Nutlin-3

For research use only.

Catalog No.S1061

47 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 47 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 Mm\lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PwW|XDqM7:TR?= MXG0POKhcA>? NGH0bYZjdG:la4OgNlcuV0iFLXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHPvcZBiemGkbHWgeI8hfGijdDDv[kBj[XOjbDDs[ZZmdHN? NWDsdVhQOjZ|NUC1OlU>
NP69 NX;ndG1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7kTWM2OD1|MT62PeKyOi53NDFOwG0> NV32TFJqOjZ{NUK1O|U>
NP460 NFL0V4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HPNGlEPTB;MkKuPFXDuTFwMUig{txO MVOyOlI2OjV5NR?=
C666-1 NYTrZlR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHIOFRxUUN3ME2xPU46PcLzOD65N{DPxE1? NV6yS5o1OjZ{NUK1O|U>
C666-1 MluxR4VtdCCYaXHibYxqfHliQYPzZZk> MoHFNVAhyrWP M3;kR|Q5KGh? M3LTd2ROW09? M3LJXJNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJJRp\SCleYTveI95cWNiZX\m[YN1KG:oIHPpd5Bt[XSrbh?= Mk\WNlYzPTJ3N{W=
C666-1  M1zodWZ2dmO2aX;uJGF{e2G7 NYXkfFBmOTBiwsXN M1z1RlI1KGh? M1fYV2ROW09? MVzhZ5RqfmG2ZYOgeIhmKHB3MzDwZZRpf2G7LDD1dJJm\3WuYYTpcocheDV|LDDwNlEh[W6mIF3kcVI> MmHkNlYzPTJ3N{W=
C666-1 MojORZBweHSxc3nzJGF{e2G7 MoLjNVAhyrWP NY\2fFF2PDhxN{KgbC=> M4r3UGROW09? NIXYUFV{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{BkcXOybHH0bY4ucW6mdXPl[EBieG:ydH;zbZM> M1\Ib|I3OjV{NUe1
A549 M{LqTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PrR|I1KGh? NYfybFhTUUN3ME2xO{43QCEEsTC0MlUzKM7:TR?= M{\afVI3OTJ3MkOw
A549-NTC Mn7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:yOEBp NX\oZ5JXUUN3ME2xPU41OiEEsTCxMlk3KM7:TR?= MYSyOlEzPTJ|MB?=
A549-920 MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPqNlQhcA>? NFXlRplKSzVyPUOzMlg2KMLzIESuPFQh|ryP MlLmNlYyOjV{M{C=
CRL-5908 Mm\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7qfmdvOjRiaB?= MV3JR|UxRTN6LkexJOKyKDJwNEOg{txO MWqyOlEzPTJ|MB?=
L6 NULsSXpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LsR|ExyqEQvF5CpC=> MV6yOE81QC95MjDo NUD5UII5TE2VTx?= NVi2fHBScW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w NHK5W5EzPTh5MUe5OC=>
C2C12 MojiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVW3dYZvOTEEoN88UeKh NXHJZWs{OjRxNEivO|IhcA>? NEf0SVBFVVOR NUjxNmlmcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w MUOyOVg4OTd7NB?=
MCF-7  NHPXWoxHfW6ldHnvckBCe3OjeR?= MkTKNVDDqM7:TR?= M2O2[2ROW09? MorxbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh NIHNU2ozPTdyMkewNy=>
DU4475  MYHGeY5kfGmxbjDBd5NigQ>? Mo[wOU8yOC9{MDFOwG0> NITieIczPMLiaB?= MWnkc5dvemWpdXzheIV{KFSxY3GtNUBld3OnIHTldIVv\GWwdHz5 MXqyOVU1PzF5NB?=
SMMC-7721 MYLGeY5kfGmxbjDBd5NigQ>? MorqNVAh|ryP NWTjPHBnPDhiaB?= NWLMOZplTE2VTx?= NIn2SJJk[XW|ZYOgSG5CKESVQjDkZY1i\2V? NHLDXpozPTV2NEO2NS=>
SMMC-7721 MkXVSpVv[3Srb36gRZN{[Xl? M3jZe|ExKM7:TR?= MnPIOFghcA>? MlnjSG1UVw>? Mk\ZbY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> M3HrelI2PTR2M{[x
SMMC-7721 MlTUSpVv[3Srb36gRZN{[Xl? MkK2NVAh|ryP M33ndFQ5KGh? MoTNSG1UVw>? NWrBc5dbcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? MV:yOVU1PDN4MR?=
SMMC-7721 NFPZZlVHfW6ldHnvckBCe3OjeR?= MYmxNEDPxE1? NGLSeIE{PiCq NYK0Wm1RTE2VTx?= M2DE[YNifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 NF\2dIEzPTV2NEO2NS=>
MCF-7 M33vb2Z2dmO2aX;uJGF{e2G7 NYL3UIhXOTEEoN88US=> M4PMbFAuOjRiaB?= MVLpcoR2[2W|IIC1N{BidmRicEKxM2NqeDF? MYOyOVQ5OjN5Mx?=
OVCAR10 M4XYVWZ2dmO2aX;uJGF{e2G7 MX2xNOKh|ryP M{HHXVIycMLi M3rMN2ROW09? M3rVZYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> NUXSZnI4OjV2Mk[1OFg>
NCI-H23 M3P2NmZ2dmO2aX;uJGF{e2G7 M{DsZ|ExyqEQvF2= NH;pd4czOWkEoB?= MnXFSG1UVw>? M4XWcIlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> NGjv[mUzPTR{NkW0PC=>
A2780 M2rCcGZ2dmO2aX;uJGF{e2G7 Moj2NVDDqM7:TR?= MYqyNYjDqA>? NHyzfGlFVVOR NGTtfpFqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ M37N[FI2PDJ4NUS4
NCI-H23 M{faXWZ2dmO2aX;uJGF{e2G7 M4DCb|ExyqEQvF2= MUiyNYjDqA>? NGXHWYZFVVOR M{nPRoRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NWXndZFyOjV2Mk[1OFg>
A2780 MoPZSpVv[3Srb36gRZN{[Xl? NF;Sd3gyOMLizszN MWWyNYjDqA>? MoPMSG1UVw>? NH7NN3hl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> NU\5OVl{OjV2Mk[1OFg>
HCT116  NFz2dWZHfW6ldHnvckBCe3OjeR?= MYixNEDDvU1? NVPndnl[OjRiaB?= M3fZOoNifXOnczDhJJA2Oy2mZYDlcoRmdnRidHX0doFxdG:rZDDHNU1ienKnc4SgbY4h\GmybH;p[EBJS1RzMU[gZ4xwdmW|IFSzJIFv\CCGOB?= NFTYSHUzPTN6MEC1OS=>
MCF-10CA1a M3XXOGZ2dmO2aX;uJGF{e2G7 NIrPU5gyOMLizszN MVW0PEBp MofZSG1UVw>? Ml;HbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? MVuyOVI2Pzd{OR?=
MCF-10A1  NWXob4E1TnWwY4Tpc44hSXO|YYm= MniyNVDDqM7:TR?= MkWyNlQwPDhiaB?= MXjEUXNQ MYfpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> MkDxNlUzPTd5Mkm=
MCF-10CA1a MWPGeY5kfGmxbjDBd5NigQ>? NXn3WVlCOTEEoN88US=> NVm5cmNWOjRiaB?= M{TkNmROW09? NEnFRW5l\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= NXnid2I6OjV{NUe3Nlk>
MCF-10CA1a M3KxcWZ2dmO2aX;uJGF{e2G7 MnXHNVDDqM7:TR?= M{HNbFI1KGh? MV\EUXNQ M2XwNYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= M2fKVFI2OjV5N{K5
SK-BR-7 M4jsXGZ2dmO2aX;uJGF{e2G7 NFSwRW8yOMLizszN NXzJNYtnOjRiaB?= M2DLUWROW09? MY\pcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? M17hfVI2OjV5N{K5
SUM102PT NXXK[m1mTnWwY4Tpc44hSXO|YYm= M3\pdFExyqEQvF2= MoTDNlQhcA>? NI\wN25FVVOR NGnnOnRqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= M3;BS|I2OjV5N{K5
RAW 264.7 NXnKWoRPTnWwY4Tpc44hSXO|YYm= NHXTUFUyOMLizszN NEOzUG8{OCCvaX6= M1nZSJBz\X[nboTzJJRp\SCyNUOgdoVlfWO2aX;uJIlvKHKnc4DvcpNmKHSxIFzQVy=> NH\tPXQzPTF5MkW0Oy=>
RAW 264.7 NW\oeXhyTnWwY4Tpc44hSXO|YYm= NWqzV2x3OTEEoN88US=> MUCzNEBucW5? MoTodoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NEG1e2EzPTF5MkW0Oy=>
RAW 264.7 NILFfG5HfW6ldHnvckBCe3OjeR?= M13KbFExyqEQvF2= NFjuWGI{OCCvaX6= MXXpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= NWLWbGRXOjVzN{K1OFc>
MCF7  NH:zNJZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUiyMlUhyrWP M3jjOlUh\A>? NVHW[lc4TE2VTx?= NETRWFZ{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u MoDoNlUxQDV7MEK=
MCF7  NWn6bGJQTnWwY4Tpc44hSXO|YYm= NYKyRllHOi53INM1US=> NWnrTHdCPDhiaB?= MYTEUXNQ NF3R[|Rl\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? NXn2eJFNOjVyOEW5NFI>
ACHN MmPXR4VtdCCYaXHibYxqfHliQYPzZZk> M1[yW|AvPS1zMDFOwG0> MlLyNE03KGR? NFrleFNFVVOR MkHnbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFXuWYozPTB4N{e4Oy=>
Caki-2 NInP[4dE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXq2ZpJYOC53LUGwJO69VQ>? MkHxNE03KGR? MXPEUXNQ MnizbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? Mne1NlUxPjd5OEe=
A498 NYjoeYtLS2WubDDWbYFjcWyrdImgRZN{[Xl? M1XvRVAvPS1zMDFOwG0> Mle0NE03KGR? MonCSG1UVw>? NHLNephqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NXHaUpE4OjVyNke3PFc>
115 M4\6cWNmdGxiVnnhZoltcXS7IFHzd4F6 MWOwMlUuOTBizszN Mn;TNE03KGR? Mk\rSG1UVw>? MVjpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NY\DOGhCOjVyNke3PFc>
117 MWfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NV7QS3BWOC53LUGwJO69VQ>? M{X0Z|AuPiCm MUnEUXNQ MU\pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWLjRlBMOjVyNke3PFc>
ACHN NF\OSlhHfW6ldHnvckBCe3OjeR?= M{fLSFAvPS9zL{Wg{txO NFvPW5M1QCCq NVv2UVN1TE2VTx?= NX7Re29xdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MYeyOVA3Pzd6Nx?=
Caki-2 M3z5PGZ2dmO2aX;uJGF{e2G7 M1zRSVAvPS9zL{Wg{txO NUfDcZFYPDhiaB?= MnrrSG1UVw>? M4X0ZYxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NUXieGc2OjVyNke3PFc>
A498 Mlf0SpVv[3Srb36gRZN{[Xl? NX\KZ4VmOC53L{GvOUDPxE1? NWPu[oFYPDhiaB?= NYDxNlA3TE2VTx?= NYDBcZlwdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= M4rQSFI2ODZ5N{i3
115 NIPZO2FHfW6ldHnvckBCe3OjeR?= NXXZWFZkOC53L{GvOUDPxE1? MlXkOFghcA>? Ml:ySG1UVw>? MnjRcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? NVT3SJF7OjVyNke3PFc>
ACHN MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXSZnN6PSEQvF2= NUe1OYhYPDhiaB?= NH7zd41FVVOR M3[2Solv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MmfWNlUxPjd5OEe=
Caki-2 MknFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor3OUDPxE1? NGPXdpo1QCCq NWXxXY82TE2VTx?= NYrid45kcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh M{DySVI2ODZ5N{i3
A498 M{fuZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nnOFUh|ryP M2eyb|Q5KGh? Mk[xSG1UVw>? MYPpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MYmyOVA3Pzd6Nx?=
115 M4\SOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn6OYxSPSEQvF2= MWS0PEBp NHOxO2NFVVOR M1ywPIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MmHUNlUxPjd5OEe=
ACHN M{nlbmZ2dmO2aX;uJGF{e2G7 NXW5SVY4PSEQvF2= MUK0PEBp MlewSG1UVw>? MYPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MXqyOVA3Pzd6Nx?=
Caki-2 M2rHSGZ2dmO2aX;uJGF{e2G7 Ml21OUDPxE1? MVS0PEBp NWHlcmxpTE2VTx?= MknqbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NXzFNmVxOjVyNke3PFc>
A498 M3zyXWZ2dmO2aX;uJGF{e2G7 MoLxOUDPxE1? NV7uUHpXPDhiaB?= MmfxSG1UVw>? NIjkRmJqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg Ml35NlUxPjd5OEe=
115 NWrXSXJuTnWwY4Tpc44hSXO|YYm= MlXvOUDPxE1? NYXjTnB4PDhiaB?= M{HQdGROW09? NF[4RopqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M2ixSVI2ODZ5N{i3
MOLM-13 M1;SOWZ2dmO2aX;uJGF{e2G7 MmW5OuKh|ryP M2X1UlAuQCCq MkmxSG1UVw>? NFHBZXVqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDwOVMtKE2GTUKsJJAzOSCjbnSgZYNmfHmuYYTl[EBxPTN? MWGyOFg5PTB6Mh?=
MOLM-13 MknLSpVv[3Srb36gRZN{[Xl? MUe2xsDPxE1? NWrYNHROPiCq MkD3SG1UVw>? M2nqOoVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= NUPSNIduOjR6OEWwPFI>
HepG2 MmHpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTtO|IhcA>? NELSUo5FVVOR MUXJR|UxRTN3Lki2JOKyKDJwOTFOwG0> NYLLZWV4OjR6OES4NFk>
HepG2/As NEjn[HNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHmO|IhcA>? NVm3VodvTE2VTx?= M2nNT2lEPTB;NkiuNVMhyrFiOT62JO69VQ>? MUmyOFg5PDhyOR?=
SMMC7721 MmfjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWG3NkBp M3KwXGROW09? NH\n[|RKSzVyPUOxMlI5KMLzIESuNkDPxE1? NF7YZ2gzPDh6NEiwPS=>
SMMC7721/Ac M2XnRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7SNmNbPzJiaB?= MVTEUXNQ NEfMOoFKSzVyPUW1MlIyKMLzIEWuNFMh|ryP M4PW[FI1QDh2OEC5
Huh-7 NUDkR5F5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTMbZI4OiCq M{T2eGROW09? NXHZTY9ZUUN3ME2zN{46PiEEsTCzMlkh|ryP MXyyOFg5PDhyOR?=
Hep3B MmHzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWm3NkBp NYjXbmJVTE2VTx?= NX7r[o97UUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= MlqxNlQ5QDR6MEm=
HepG2 M4fENmFxd3C2b4Ppd{BCe3OjeR?= NXO2NI1xcW6mdXPld{BieG:ydH;zbZM> MkfkNlQ5QDR6MEm=
SMMC7721 M3joN2Fxd3C2b4Ppd{BCe3OjeR?= NHnNZmxqdmS3Y3XzJIFxd3C2b4Ppdy=> M{HkV|I1QDh2OEC5
Huh-7 NHv0Wo1CeG:ydH;zbZMhSXO|YYm= MoDkbY5lfWOnczDhdI9xfG:|aYO= NVG5RnR{OjR6OES4NFk>
Hep3B NIn1fnJCeG:ydH;zbZMhSXO|YYm= M3TLdIlv\HWlZYOgZZBweHSxc3nz MVKyOFg5PDhyOR?=
U2OS  NHK0dppHfW6ldHnvckBCe3OjeR?= NV;m[llqOjBizszN MmnINlQhcA>? NEfMV4hqdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX Mlr4NlQ5Pjd{NUm=
AML2 MVrBdI9xfG:|aYOgRZN{[Xl? MUeyM|ExKM7:TR?= NYrDSpRROjRxNEigbC=> MknibY5lfWOnczDhdI9xfG:|aYO= NYLwWIJPOjR4NUm3OFk>
MOML13 M37FTGFxd3C2b4Ppd{BCe3OjeR?= NWD6coNnOi9zMDFOwG0> NHrzRo4zPC92ODDo MX7pcoR2[2W|IHHwc5B1d3Orcx?= NHSzR3UzPDZ3OUe0PS=>
AML2 MmP1SpVv[3Srb36gRZN{[Xl? NInpdWsyOM7:TR?= NV7yO|FGOi92IHi= MlKwbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MkOwNlQ3PTl5NEm=
AML3 NGLmd2pHfW6ldHnvckBCe3OjeR?= NWTTVJlwOTEQvF2= NFfLXHMzNzRiaB?= MWHpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= NXPZb3kxOjR4NUm3OFk>
MOML13 MU\GeY5kfGmxbjDBd5NigQ>? NHf6bFcyOM7:TR?= M1jtXFIwPCCq M1z2Tolv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NFf5fVEzPDZ3OUe0PS=>
BeWo M1n2bWZ2dmO2aX;uJGF{e2G7 NFPHZnA{OCEEtV2= M3;lSFI1KGh? MnfnbY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs MUmyOFQ6QDF3NB?=
BeWo MVLBdI9xfG:|aYOgRZN{[Xl? MV:zNEDDvU1? NWPESoJDOjRiaB?= M3rBZ4lv[3KnYYPld{BieG:ydH;zbZM> NFjPWlEzPDR7OEG1OC=>
OCI MW\GeY5kfGmxbjDBd5NigQ>? NHrHXWYyOCEQvF2= MYOyOEBp M{PZSZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NHrlOoYzPDR5M{W2Ni=>
MOLM NXiwTVJCTnWwY4Tpc44hSXO|YYm= NHztfWoyOCEQvF2= M3z6RlI1KGh? M1;nSJVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= NUXQcHRpOjR2N{O1OlI>
U2OS  NUXSSpoxTnWwY4Tpc44hSXO|YYm= Ml32NlAh|ryP M1rWWVI1KGh? NIHjdIlqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NY\o[Yp[OjR|Nk[wNFc>
RKO NUfoUFczTnWwY4Tpc44hSXO|YYm= NFvvN28zOCEQvF2= MX[yOEBp NV;CV|BkcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= MWeyOFM3PjByNx?=
U2OS  MofZSpVv[3Srb36gRZN{[Xl? MUOyNEDPxE1? MW[yOEBp NV;CW2tpcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> NIrzWmYzPDN4NkCwOy=>
RKO MUTGeY5kfGmxbjDBd5NigQ>? MlfNNlAh|ryP M2HXcFI1KGh? NIfucmRqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MUKyOFM3PjByNx?=
SMMC-7721  NIr5RmRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYCxMlI2NTJyIN88US=> M4TRO|I1NzR6L{eyJIg> NITaV5ZFVVOR M3vTU4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NUK5Vos2OjR{OE[zNVI>
HuH-7 Ml7aR4VtdCCYaXHibYxqfHliQYPzZZk> MVixMlI2NTJyIN88US=> M4XtcFI1NzR6L{eyJIg> MWjEUXNQ NIHxdGNqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NVG2W2p{OjR{OE[zNVI>
SMMC-7721  M2XpRmFxd3C2b4Ppd{BCe3OjeR?= NIC3Z2QzOCEQvF2= NVG5b4dOPDhiaB?= Mn\zSG1UVw>? M2TDd4lv\HWlZYOgZZBweHSxc3nz NF\hWoYzPDJ6NkOxNi=>
HuH-7 NWjJ[I54SXCxcITvd4l{KEG|c3H5 M2W0NlIxKM7:TR?= NV;tWXdEPDhiaB?= MYDEUXNQ M3fjWIlv\HWlZYOgZZBweHSxc3nz NFfxbIEzPDJ6NkOxNi=>
SMMC-7721  M2Pp[GZ2dmO2aX;uJGF{e2G7 M4fjZVExKM7:TR?= M{j3SFM3KGh? MoW3SG1UVw>? M2fCbIRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ M3;pdVI1Ojh4M{Gy
HuH-7 M32xRWZ2dmO2aX;uJGF{e2G7 NHPDXmEyOCEQvF2= MXizOkBp M1zPOGROW09? M2nS[IRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ NUDwXlFnOjR{OE[zNVI>
AT2 M120TmZ2dmO2aX;uJGF{e2G7 MUe1M|ExKM7:TR?= MkfFcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? NELRXpkzPDJ2MEKwNy=>
REH MmHuSpVv[3Srb36gRZN{[Xl? M2DjXVUwOTBizszN NV6ySZRkdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= MkXQNlQzPDB{MEO=
UoCB6 M{nUXWZ2dmO2aX;uJGF{e2G7 Ml7vOU8yOCEQvF2= NXLHU29XdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= MXKyOFI1ODJyMx?=
AT2 MVfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{Lz[|AuOjVizszN MW\pcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MXSyOFI1ODJyMx?=
REH MXXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVSwMVI2KM7:TR?= MmPkbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M37Nd|I1OjRyMkCz
UoCB6 MVLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{m4WlAuOjVizszN M2rSV4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NG\2cFYzPDJ2MEKwNy=>
A2780 MX\GeY5kfGmxbjDBd5NigQ>? MUi1M|ExNzJyIN88US=> MYCyOEBp NV\rbXc2fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M4DwVlI1OTN4MUS3
H460 M{nmZmZ2dmO2aX;uJGF{e2G7 NXTEWHZ2PS9zMD:yNEDPxE1? NHrVd5AzPCCq MoX0eZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MmLRNlQyOzZzNEe=
Lovo  NGS5THZHfW6ldHnvckBCe3OjeR?= M1vhXVUwOTBxMkCg{txO M3f3b|I1KGh? M1\WUpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NFjq[IQzPDF|NkG0Oy=>
A2780 M2jBbWFxd3C2b4Ppd{BCe3OjeR?= M1G2cFUwOTBxMkCg{txO Ml:0NlQhcA>? M2PKToVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M1nBeFI1OTN4MUS3
H460 NFv2T49CeG:ydH;zbZMhSXO|YYm= MWq1M|ExNzJyIN88US=> NYfxcIdOOjRiaB?= NV3uWXhE\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? NHvKS5IzPDF|NkG0Oy=>
Lovo  NW\hbZNiSXCxcITvd4l{KEG|c3H5 MXO1M|ExNzJyIN88US=> M1PrNFI1KGh? M1LJd4VvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN NITaOIczPDF|NkG0Oy=>

... 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
    Concentration
    Volume
    Molecular Weight

*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
    V1
    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):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    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