Nutlin-3

For research use only.

Catalog No.S1061

58 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 58 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
SMMC-7721  NVvTTnZZTnWwY4Tpc44hSXO|YYm= NYnXVIZnOTBizszN MkHCN|YhcA>? M1\peGROW09? NWfhO|A1\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NFe5TFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
HuH-7 MljoRZBweHSxc3nzJGF{e2G7 NGLMT2szOCEQvF2= MkjBOFghcA>? NHnSdI1FVVOR NVHK[HQ3cW6mdXPld{BieG:ydH;zbZM> M4HIfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
SMMC-7721  NFW1cItCeG:ydH;zbZMhSXO|YYm= MoDsNlAh|ryP NUD2fJhzPDhiaB?= MnLuSG1UVw>? NUHJN4JjcW6mdXPld{BieG:ydH;zbZM> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 NIDjd|VE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2TY[VEvOjVvMkCg{txO NIHLSJozPC92OD:3NkBp M17nc2ROW09? NF[1eFNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M1:1NFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
SMMC-7721  MV7D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MYOxMlI2NTJyIN88US=> M{ThPVI1NzR6L{eyJIg> M{jye2ROW09? NFr3dpJqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MkPtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
RKO M{OzXGZ2dmO2aX;uJGF{e2G7 M3v1elIxKM7:TR?= M2juW|I1KGh? MmjlbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= M1y4O|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{[2NFA4Lz5{NEO2OlAxPzxxYU6=
U2OS  MWDGeY5kfGmxbjDBd5NigQ>? NIG2WIwzOCEQvF2= M{LRbVI1KGh? MXTpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NkCwO{c,OjR|Nk[wNFc9N2F-
RKO MlXXSpVv[3Srb36gRZN{[Xl? MUWyNEDPxE1? NX;XNGR7OjRiaB?= NVfxOo1OcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= NXLhRZpQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlYxODdpPkK0N|Y3ODB5PD;hQi=>
U2OS  MYTGeY5kfGmxbjDBd5NigQ>? NUPqbVJNOjBizszN MkPpNlQhcA>? NEjXbYRqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NGDIXIg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
MOLM Mn\XSpVv[3Srb36gRZN{[Xl? MVuxNEDPxE1? NF22fGgzPCCq NEjVOG92eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MmfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
OCI M3;5XGZ2dmO2aX;uJGF{e2G7 MX:xNEDPxE1? MY[yOEBp NUPmU4pYfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u M{[5bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEezOVYzLz5{NES3N|U3OjxxYU6=
BeWo MnjCRZBweHSxc3nzJGF{e2G7 MoLzN|AhyrWP NXvWV201OjRiaB?= MVrpcoNz\WG|ZYOgZZBweHSxc3nz NF75VWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NES5PFE2PCd-MkS0PVgyPTR:L3G+
BeWo MlnrSpVv[3Srb36gRZN{[Xl? NXPKcFJlOzBiwsXN NELwdIQzPCCq MWfpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= M2PBZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm4NVU1Lz5{NES5PFE2PDxxYU6=
MOML13 M2\6R2Z2dmO2aX;uJGF{e2G7 MnvLNVDPxE1? MXmyM|QhcA>? NYDIOnNRcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> M4jtPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
AML3 MlvSSpVv[3Srb36gRZN{[Xl? NXTEe3dsOTEQvF2= MWKyM|QhcA>? MkGwbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= M4rFW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
AML2 MV3GeY5kfGmxbjDBd5NigQ>? MYexNO69VQ>? M4nSWlIwPCCq MkXjbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= NXOwWFNHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
MOML13 NFv5XHpCeG:ydH;zbZMhSXO|YYm= NFr6bmgzNzFyIN88US=> MVKyOE81QCCq MkT0bY5lfWOnczDhdI9xfG:|aYO= NWrlblFbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML2 MkTBRZBweHSxc3nzJGF{e2G7 MUOyM|ExKM7:TR?= NWfk[XFSOjRxNEigbC=> MWXpcoR2[2W|IHHwc5B1d3Orcx?= M1nZclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
U2OS  M16yO2Z2dmO2aX;uJGF{e2G7 NW\VN5VHOjBizszN NUDoTFVLOjRiaB?= NF24N2VqdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX M4LSPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OE[3NlU6Lz5{NEi2O|I2QTxxYU6=
Hep3B MnzKRZBweHSxc3nzJGF{e2G7 Mn7HbY5lfWOnczDhdI9xfG:|aYO= MnmyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
Huh-7 NFvhdVJCeG:ydH;zbZMhSXO|YYm= M3u2dolv\HWlZYOgZZBweHSxc3nz MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721 MlvlRZBweHSxc3nzJGF{e2G7 M2PWN4lv\HWlZYOgZZBweHSxc3nz NGSwUIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2 M37XWWFxd3C2b4Ppd{BCe3OjeR?= MmfCbY5lfWOnczDhdI9xfG:|aYO= M1PFfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
Hep3B M2n1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV63b|l6PzJiaB?= NWDmPJltTE2VTx?= NWTMe5pKUUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= M4j2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
Huh-7 M2jsR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVK3NkBp NH3K[GpFVVOR MWrJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> MoTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
SMMC7721/Ac NYjtfI1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jJRVczKGh? NIP0SI1FVVOR M2OySmlEPTB;NUWuNlEhyrFiNT6wN{DPxE1? MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721 NGHNNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjvO|IhcA>? NULienVVTE2VTx?= NEi4cGRKSzVyPUOxMlI5KMLzIESuNkDPxE1? NHXOO2U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2/As MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHuwSWg4OiCq NYLaWW9bTE2VTx?= NFz4U4VKSzVyPU[4MlE{KMLzIEmuOkDPxE1? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
HepG2 NHT2OZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13oOVczKGh? MmXtSG1UVw>? NYLIU2tkUUN3ME2zOU45PiEEsTCyMlkh|ryP MojVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
MOLM-13 MmDmSpVv[3Srb36gRZN{[Xl? NILYW2Y3yqEQvF2= MnHDOkBp M1LSXmROW09? NGGxfpVmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw M3rtdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1NFgzLz5{NEi4OVA5OjxxYU6=
MOLM-13 NGfsfXJHfW6ldHnvckBCe3OjeR?= M4fWXFbDqM7:TR?= NVPVS|lmOC16IHi= MXvEUXNQ MmL0bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ MmnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEWwPFIoRjJ2OEi1NFgzRC:jPh?=
115 Mk\xSpVv[3Srb36gRZN{[Xl? MmPHOUDPxE1? M3TVcFQ5KGh? MV\EUXNQ MYjpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M3;XelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 MoDxSpVv[3Srb36gRZN{[Xl? NWfxWlV1PSEQvF2= MnjSOFghcA>? NGOwc4lFVVOR MWnpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MmrBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 MnPaSpVv[3Srb36gRZN{[Xl? NWDzbGlmPSEQvF2= NX;tXnhjPDhiaB?= Mn7PSG1UVw>? NH;BeJpqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg NYHoXYRTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
ACHN MYLGeY5kfGmxbjDBd5NigQ>? M{PsPVUh|ryP M{jpW|Q5KGh? MYfEUXNQ NF;mOnZqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MlnKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjMWpprPSEQvF2= M2W0UlQ5KGh? M1myR2ROW09? NV;rTGtqcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh M2jVelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 NYnhTIF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXTOUDPxE1? M2TIWlQ5KGh? NXTZPGxKTE2VTx?= Ml7IbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MnO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPORnY2KM7:TR?= M1rkc|Q5KGh? MUHEUXNQ M1GwfIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
ACHN NETLTlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHiUJVGPSEQvF2= NHTCNoU1QCCq NVrPTVhOTE2VTx?= NX\r[ZpQcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MmjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
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A498 MnrYSpVv[3Srb36gRZN{[Xl? NWjlUZZ3OC53L{GvOUDPxE1? Mmq1OFghcA>? NGrTbnZFVVOR NH7ycmlt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= Ml3GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
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NP460 MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkL3TWM2OD1{Mj64OeKyOS5zODFOwG0> Mm\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{NUK1O|UoRjJ4MkWyOVc2RC:jPh?=
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AT2 M3ztTmNmdGxiVnnhZoltcXS7IFHzd4F6 M{foW|AuOjVizszN NHiwWJBqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NGjrOFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK0NFIxOyd-MkSyOFAzODN:L3G+
REH NUDNeZZRS2WubDDWbYFjcWyrdImgRZN{[Xl? NXnwZ3JwOC1{NTFOwG0> NGXyPJJqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NHLkR3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK0NFIxOyd-MkSyOFAzODN:L3G+
UoCB6 M1;KOGNmdGxiVnnhZoltcXS7IFHzd4F6 NHHKOWExNTJ3IN88US=> MUfpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NUXPXW9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFAzODNpPkK0NlQxOjB|PD;hQi=>
A2780 M2DOeGZ2dmO2aX;uJGF{e2G7 MXe1M|ExNzJyIN88US=> NGS2TXUzPCCq MmL3eZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NXj1UJBGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|YyPDdpPkK0NVM3OTR5PD;hQi=>
H460 NX;Hd5BjTnWwY4Tpc44hSXO|YYm= MUS1M|ExNzJyIN88US=> MXSyOEBp MlvaeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF|NkG0O{c,OjRzM{[xOFc9N2F-
Lovo  Mm\FSpVv[3Srb36gRZN{[Xl? MXm1M|ExNzJyIN88US=> NYG3PFNpOjRiaB?= NWm1TnZTfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M2rNVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO2NVQ4Lz5{NEGzOlE1PzxxYU6=
A2780 M37rcGFxd3C2b4Ppd{BCe3OjeR?= NF76T5Q2NzFyL{KwJO69VQ>? M4rVOlI1KGh? NVi1UYFl\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? M{W2fFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO2NVQ4Lz5{NEGzOlE1PzxxYU6=
H460 NXr0Z4NDSXCxcITvd4l{KEG|c3H5 Mo\EOU8yOC9{MDFOwG0> MofiNlQhcA>? MYDlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> M4jqZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUO2NVQ4Lz5{NEGzOlE1PzxxYU6=
Lovo  M33zb2Fxd3C2b4Ppd{BCe3OjeR?= M3rmeFUwOTBxMkCg{txO M2fib|I1KGh? M1y0TYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN NGrremw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOlE1Pyd-MkSxN|YyPDd:L3G+
U87MG M1PnO2Z2dmO2aX;uJIF{e2G7 MmPJNVAhdWmwcx?= MkDZRolv\GmwZzDh[oZqdmm2eTD0c{BOTE1{IHnuJIh2dWGwIGW4O21IKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gUWROOi:yNUOgdJJwfGWrbjDpcpRmemGldHnvckBi\nSncjCxNEBucW6|IHL5JJF2[W62aYTheIl3\SC|YX7ke4lkcCCrbX31co8h[XO|YYmsJGlEPTBiPTCwMlExPDVizszNMi=> MkLLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNUC3PFIoRjJ5MEWwO|gzRC:jPh?=
U87MG M4PFNWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXGzWnV{PDhiaILz NFy0fZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGW4O21IKGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKHB3MzDh[pRmeiB2ODDodpMh[nliTWTTJIF{e2G7LDDJR|UxKD1iNj61JO69VS5? MmPyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyNUC3PFIoRjJ5MEWwO|gzRC:jPh?=
U343MG NXT1dZFrSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmHGOFghcHK| MmLuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXM{SzUWch[2WubIOg[ZhxemW|c3nu[{B4cWymIIT5dIUheDV|IHHmeIVzKDR6IHjyd{BjgSCPVGOgZZN{[XluIFnDOVAhRSBzMj62JO69VS5? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzB3MEe4Nkc,OjdyNUC3PFI9N2F-
SW620 NIPkZ|FEgXSxdH;4bYNqfHliYYPzZZk> M1myc|czKGi{cx?= M4fyUWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNYPjJyIHPlcIx{KGGodHXyJFczKGi{czDifUBUWkJiYYPzZZktKEmFNUCgQUAxNjN6IN88UU4> Mm[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+R4hGVUKOPD;hQi=>
A549 MlXvR5l1d3SxeHnjbZR6KGG|c3H5 MVW3NkBpenN? NX;uN3o{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwJF0hOC52MTFOwG0v MkTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+R4hGVUKOPD;hQi=>
SJSA1 NX\VelByS3m2b4TvfIlkcXS7IHHzd4F6 MmHWO|IhcHK| NYOwSZRCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0qVQUGgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KFOUQjDhd5NigSxiSVO1NEA:KDFwOEGg{txONg>? NIG0[2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5EcEWPQly8M4E,
HCT116 MoLtR5l1d3SxeHnjbZR6KGG|c3H5 M13CUFczKGi{cx?= MYLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JHNTSiCjc4PhfUwhUUN3MDC9JFQvPjNizszNMi=> MojMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVkyOzN2Lze+R4hGVUKOPD;hQi=>
PC3 NXvkZohOS3m2b4TvfIlkcXS7IHHzd4F6 MVO3NkBpenN? Ml3WR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDTVmIh[XO|YYmsJGlEPTBiPTC2MlM4KM7:TT6= NH;sOpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyQTF|M{SvK|5EcEWPQly8M4E,

... 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

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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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.

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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.

Mdm2 Signaling Pathway Map

Related Mdm2 Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID