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
USD 110 In stock
USD 170 In stock
USD 370 In stock
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4 Customer Reviews

  •  

    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.

  • 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.

    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 NGXpXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVy1xsDPxE1? Ml2wOFjDqGh? MkXuZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ NYXKVplIOjZ|NUC1OlU>
NP69 NHLWUnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPrbFhKSzVyPUOxMlY6yrF{LkW0JO69VQ>? NIThO|EzPjJ3MkW3OS=>
NP460 NYnpNItST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\OOIVKSzVyPUKyMlg2yrFzLkG4JO69VQ>? M37ubVI3OjV{NUe1
C666-1 M3;td2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF7Lkm1xtE5Njl|IN88US=> M2P0Z|I3OjV{NUe1
C666-1 NFTvZXRE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MWixNEDDvU1? M{jDRlQ5KGh? NGHVTXFFVVOR M2j0UpNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJJRp\SCleYTveI95cWNiZX\m[YN1KG:oIHPpd5Bt[XSrbh?= M33Q[lI3OjV{NUe1
C666-1  NVvHPJdkTnWwY4Tpc44hSXO|YYm= NYmwd4I4OTBiwsXN MYqyOEBp NXXkXYZpTE2VTx?= MnzLZYN1cX[jdHXzJJRp\SCyNUOgdIF1cHejeTygeZBz\We3bHH0bY5oKHB3MzygdFIyKGGwZDDN[I0z NX7F[GZGOjZ{NUK1O|U>
C666-1 M4C5WmFxd3C2b4Ppd{BCe3OjeR?= NILQcVIyOCEEtV2= MVy0PE84OiCq NHjJeZZFVVOR M4\XTZNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJINqe3CuYYTpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> MnLMNlYzPTJ3N{W=
A549 MkLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYGyOEBp NFzYZppKSzVyPUG3MlY5KMLzIESuOVIh|ryP MVmyOlEzPTJ|MB?=
A549-NTC NXnTeJJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVLTXHl{OjRiaB?= MVzJR|UxRTF7LkSyJOKyKDFwOU[g{txO MWiyOlEzPTJ|MB?=
A549-920 NES1SotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPI[mVWOjRiaB?= NUWzVY9bUUN3ME2zN{45PSEEsTC0Mlg1KM7:TR?= NXzjTmZEOjZzMkWyN|A>
CRL-5908 M3LzSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTFPVdMOjRiaB?= M{fSU2lEPTB;M{iuO|EhyrFiMj60N{DPxE1? NEnWT|gzPjF{NUKzNC=>
L6 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLXc45FOTEEoN88UeKh M1nGclI1NzR6L{eyJIg> NIPuSnhFVVOR NFvne5RqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? NVfQfnhlOjV6N{G3PVQ>
C2C12 M{nSd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7IR|UzOTEEoN88UeKh MVKyOE81QC95MjDo MU\EUXNQ M{fyUYlvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? M2\OXlI2QDdzN{m0
MCF-7  MofaSpVv[3Srb36gRZN{[Xl? M4HkR|ExyqEQvF2= MkfuSG1UVw>? MXvpcohq[mm2czDjfYNtcW5iREGgZY5lKESrY3XyxsA> NXnwOFE3OjV5MEK3NFM>
DU4475  MWPGeY5kfGmxbjDBd5NigQ>? NV2xVWtMPS9zMD:yNEDPxE1? NFfZSWUzPMLiaB?= M4nNN4Rwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> M1TwZlI2PTR5MUe0
SMMC-7721 MX;GeY5kfGmxbjDBd5NigQ>? NYriNWJ1OTBizszN NXHKZ2dLPDhiaB?= MVvEUXNQ M2fP[4NifXOnczDEUmEhTFOEIHThcYFo\Q>? Ml:0NlU2PDR|NkG=
SMMC-7721 MV;GeY5kfGmxbjDBd5NigQ>? MmPINVAh|ryP MVS0PEBp NVT6UY9bTE2VTx?= MYTpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg NX3pVJl4OjV3NESzOlE>
SMMC-7721 NG\DTm9HfW6ldHnvckBCe3OjeR?= MVKxNEDPxE1? NXnv[JVzPDhiaB?= NYTMWIV6TE2VTx?= NYHaVW5OcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? MWqyOVU1PDN4MR?=
SMMC-7721 M4LqZmZ2dmO2aX;uJGF{e2G7 M2DofFExKM7:TR?= M{HxZlM3KGh? NYnvSnlXTE2VTx?= NIfU[o9k[XW|ZYOgeIhmKGWldH;wbYMh\XiycnXzd4lwdiCxZjDJSmkyPg>? MoHqNlU2PDR|NkG=
MCF-7 NIHVfWtHfW6ldHnvckBCe3OjeR?= M{jJVVExyqEQvF2= NXzWd|g2OC1{NDDo NUH6[2VEcW6mdXPld{BxPTNiYX7kJJAzOS:FaYCx NVjBd5FIOjV2OEKzO|M>
OVCAR10 MULGeY5kfGmxbjDBd5NigQ>? MVqxNOKh|ryP NI\5dmMzOWkEoB?= NV72Z49mTE2VTx?= NIrRd5JqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MWWyOVQzPjV2OB?=
NCI-H23 Mkf1SpVv[3Srb36gRZN{[Xl? MnTpNVDDqM7:TR?= MVWyNYjDqA>? M4Xn[2ROW09? Mn3XbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NX7hRYdmOjV2Mk[1OFg>
A2780 NHrJVlRHfW6ldHnvckBCe3OjeR?= MoD3NVDDqM7:TR?= NIHlXmkzOWkEoB?= NHv3RoZFVVOR MWnpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NEXBfYUzPTR{NkW0PC=>
NCI-H23 Mm\HSpVv[3Srb36gRZN{[Xl? NW\oe4dzOTEEoN88US=> NWHUR2hNOjGqwrC= NIrO[llFVVOR NHvMe4Rl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> MmTuNlU1OjZ3NEi=
A2780 MnrjSpVv[3Srb36gRZN{[Xl? MV2xNOKh|ryP M13ZSVIycMLi NHXMTXFFVVOR NGHjepNl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> NVL4NI9KOjV2Mk[1OFg>
HCT116  NHrlXnZHfW6ldHnvckBCe3OjeR?= NYHnepJ{OTBiwsXN NHPGOGIzPCCq NHK5cI1k[XW|ZYOgZUBxPTNvZHXw[Y5l\W62IITleJJieGyxaXSgS|Eu[XK{ZYP0JIlvKGSrcHzvbYQhUEOWMUG2JINtd26nczDEN{BidmRiREi= NWjn[WJCOjV|OECwOVU>
MCF-10CA1a M4rYVmZ2dmO2aX;uJGF{e2G7 Mlf4NVDDqM7:TR?= NV;PNFdpPDhiaB?= Mm[0SG1UVw>? MU\pcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ MmnZNlUzPTd5Mkm=
MCF-10A1  MX7GeY5kfGmxbjDBd5NigQ>? Mnf1NVDDqM7:TR?= MYOyOE81QCCq MWXEUXNQ MmLabY5pcWKrdIOgcYloemG2aX;uJI9nKG6xcn3hcEBjemWjc4Sg[ZBqfGinbHnhcOKh NWH3O5VMOjV{NUe3Nlk>
MCF-10CA1a NWPIWJE5TnWwY4Tpc44hSXO|YYm= M{GzO|ExyqEQvF2= M2ruVVI1KGh? M4i4emROW09? NYS1TodW\GWlcnXhd4V{KHSqZTDUS2Yu|rJ|LXnu[JVk\WRibWLORUBt\X[nbIOgc4ZOVVB{LNMgUW1RQSxiYX7kxsBqdnSnZ4LpcuKh|rMEoEO= MYGyOVI2Pzd{OR?=
MCF-10CA1a NVP0WotUTnWwY4Tpc44hSXO|YYm= NH6wVW0yOMLizszN M1S1U|I1KGh? MojTSG1UVw>? NXrzN5RqcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MYiyOVI2Pzd{OR?=
SK-BR-7 NVrJUnBGTnWwY4Tpc44hSXO|YYm= MoTBNVDDqM7:TR?= M1z4W|I1KGh? NVu5TGpXTE2VTx?= NIjxbo5qdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NH7VUmgzPTJ3N{eyPS=>
SUM102PT M4XPWmZ2dmO2aX;uJGF{e2G7 NFfyUmUyOMLizszN MXeyOEBp MkPUSG1UVw>? MmHBbY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w MoK0NlUzPTd5Mkm=
RAW 264.7 MW\GeY5kfGmxbjDBd5NigQ>? NFLaZ|EyOMLizszN MonkN|AhdWmw NETnXpdxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> MkC1NlUyPzJ3NEe=
RAW 264.7 MYjGeY5kfGmxbjDBd5NigQ>? MlrGNVDDqM7:TR?= MVmzNEBucW5? MXTy[YR2[2W|IITo[UBNWFNvYYXncYVvfGWmIITo[UBPTi4QulKgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHjeIl3cXS7 NVrjSHJSOjVzN{K1OFc>
RAW 264.7 NH;WdIxHfW6ldHnvckBCe3OjeR?= MnHpNVDDqM7:TR?= Mn3RN|AhdWmw MYrpcohq[mm2czDMVHMucW6mdXPl[EBPVyCycn;keYN1cW:wwrC= M13RSVI2OTd{NUS3
MCF7  MnO0R4VtdCCYaXHibYxqfHliQYPzZZk> M1HYWVIvPSEEtV2= NH2wcng2KGR? NHLTR4JFVVOR NHOzfYp{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u NV\vOo14OjVyOEW5NFI>
MCF7  NXfyNlJLTnWwY4Tpc44hSXO|YYm= NF;5OYkzNjViwsXN MluzOFghcA>? NFToZ5FFVVOR M2DFRoRm[3KnYYPld{B1cGViaH;tc4xw\2:3czDEV2IhemWyYXnyJIZz\XG3ZX7jbYV{ Mmf4NlUxQDV7MEK=
ACHN NWHXWot3S2WubDDWbYFjcWyrdImgRZN{[Xl? NGTLR3oxNjVvMUCg{txO MVSwMVYh\A>? MWHEUXNQ Mn3LbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NX:wbHlmOjVyNke3PFc>
Caki-2 MV;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NWnucGgzOC53LUGwJO69VQ>? MUCwMVYh\A>? MknYSG1UVw>? MVTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4XhfVI2ODZ5N{i3
A498 NGfjTWxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXvyTVV2OC53LUGwJO69VQ>? M2TadFAuPiCm MmraSG1UVw>? M17rbYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NYTUVWhOOjVyNke3PFc>
115 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MkLLNE42NTFyIN88US=> NXvXNWl7OC14IHS= MYHEUXNQ NWLOPGF4cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= Ml\CNlUxPjd5OEe=
117 MmD2R4VtdCCYaXHibYxqfHliQYPzZZk> NVrrdFl5OC53LUGwJO69VQ>? MVywMVYh\A>? NWniOWFwTE2VTx?= M4PWTYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWXuTXlzOjVyNke3PFc>
ACHN NFLrNFlHfW6ldHnvckBCe3OjeR?= MoXQNE42NzFxNTFOwG0> MXu0PEBp NHjveY1FVVOR Mlm3cIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? NU\ndWl2OjVyNke3PFc>
Caki-2 MYrGeY5kfGmxbjDBd5NigQ>? NFHIXmsxNjVxMT:1JO69VQ>? NWnZcG9rPDhiaB?= MmS1SG1UVw>? MVLs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? M3XsUVI2ODZ5N{i3
A498 NF3JbWxHfW6ldHnvckBCe3OjeR?= MmT1NE42NzFxNTFOwG0> M1n3cFQ5KGh? MoLQSG1UVw>? NY\WWZhjdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NHLQ[4czPTB4N{e4Oy=>
115 Mn24SpVv[3Srb36gRZN{[Xl? M{j3VlAvPS9zL{Wg{txO M3HIO|Q5KGh? NGLJbolFVVOR NFT0cVZt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NV\lPVF3OjVyNke3PFc>
ACHN MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;UZVUh|ryP MYq0PEBp NH3yc3NFVVOR MnXObY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MoXxNlUxPjd5OEe=
Caki-2 NUWwVnBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof0OUDPxE1? NEGyTJE1QCCq NYruR4ZVTE2VTx?= NH3xPWpqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NYftPHAxOjVyNke3PFc>
A498 NUGxNHZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW[1JO69VQ>? NXjtb|BVPDhiaB?= MmX3SG1UVw>? M1fkb4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NULSWlFiOjVyNke3PFc>
115 M3:2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWS1JO69VQ>? MWG0PEBp NULvVpUyTE2VTx?= M4jjcYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> M3u4VFI2ODZ5N{i3
ACHN NWD2[lV1TnWwY4Tpc44hSXO|YYm= MWO1JO69VQ>? M{LCbVQ5KGh? NVTxNJVtTE2VTx?= MojHbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NU[0WIRyOjVyNke3PFc>
Caki-2 NHT2TYFHfW6ldHnvckBCe3OjeR?= M1PXRVUh|ryP M2K3W|Q5KGh? NVqyW4FmTE2VTx?= MV\pcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NUjxVVhvOjVyNke3PFc>
A498 MnXnSpVv[3Srb36gRZN{[Xl? MkX2OUDPxE1? Mmn5OFghcA>? NWPDdHhSTE2VTx?= NFvONmdqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg NIK0eHIzPTB4N{e4Oy=>
115 NXTqeWdqTnWwY4Tpc44hSXO|YYm= MV21JO69VQ>? Mn;3OFghcA>? M1;mWWROW09? MkjvbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NVHodFJPOjVyNke3PFc>
MOLM-13 Mmq4SpVv[3Srb36gRZN{[Xl? MmXTOuKh|ryP NGD0RZQxNThiaB?= M4\G[WROW09? NIe1WYhqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDwOVMtKE2GTUKsJJAzOSCjbnSgZYNmfHmuYYTl[EBxPTN? M{jrOFI1QDh3MEiy
MOLM-13 M3LacmZ2dmO2aX;uJGF{e2G7 NH:yW4U3yqEQvF2= NUXxXpo4PiCq MoDRSG1UVw>? Mnvz[Y5p[W6lZYOgeIhmKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFJDKGGwZDDo[YF1KHOqb3PrJJBzd3SnaX7zJGh{eDJ5IHHu[EBJe3B7MB?= M4rHNlI1QDh3MEiy
HepG2 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\VO|IhcA>? MXvEUXNQ NV3hTIQzUUN3ME2zOU45PiEEsTCyMlkh|ryP MkftNlQ5QDR6MEm=
HepG2/As NYfQNZBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn;WO|IhcA>? Ml62SG1UVw>? NGniendKSzVyPU[4MlE{KMLzIEmuOkDPxE1? NV20NnloOjR6OES4NFk>
SMMC7721 NILCS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUS3NkBp NEm1NW1FVVOR MkHHTWM2OD1|MT6yPEDDuSB2LkKg{txO M1i5ZVI1QDh2OEC5
SMMC7721/Ac NV3ZR3BET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXmOoI4OiCq M4\KS2ROW09? MmezTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? NYPPWWp{OjR6OES4NFk>
Huh-7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzuO|IhcA>? MVrEUXNQ NXrsXXBXUUN3ME2zN{46PiEEsTCzMlkh|ryP MUSyOFg5PDhyOR?=
Hep3B MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETOb2Y4OiCq M17neWROW09? NFL4U2pKSzVyPUKwMlE5KMLzIEGuPFQh|ryP MUWyOFg5PDhyOR?=
HepG2 MYXBdI9xfG:|aYOgRZN{[Xl? MkPibY5lfWOnczDhdI9xfG:|aYO= MVeyOFg5PDhyOR?=
SMMC7721 M1rEfmFxd3C2b4Ppd{BCe3OjeR?= MnvQbY5lfWOnczDhdI9xfG:|aYO= NVrUfG91OjR6OES4NFk>
Huh-7 Mo\xRZBweHSxc3nzJGF{e2G7 NEfPPXBqdmS3Y3XzJIFxd3C2b4Ppdy=> Mn;UNlQ5QDR6MEm=
Hep3B MWPBdI9xfG:|aYOgRZN{[Xl? MlzWbY5lfWOnczDhdI9xfG:|aYO= MYiyOFg5PDhyOR?=
U2OS  MmCzSpVv[3Srb36gRZN{[Xl? MYiyNEDPxE1? NXjEW3B5OjRiaB?= MnfSbY5kemWjc3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhSkOOMlGxMEBDS0y[TNMgZY5lSkOOVx?= Mm\nNlQ5Pjd{NUm=
AML2 NFrwWI1CeG:ydH;zbZMhSXO|YYm= MUeyM|ExKM7:TR?= MUOyOE81QCCq MX7pcoR2[2W|IHHwc5B1d3Orcx?= M37TPVI1PjV7N{S5
MOML13 Mnq0RZBweHSxc3nzJGF{e2G7 NFvSR4szNzFyIN88US=> M2\wNVI1NzR6IHi= MYjpcoR2[2W|IHHwc5B1d3Orcx?= NFrCeoozPDZ3OUe0PS=>
AML2 NX3GWGd4TnWwY4Tpc44hSXO|YYm= NETwZWsyOM7:TR?= NFP0[5YzNzRiaB?= MV\pcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= M33vTFI1PjV7N{S5
AML3 MVXGeY5kfGmxbjDBd5NigQ>? MXyxNO69VQ>? NGDyb4wzNzRiaB?= NUTB[HV1cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NEfWOWMzPDZ3OUe0PS=>
MOML13 MYXGeY5kfGmxbjDBd5NigQ>? NHnQZYkyOM7:TR?= M1LO[|IwPCCq MlfXbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= NVHuW29ROjR4NUm3OFk>
BeWo NXmzWpNUTnWwY4Tpc44hSXO|YYm= M2nqTVMxKML3TR?= NVjScHVpOjRiaB?= M2\6e4lv[3KnYYPld{BxPTNuIF3kcVItKHB{MTDhcoQhWHWvYTDheEB1cGVicILveIVqdiCuZY\lcC=> NH;0OHUzPDR7OEG1OC=>
BeWo M17he2Fxd3C2b4Ppd{BCe3OjeR?= NUnV[IdLOzBiwsXN MnTDNlQhcA>? MYnpcoNz\WG|ZYOgZZBweHSxc3nz NVPrcZlUOjR2OUixOVQ>
OCI M2TBdmZ2dmO2aX;uJGF{e2G7 M1;ER|ExKM7:TR?= MnPjNlQhcA>? M2XibZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= M1XJclI1PDd|NU[y
MOLM NGLkNZJHfW6ldHnvckBCe3OjeR?= MX2xNEDPxE1? M{TMe|I1KGh? MnXFeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w NHzJRZgzPDR5M{W2Ni=>
U2OS  MkL5SpVv[3Srb36gRZN{[Xl? MnyxNlAh|ryP MlHPNlQhcA>? NHPlXlBqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MU[yOFM3PjByNx?=
RKO M{LDW2Z2dmO2aX;uJGF{e2G7 M{fUVVIxKM7:TR?= MWqyOEBp MmXXbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? MY[yOFM3PjByNx?=
U2OS  NGLseWZHfW6ldHnvckBCe3OjeR?= NXHNUYN6OjBizszN MnzaNlQhcA>? M3qyS4lv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u M3rJS|I1OzZ4MEC3
RKO MoPGSpVv[3Srb36gRZN{[Xl? MU[yNEDPxE1? NYfVW3A5OjRiaB?= M{i3VYlv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u M3jCN|I1OzZ4MEC3
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HuH-7 MojGR4VtdCCYaXHibYxqfHliQYPzZZk> MU[xMlI2NTJyIN88US=> NEnocGgzPC92OD:3NkBp MYXEUXNQ MmrnbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= NWjqSWhNOjR{OE[zNVI>
SMMC-7721  MYfBdI9xfG:|aYOgRZN{[Xl? MlHJNlAh|ryP NGrsTZk1QCCq M4nOcWROW09? NWGyWpB{cW6mdXPld{BieG:ydH;zbZM> NHXYRmEzPDJ6NkOxNi=>
HuH-7 NG\NNIVCeG:ydH;zbZMhSXO|YYm= MoSxNlAh|ryP NW\NXohQPDhiaB?= M4\adGROW09? NILze2hqdmS3Y3XzJIFxd3C2b4Ppdy=> NGHTe|czPDJ6NkOxNi=>
SMMC-7721  NGj5WlZHfW6ldHnvckBCe3OjeR?= Mn;LNVAh|ryP M4rNOFM3KGh? MWDEUXNQ NXniSWpL\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? Mn;VNlQzQDZ|MUK=
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AT2 MXHGeY5kfGmxbjDBd5NigQ>? M3XYc|UwOTBizszN MkC2cIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? MljkNlQzPDB{MEO=
REH M2rsVWZ2dmO2aX;uJGF{e2G7 MUi1M|ExKM7:TR?= M1XpRoxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MVKyOFI1ODJyMx?=
UoCB6 NXXJT45zTnWwY4Tpc44hSXO|YYm= M3\FV|UwOTBizszN MmrScIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? MVyyOFI1ODJyMx?=
AT2 NXK5U2V5S2WubDDWbYFjcWyrdImgRZN{[Xl? NGriO4kxNTJ3IN88US=> M2LYSolvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NFHX[5UzPDJ2MEKwNy=>
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UoCB6 M{LqfGNmdGxiVnnhZoltcXS7IFHzd4F6 MViwMVI2KM7:TR?= NWrHVGRqcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NEPWN2IzPDJ2MEKwNy=>
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H460 M4jTe2Z2dmO2aX;uJGF{e2G7 MoT5OU8yOC9{MDFOwG0> NHGzblAzPCCq NX2xe3p4fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NGXINFMzPDF|NkG0Oy=>
Lovo  M1nMSGZ2dmO2aX;uJGF{e2G7 M1LtOFUwOTBxMkCg{txO MmCwNlQhcA>? MmjZeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NFTPd3UzPDF|NkG0Oy=>
A2780 MW\BdI9xfG:|aYOgRZN{[Xl? M3W1OFUwOTBxMkCg{txO Mmr6NlQhcA>? NIjkTYlmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? MYeyOFE{PjF2Nx?=
H460 NIL5fXRCeG:ydH;zbZMhSXO|YYm= MWG1M|ExNzJyIN88US=> MW[yOEBp NWLhdIE6\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? MlLSNlQyOzZzNEe=
Lovo  M3HxO2Fxd3C2b4Ppd{BCe3OjeR?= NHT5dJk2NzFyL{KwJO69VQ>? NIDrXIkzPCCq MYflcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> NIruRXEzPDF|NkG0Oy=>

... Click to View More Cell Line Experimental Data

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 slightly soluble or 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 (g) = Concentration (mol/L) × Volume (L) × 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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    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):
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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:

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

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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.

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID