nNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXMXYg3PSEQvF2= MVy0PEBp MVPEUXNQ MVLpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NIHSWoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
Caki-2 MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:1JO69VQ>? MYS0PEBp MYnEUXNQ M3L4[4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M4ewbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
ACHN NH;wenBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGji[oE2KM7:TR?= NF\pNnE1QCCq M1\aW2ROW09? M4\FTIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MljaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 MW\GeY5kfGmxbjDBd5NigQ>? NFqweosxNjVxMT:1JO69VQ>? NIDYNGg1QCCq M4X3[GROW09? MlnJcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
A498 M3;CSGZ2dmO2aX;uJGF{e2G7 NVnHd5hMOC53L{GvOUDPxE1? NV65b2c3PDhiaB?= M3fNS2ROW09? NHTyUFht\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NH;4eHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
Caki-2 NV3Ycnd2TnWwY4Tpc44hSXO|YYm= MUewMlUwOS93IN88US=> M3vsO|Q5KGh? MVLEUXNQ NWWyUmdGdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MmXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
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UoCB6 NU\UR3JKTnWwY4Tpc44hSXO|YYm= MVe1M|ExKM7:TR?= M3TIfYxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MlPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NECyNFMoRjJ2MkSwNlA{RC:jPh?=
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H460 NX:wb|c3TnWwY4Tpc44hSXO|YYm= M4rHSFUwOTBxMkCg{txO NWO4bIxzOjRiaB?= Mn;weZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NHv2PZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOlE1Pyd-MkSxN|YyPDd:L3G+
Lovo  NFPSWYJHfW6ldHnvckBCe3OjeR?= MljUOU8yOC9{MDFOwG0> MUOyOEBp NHHxVXZ2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= NGLKXXQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOlE1Pyd-MkSxN|YyPDd:L3G+
A2780 NYXJbGdzSXCxcITvd4l{KEG|c3H5 NUnmWVlGPS9zMD:yNEDPxE1? NFrkWngzPCCq M4rm[IVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M3S4bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO2NVQ4Lz5{NEGzOlE1PzxxYU6=
H460 MUHBdI9xfG:|aYOgRZN{[Xl? MUe1M|ExNzJyIN88US=> MVGyOEBp MorS[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> NVe3UXVYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|YyPDdpPkK0NVM3OTR5PD;hQi=>
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U87MG M2ixWmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MV20PEBpenN? NHzONYlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGW4O21IKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDJR|UxKD1iNj61JO69VS5? NXW2eXFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewOVA4QDJpPkK3NFUxPzh{PD;hQi=>
U343MG NIK1ZWhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MkK3OFghcHK| NHPnUphCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGWzOFNOTyClZXzsd{BmgHC{ZYPzbY5oKHerbHSgeJlx\SCyNUOgZYZ1\XJiNEigbJJ{KGK7IF3UV{Bie3OjeTygTWM2OCB;IEGyMlYh|ryPLh?= Mkn0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNUC3PFIoRjJ5MEWwO|gzRC:jPh?=
SW620 MkS0R5l1d3SxeHnjbZR6KGG|c3H5 NHGz[XI4OiCqcoO= NXfsepBKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW1d4MkCgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDBwM{ig{txONg>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
A549 NY\6b2ZjS3m2b4TvfIlkcXS7IHHzd4F6 MVi3NkBpenN? NF\nTXJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjRzIN88UU4> NG\UVnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5EcEWPQly8M4E,
SJSA1 MkLVR5l1d3SxeHnjbZR6KGG|c3H5 NGjVOlg4OiCqcoO= MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{Bi\nSncjC3NkBpenNiYomgV3JDKGG|c3H5MEBKSzVyIE2gNU45OSEQvF2u MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
HCT116 MXzDfZRwfG:6aXPpeJkh[XO|YYm= MWS3NkBpenN? NYCxNWdUS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCVUlKgZZN{[XluIFnDOVAhRSB2Lk[zJO69VS5? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
PC3 MW\DfZRwfG:6aXPpeJkh[XO|YYm= M2jOb|czKGi{cx?= MlG3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTC2MlM4KM7:TT6= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxPVE{OzRxJ{7DbGVOSkx:L3G+
Assay
Methods Test Index PMID
Western blot MDM2 / p53 / ALKBH2 / p21 / PUMA ; RRM1 / RRM2 / p53R2 / p21 / p53 / pS6 / S6 23258843 28507282
Immunofluorescence Lamin A / Lamin C / p16 / H3K9me3 ; Merlin / cyclin D1 / p53 / MDM2 ; p53 30728349 30274821 24286312
Growth inhibition assay Cell viability 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

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

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 581.5
Formula

C30H30Cl2N4O4

CAS No. 890090-75-2
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

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

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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.

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