Nutlin-3

Catalog No.S1061

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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In DMSO USD 185 In stock
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Cited by 18 Publications

5 Customer Reviews

  • Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.

    Int J Oncol 2014 44, 761-8. Nutlin-3 purchased from Selleck.

  •  

    p53 activation in A76T p53-mutated UKF-NB-3’RITA(10 uM) IV cells. Cells were treated with RITA (10 uM) or nutlin-3 (10 uM) for 24 h and investigated by western blot for the expression of p53 target genes

    Cell Death Dis 2012 3, e294. Nutlin-3 purchased from Selleck.

  • Caspase 3/7 activation in UKF-NB-3 or UKF-NB-3rNutlin10 μM cells treated nutlin-3 (10 μM), VCR (10 ng/ml), DOX (20 ng/ml), or CDDP (1000 ng/ml).

    Cell Death Dis 2011 2, e243. Nutlin-3 purchased from Selleck.

  • J Cell Physiol, 2018, 233(9):7424-7434. Nutlin-3 purchased from Selleck.

  • d qPCR evaluation of DKK1 in MSCs exposed to melphalan in combination with increasing concentrations of nutlin-3 for 24 h. Cells were pre-treated with nutlin-3 for 20 min prior to chemotherapy. *Indicates p value<0.05, One-way ANOVA with Holm-Sidak post hoc

    Med Oncol, 2016, 33(10):113. Nutlin-3 purchased from Selleck.

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 NH\WSmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULFd2FLPcLizszN MX[0POKhcA>? MXLicI9kc3NiMketU2hENWmwZIXj[YQh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDhdoFjdGVidH:geIhifCCxZjDiZZNidCCuZY\lcJM> NH3COoIzPjN3MEW2OS=>
NP69 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNzLk[5xtEzNjV2IN88US=> MXqyOlI2OjV5NR?=
NP460 NXnMbodpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkj5TWM2OD1{Mj64OeKyOS5zODFOwG0> NWCyUoRsOjZ{NUK1O|U>
C666-1 MnjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTF7Lkm1xtE5Njl|IN88US=> M2rXOFI3OjV{NUe1
C666-1 MofFR4VtdCCYaXHibYxqfHliQYPzZZk> MmfTNVAhyrWP MX[0PEBp M1T0bWROW09? NHjwUFR{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDjbZNxdGG2aX6= NE\0ZlYzPjJ3MkW3OS=>
C666-1  M2XQbGZ2dmO2aX;uJGF{e2G7 MYqxNEDDvU1? M4LRZVI1KGh? NWroUHRGTE2VTx?= M3jlcYFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? NFr2XZEzPjJ3MkW3OS=>
C666-1 MoW5RZBweHSxc3nzJGF{e2G7 M1HiR|ExKML3TR?= NVjJc2ltPDhxN{KgbC=> NXPqT|NCTE2VTx?= M{TESJNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJINqe3CuYYTpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NFj6OFczPjJ3MkW3OS=>
A549 NHvZS3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvKeXp2OjRiaB?= M3LLe2lEPTB;MUeuOlghyrFiND61NkDPxE1? MXmyOlEzPTJ|MB?=
A549-NTC NF7Pb4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHHRZRjOjRiaB?= Mn\2TWM2OD1zOT60NkDDuSBzLkm2JO69VQ>? NEXhO5UzPjF{NUKzNC=>
A549-920 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXkT|NCOjRiaB?= NFXx[ZJKSzVyPUOzMlg2KMLzIESuPFQh|ryP MWCyOlEzPTJ|MB?=
CRL-5908 M3r1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\ofVF4OjRiaB?= NHL0dIlKSzVyPUO4MlcyKMLzIEKuOFMh|ryP MkfkNlYyOjV{M{C=
L6 M17QPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLKbG1LOTEEoN88UeKh M1zuPFI1NzR6L{eyJIg> NYPKVY1HTE2VTx?= NUT2bFFYcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w NVG5O2U5OjV6N{G3PVQ>
C2C12 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTpNVDDqM7:TdMg Ml\NNlQwPDhxN{KgbC=> M1vxOWROW09? NUiwPHZwcW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w NWK1PJJCOjV6N{G3PVQ>
MCF-7  NX;LTm1vTnWwY4Tpc44hSXO|YYm= M1S2TVExyqEQvF2= NH[yToVFVVOR MUXpcohq[mm2czDjfYNtcW5iREGgZY5lKESrY3XyxsA> NVXaWng3OjV5MEK3NFM>
DU4475  MojUSpVv[3Srb36gRZN{[Xl? Mnf1OU8yOC9{MDFOwG0> MVuyOOKhcA>? M2ixfoRwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> M13aXFI2PTR5MUe0
SMMC-7721 MlSzSpVv[3Srb36gRZN{[Xl? Mnz0NVAh|ryP MWe0PEBp M2jS[mROW09? NIKxR5pk[XW|ZYOgSG5CKESVQjDkZY1i\2V? NF3MdXozPTV2NEO2NS=>
SMMC-7721 MUXGeY5kfGmxbjDBd5NigQ>? NGi3eHcyOCEQvF2= M3;mcVQ5KGh? NVTNOWxjTE2VTx?= Ml;obY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> MoTFNlU2PDR|NkG=
SMMC-7721 MWDGeY5kfGmxbjDBd5NigQ>? MYixNEDPxE1? NETZR2Y1QCCq NUDRb4dCTE2VTx?= MXnpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B Moi5NlU2PDR|NkG=
SMMC-7721 NHvSRllHfW6ldHnvckBCe3OjeR?= M1f1WlExKM7:TR?= NU\PR5JROzZiaB?= MmnpSG1UVw>? M136dYNifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 NGrreVYzPTV2NEO2NS=>
MCF-7 NGK1XJZHfW6ldHnvckBCe3OjeR?= MWqxNOKh|ryP MX6wMVI1KGh? M3rDd4lv\HWlZYOgdFU{KGGwZDDwNlEwS2myMR?= NV;kfm9SOjV2OEKzO|M>
OVCAR10 NF3BT2ZHfW6ldHnvckBCe3OjeR?= M3nIOFExyqEQvF2= NEDtWWszOWkEoB?= NV30ZoVLTE2VTx?= MUDpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz MnPXNlU1OjZ3NEi=
NCI-H23 MYLGeY5kfGmxbjDBd5NigQ>? NEXHcJgyOMLizszN M4nCflIycMLi NVTvU4ozTE2VTx?= MVnpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NVTi[4ZjOjV2Mk[1OFg>
A2780 M{KyfWZ2dmO2aX;uJGF{e2G7 M4ToflExyqEQvF2= M3zXdlIycMLi NV;MRpdRTE2VTx?= MXfpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NFnPWXEzPTR{NkW0PC=>
NCI-H23 NF\KTW5HfW6ldHnvckBCe3OjeR?= MoXsNVDDqM7:TR?= NF3EWW8zOWkEoB?= NVzQfmVOTE2VTx?= MoHu[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= MmnjNlU1OjZ3NEi=
A2780 NWLleVdwTnWwY4Tpc44hSXO|YYm= NG\CdJcyOMLizszN NHjnW4EzOWkEoB?= MlTmSG1UVw>? MkDF[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= NFHjSokzPTR{NkW0PC=>
HCT116  MYHGeY5kfGmxbjDBd5NigQ>? MkfTNVAhyrWP MlXYNlQhcA>? NULJXXRx[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 M{jSclI2OzhyMEW1
MCF-10CA1a M4KzS2Z2dmO2aX;uJGF{e2G7 NYrRZ|IzOTEEoN88US=> MkfFOFghcA>? M3TjdmROW09? NFixOmFqdmirYnn0d{Bj[XOjbDDpcpZie2mxbjDhcoQhemWmdXPl[EBVT0ZvzsKzMYlv\HWlZXSgbY53[XOrb36geI8h[mG|YXygcIV3\Wy| MlLwNlUzPTd5Mkm=
MCF-10A1  M{Tt[GZ2dmO2aX;uJGF{e2G7 MnLCNVDDqM7:TR?= M1u0Z|I1NzR6IHi= NYLrfZpVTE2VTx?= MoC1bY5pcWKrdIOgcYloemG2aX;uJI9nKG6xcn3hcEBjemWjc4Sg[ZBqfGinbHnhcOKh MUSyOVI2Pzd{OR?=
MCF-10CA1a NXOwOIdzTnWwY4Tpc44hSXO|YYm= NU\XUpN5OTEEoN88US=> MW[yOEBp NIG2[lBFVVOR MUHk[YNz\WG|ZYOgeIhmKFSJRj5OtlMucW6mdXPl[EBuWk6DIHzleoVteyCxZl3NVFItyqCPTWC5MEBidmUEoHnueIVoemmwwrFOtuKhOw>? M{LX[|I2OjV5N{K5
MCF-10CA1a MXrGeY5kfGmxbjDBd5NigQ>? MojmNVDDqM7:TR?= MUCyOEBp NG\FfZVFVVOR NIPOR3hqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MWGyOVI2Pzd{OR?=
SK-BR-7 M4mzPWZ2dmO2aX;uJGF{e2G7 MoGwNVDDqM7:TR?= MY[yOEBp MYLEUXNQ NVnlVVgzcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u NYrDfI12OjV{NUe3Nlk>
SUM102PT NEXVdIFHfW6ldHnvckBCe3OjeR?= Mn\HNVDDqM7:TR?= NVj6RWM1OjRiaB?= NXLCXmVVTE2VTx?= MnfpbY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w MYqyOVI2Pzd{OR?=
RAW 264.7 M4nkU2Z2dmO2aX;uJGF{e2G7 MXyxNOKh|ryP MXOzNEBucW5? Ml:zdJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT M{juWlI2OTd{NUS3
RAW 264.7 NHjNWVVHfW6ldHnvckBCe3OjeR?= M3z0WFExyqEQvF2= NEfWeG8{OCCvaX6= Mm\0doVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= MWeyOVE4OjV2Nx?=
RAW 264.7 M{TzSmZ2dmO2aX;uJGF{e2G7 M1fxTlExyqEQvF2= Ml;PN|AhdWmw M3\SVIlvcGmkaYTzJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb39CpC=> MmnCNlUyPzJ3NEe=
MCF7  Mk\IR4VtdCCYaXHibYxqfHliQYPzZZk> MUeyMlUhyrWP M2jxclUh\A>? M1;2WWROW09? MnLnd4Vve2m2aYrld{BOS0Z5IITvJHBCWlBiaX7obYJqfGmxbh?= Mk\RNlUxQDV7MEK=
MCF7  MULGeY5kfGmxbjDBd5NigQ>? MX:yMlUhyrWP M2P4blQ5KGh? NVPLSVNLTE2VTx?= Mn71[IVkemWjc3XzJJRp\SCqb33vcI9od3W|IFTTRkBz\XCjaYKg[pJmeXWnbnPp[ZM> NF;SVGozPTB6NUmwNi=>
ACHN NY\vUXV4S2WubDDWbYFjcWyrdImgRZN{[Xl? MoryNE42NTFyIN88US=> MXKwMVYh\A>? NXG3O2d[TE2VTx?= NFLSepVqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MVqyOVA3Pzd6Nx?=
Caki-2 NYfPfIc3S2WubDDWbYFjcWyrdImgRZN{[Xl? NXW0VGFROC53LUGwJO69VQ>? MUWwMVYh\A>? M3mwemROW09? NGLtWnRqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MljZNlUxPjd5OEe=
A498 M3zxOWNmdGxiVnnhZoltcXS7IFHzd4F6 NFrvbmsxNjVvMUCg{txO NGnGUVAxNTZiZB?= NHjsV|hFVVOR MmjjbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUmyOVA3Pzd6Nx?=
115 NV3jcnViS2WubDDWbYFjcWyrdImgRZN{[Xl? M2DKeVAvPS1zMDFOwG0> MVewMVYh\A>? MVvEUXNQ NXm2WWFZcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnPtNlUxPjd5OEe=
117 MY\D[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mlu4NE42NTFyIN88US=> M4e4NVAuPiCm NIrCZ4xFVVOR MVPpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3uwU|I2ODZ5N{i3
ACHN MlLESpVv[3Srb36gRZN{[Xl? M{H6U|AvPS9zL{Wg{txO MmDvOFghcA>? NHS4XYdFVVOR M4f3Toxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz NG\ic4czPTB4N{e4Oy=>
Caki-2 NHvQWXJHfW6ldHnvckBCe3OjeR?= NHPs[3cxNjVxMT:1JO69VQ>? NEXyS|k1QCCq MVHEUXNQ NGSzNopt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= M1vRWFI2ODZ5N{i3
A498 NYTs[JZpTnWwY4Tpc44hSXO|YYm= NUfpUHZTOC53L{GvOUDPxE1? MXq0PEBp NXfTOYhtTE2VTx?= MUjs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MkfJNlUxPjd5OEe=
115 MV7GeY5kfGmxbjDBd5NigQ>? M2TlOlAvPS9zL{Wg{txO NID3S|k1QCCq NFfibm5FVVOR NVHjZWV7dGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MV[yOVA3Pzd6Nx?=
ACHN NFvhS5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PwR|Uh|ryP MmW4OFghcA>? NHjGOI9FVVOR Mm\ybY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg M2\nUFI2ODZ5N{i3
Caki-2 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\kVIs2KM7:TR?= NHPHUIU1QCCq NWXpTFB{TE2VTx?= MmP3bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg NVnwU2ZGOjVyNke3PFc>
A498 MnjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLZXVE2KM7:TR?= MWq0PEBp MWfEUXNQ M1nhRYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M2[0blI2ODZ5N{i3
115 M3jVVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUfWcpBjPSEQvF2= Ml:wOFghcA>? MUHEUXNQ MnT6bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MVeyOVA3Pzd6Nx?=
ACHN MnKzSpVv[3Srb36gRZN{[Xl? M1rvN|Uh|ryP NHLIbpM1QCCq MV\EUXNQ MnSzbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M3TDfVI2ODZ5N{i3
Caki-2 M2PScGZ2dmO2aX;uJGF{e2G7 NUnDTIZ2PSEQvF2= MUW0PEBp NH3UcpJFVVOR MXPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NV3ibpJjOjVyNke3PFc>
A498 MoXkSpVv[3Srb36gRZN{[Xl? NGHLTVk2KM7:TR?= NXjacFN7PDhiaB?= NHLqWFJFVVOR Mo[4bY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M13kS|I2ODZ5N{i3
115 NX7jflZMTnWwY4Tpc44hSXO|YYm= NFvnPXk2KM7:TR?= M{LuRVQ5KGh? MnGySG1UVw>? MUjpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MYWyOVA3Pzd6Nx?=
MOLM-13 NEHKWVZHfW6ldHnvckBCe3OjeR?= NFHDOpg3yqEQvF2= M3PRUlAuQCCq NH\HW3hFVVOR NYDPWJpKcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| M4PZeFI1QDh3MEiy
MOLM-13 NIqzTm9HfW6ldHnvckBCe3OjeR?= NYHVfopXPsLizszN MnjsOkBp M3rUZmROW09? NXmzeIN{\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> NWHa[YRFOjR6OEWwPFI>
HepG2 NGKzWmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVf4WppSPzJiaB?= NEjVVVZFVVOR M4j4ZmlEPTB;M{WuPFYhyrFiMj65JO69VQ>? NHnYWIIzPDh6NEiwPS=>
HepG2/As MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3BO3VNPzJiaB?= NIrldFVFVVOR M3TUV2lEPTB;NkiuNVMhyrFiOT62JO69VQ>? M3;jPVI1QDh2OEC5
SMMC7721 MljPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUG3NkBp MVvEUXNQ NIfTN4RKSzVyPUOxMlI5KMLzIESuNkDPxE1? MnzaNlQ5QDR6MEm=
SMMC7721/Ac NWXWe5I3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYW5SHBIPzJiaB?= MlHCSG1UVw>? MnLYTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MUWyOFg5PDhyOR?=
Huh-7 NFjLVoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjYOotpPzJiaB?= M1PofmROW09? M3fQS2lEPTB;M{OuPVYhyrFiMz65JO69VQ>? NWD5ZnBzOjR6OES4NFk>
Hep3B MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXvRZc4OiCq M3nwd2ROW09? NUHJcZBjUUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= MYWyOFg5PDhyOR?=
HepG2 NGHmWllCeG:ydH;zbZMhSXO|YYm= MojWbY5lfWOnczDhdI9xfG:|aYO= MljqNlQ5QDR6MEm=
SMMC7721 M1jVTmFxd3C2b4Ppd{BCe3OjeR?= Mom2bY5lfWOnczDhdI9xfG:|aYO= M3XtfFI1QDh2OEC5
Huh-7 MWLBdI9xfG:|aYOgRZN{[Xl? NVLrOHJPcW6mdXPld{BieG:ydH;zbZM> NH7LbJkzPDh6NEiwPS=>
Hep3B MmXURZBweHSxc3nzJGF{e2G7 NGTaVodqdmS3Y3XzJIFxd3C2b4Ppdy=> NGfQR|kzPDh6NEiwPS=>
U2OS  MnziSpVv[3Srb36gRZN{[Xl? MWKyNEDPxE1? M1fvW|I1KGh? NUPDNZlwcW6lcnXhd4V{KHSqZTDtVm5CKGyndnXsd{Bw\sLiQlPMNmEyNCCEQ1zYUOKh[W6mQlPMWy=> MojYNlQ5Pjd{NUm=
AML2 NFPHTWlCeG:ydH;zbZMhSXO|YYm= MUSyM|ExKM7:TR?= MW[yOE81QCCq M3\6VYlv\HWlZYOgZZBweHSxc3nz NX72Z|g3OjR4NUm3OFk>
MOML13 NYW4WppZSXCxcITvd4l{KEG|c3H5 M3;3d|IwOTBizszN M3HVXlI1NzR6IHi= M2fiW4lv\HWlZYOgZZBweHSxc3nz MYCyOFY2QTd2OR?=
AML2 MWHGeY5kfGmxbjDBd5NigQ>? MlnLNVDPxE1? NGDqNWIzNzRiaB?= M2fzUIlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NVPHVI1ZOjR4NUm3OFk>
AML3 Ml7jSpVv[3Srb36gRZN{[Xl? MnvPNVDPxE1? NFLxZZkzNzRiaB?= NYfZW|NjcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MWCyOFY2QTd2OR?=
MOML13 MYrGeY5kfGmxbjDBd5NigQ>? MkW3NVDPxE1? NFvyU2kzNzRiaB?= M3\q[Ylv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NF76eGEzPDZ3OUe0PS=>
BeWo NHzHc3VHfW6ldHnvckBCe3OjeR?= NU\MOnhjOzBiwsXN M1P1TVI1KGh? NXWxRYVEcW6lcnXhd4V{KHB3MzygUYRuOixicEKxJIFv\CCSdX3hJIF1KHSqZTDwdo91\WmwIHzleoVt NUHoOVVvOjR2OUixOVQ>
BeWo MnPlRZBweHSxc3nzJGF{e2G7 M2T6TVMxKML3TR?= MW[yOEBp NWq4WVc6cW6lcnXhd4V{KGGyb4D0c5Nqew>? MkOxNlQ1QThzNUS=
OCI NFPBbG1HfW6ldHnvckBCe3OjeR?= MnjLNVAh|ryP MXSyOEBp Mn;HeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w NYrwSZA2OjR2N{O1OlI>
MOLM MmP3SpVv[3Srb36gRZN{[Xl? MV:xNEDPxE1? NVv1RmRDOjRiaB?= MUn1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? NIX5bpMzPDR5M{W2Ni=>
U2OS  NGDxUm9HfW6ldHnvckBCe3OjeR?= NVzYRXlDOjBizszN M2DJNVI1KGh? MV7pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MlLONlQ{PjZyMEe=
RKO NX:0SVRCTnWwY4Tpc44hSXO|YYm= NFTvOlAzOCEQvF2= M1GyOlI1KGh? MW\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NVfxN40{OjR|Nk[wNFc>
U2OS  MXfGeY5kfGmxbjDBd5NigQ>? NFT1XWYzOCEQvF2= NV3ZXVl{OjRiaB?= M1\IPIlv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u M1T3dVI1OzZ4MEC3
RKO MorjSpVv[3Srb36gRZN{[Xl? MU[yNEDPxE1? MWKyOEBp NXjHdWpYcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MoTvNlQ{PjZyMEe=
SMMC-7721  MUHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVKxMlI2NTJyIN88US=> Mlf6NlQwPDhxN{KgbC=> M1H4dGROW09? M3G4SYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 M3vMclI1Ojh4M{Gy
HuH-7 NUX4W|M4S2WubDDWbYFjcWyrdImgRZN{[Xl? MVGxMlI2NTJyIN88US=> NHLZd|YzPC92OD:3NkBp NWPh[nl{TE2VTx?= NUXqfWNDcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> MlLpNlQzQDZ|MUK=
SMMC-7721  MWjBdI9xfG:|aYOgRZN{[Xl? NY\0WIM5OjBizszN NU\hcWFDPDhiaB?= Ml7MSG1UVw>? NG\jT5pqdmS3Y3XzJIFxd3C2b4Ppdy=> MkLlNlQzQDZ|MUK=
HuH-7 NV7zWnR5SXCxcITvd4l{KEG|c3H5 MXiyNEDPxE1? NEHDVW01QCCq MmS2SG1UVw>? NInDWZVqdmS3Y3XzJIFxd3C2b4Ppdy=> NFHpUGIzPDJ6NkOxNi=>
SMMC-7721  M4D4XGZ2dmO2aX;uJGF{e2G7 MUOxNEDPxE1? MVezOkBp NFvvR5NFVVOR MWDkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> MXSyOFI5PjNzMh?=
HuH-7 M172b2Z2dmO2aX;uJGF{e2G7 NIO5NnUyOCEQvF2= MWOzOkBp NVHMRotETE2VTx?= MWTkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> MYeyOFI5PjNzMh?=
AT2 MlW0SpVv[3Srb36gRZN{[Xl? MoXEOU8yOCEQvF2= MUDs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? NUHCNFRsOjR{NECyNFM>
REH NY\rfHQ3TnWwY4Tpc44hSXO|YYm= MV:1M|ExKM7:TR?= NUTwPG9YdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NHTtNpMzPDJ2MEKwNy=>
UoCB6 Mm[zSpVv[3Srb36gRZN{[Xl? M4DsVlUwOTBizszN M2rwTIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li NVPqWoJkOjR{NECyNFM>
AT2 M2fKfGNmdGxiVnnhZoltcXS7IFHzd4F6 M{Lvd|AuOjVizszN MXHpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 MX6yOFI1ODJyMx?=
REH M{fodWNmdGxiVnnhZoltcXS7IFHzd4F6 M3HYblAuOjVizszN NXy1TlhycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= M1zFTlI1OjRyMkCz
UoCB6 M1j2XGNmdGxiVnnhZoltcXS7IFHzd4F6 MYWwMVI2KM7:TR?= MYjpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NY\ZbpV6OjR{NECyNFM>
A2780 MWrGeY5kfGmxbjDBd5NigQ>? MlnjOU8yOC9{MDFOwG0> MXiyOEBp MlXWeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MlzqNlQyOzZzNEe=
H460 M4TYOGZ2dmO2aX;uJGF{e2G7 M3fEc|UwOTBxMkCg{txO MYKyOEBp NXe3XHhNfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= M{j5b|I1OTN4MUS3
Lovo  MlvaSpVv[3Srb36gRZN{[Xl? M1fIclUwOTBxMkCg{txO MlPJNlQhcA>? NV;BdZVPfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= MV6yOFE{PjF2Nx?=
A2780 MWHBdI9xfG:|aYOgRZN{[Xl? NWrTRVhRPS9zMD:yNEDPxE1? MlXlNlQhcA>? M2TxRoVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN MkHnNlQyOzZzNEe=
H460 M{LpVmFxd3C2b4Ppd{BCe3OjeR?= MnXqOU8yOC9{MDFOwG0> MnG3NlQhcA>? MnTh[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> M1r1[lI1OTN4MUS3
Lovo  NXvvN21vSXCxcITvd4l{KEG|c3H5 MY[1M|ExNzJyIN88US=> M4q1TFI1KGh? M2rIXIVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M3nCT|I1OTN4MUS3

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
  • Formulation: Formulated in 2% Klucel, 0.5% Tween 80
  • 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

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)

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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 )

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* 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):
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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.

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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