Nutlin-3

For research use only. Not for use in humans.

Catalog No.S1061

32 publications

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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Selleck's Nutlin-3 has been cited by 32 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 NYXITHNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGqxUpA2yqEQvF2= NY[zOW04PDkEoHi= NGjZU5hjdG:la4OgNlcuV0iFLXnu[JVk\WRiY3XscEBxem:uaX\ldoF1cW:wIHPvcZBiemGkbHWgeI8hfGijdDDv[kBj[XOjbDDs[ZZmdHN? NVHCTFRQOjZ|NUC1OlU>
NP69 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHZTWM2OD1|MT62PeKyOi53NDFOwG0> NHrrWGUzPjJ3MkW3OS=>
NP460 NWTpR5BCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXiR2hKSzVyPUKyMlg2yrFzLkG4JO69VQ>? NHO0VGszPjJ3MkW3OS=>
C666-1 NYDsfnF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nlRmlEPTB;MUmuPVXDuThwOUOg{txO NF[1Om4zPjJ3MkW3OS=>
C666-1 M1rBPWNmdGxiVnnhZoltcXS7IFHzd4F6 NUO4TY9{OTBiwsXN NXnYSWp5PDhiaB?= M4jwPGROW09? NFuycY5{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDjbZNxdGG2aX6= MVSyOlI2OjV5NR?=
C666-1  NHzrdlBHfW6ldHnvckBCe3OjeR?= MofuNVAhyrWP M3[4XFI1KGh? NU\QNlJVTE2VTx?= NWDnSmgx[WO2aY\heIV{KHSqZTDwOVMheGG2aIfhfUwhfXC{ZXf1cIF1cW6pIIC1N{wheDJzIHHu[EBO\G1{ M4CzO|I3OjV{NUe1
C666-1 NUXxdWpqSXCxcITvd4l{KEG|c3H5 MmT2NVAhyrWP MWO0PE84OiCq NFi4R4ZFVVOR NXrFVIhHe2Wwc3n0bZpmeyCFNk[2MVEh[2WubIOgeI8h[2m|cHzheIlvNWmwZIXj[YQh[XCxcITvd4l{ MkXKNlYzPTJ3N{W=
A549 M3G0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXBVIkzPCCq MoDwTWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? MYSyOlEzPTJ|MB?=
A549-NTC MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4P4U|I1KGh? MYfJR|UxRTF7LkSyJOKyKDFwOU[g{txO NVL5bHRJOjZzMkWyN|A>
A549-920 MofOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVOyOEBp NXXpUpBnUUN3ME2zN{45PSEEsTC0Mlg1KM7:TR?= MWmyOlEzPTJ|MB?=
CRL-5908 MnjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnXdlhWOjRiaB?= MV\JR|UxRTN6LkexJOKyKDJwNEOg{txO MYiyOlEzPTJ|MB?=
L6 NWPkTIxTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTTNVDDqM7:TdMg M{PDUlI1NzR6L{eyJIg> MY\EUXNQ NHTW[|BqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MUCyOVg4OTd7NB?=
C2C12 MkHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[xNOKh|ryPwrC= NXznVZhiOjRxNEivO|IhcA>? MYnEUXNQ NHvlU4xqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? NXvnOpVMOjV6N{G3PVQ>
MCF-7  NIjUTGxHfW6ldHnvckBCe3OjeR?= NVfhSndvOTEEoN88US=> Mn\VSG1UVw>? MVfpcohq[mm2czDjfYNtcW5iREGgZY5lKESrY3XyxsA> NVrtU5BuOjV5MEK3NFM>
DU4475  NXvFblNvTnWwY4Tpc44hSXO|YYm= Ml;TOU8yOC9{MDFOwG0> Mn;DNlTDqGh? M2XaeYRwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> MV2yOVU1PzF5NB?=
SMMC-7721 Mlv3SpVv[3Srb36gRZN{[Xl? M4nrO|ExKM7:TR?= NVL4Z|VvPDhiaB?= NGOzT25FVVOR Mme1Z4F2e2W|IFTORUBFW0JiZHHtZYdm Mn3JNlU2PDR|NkG=
SMMC-7721 MonNSpVv[3Srb36gRZN{[Xl? NXjhc3drOTBizszN NVzTWWFuPDhiaB?= NYrEO3VoTE2VTx?= MlrtbY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> NFrFZnczPTV2NEO2NS=>
SMMC-7721 M{n3dmZ2dmO2aX;uJGF{e2G7 MYOxNEDPxE1? NH3wc3Q1QCCq M3u4N2ROW09? MUXpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B MX[yOVU1PDN4MR?=
SMMC-7721 M1r3d2Z2dmO2aX;uJGF{e2G7 MWmxNEDPxE1? NXzZc2ZqOzZiaB?= M3LjNmROW09? M2H0O4NifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 M4r2VlI2PTR2M{[x
MCF-7 NGPGXmZHfW6ldHnvckBCe3OjeR?= MoPaNVDDqM7:TR?= MYqwMVI1KGh? Mmj6bY5lfWOnczDwOVMh[W6mIICyNU9EcXBz M{i5dlI2PDh{M{ez
OVCAR10 MYTGeY5kfGmxbjDBd5NigQ>? MY[xNOKh|ryP M3PBWlIycMLi MW\EUXNQ MnfjbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MnTiNlU1OjZ3NEi=
NCI-H23 NEjCUnNHfW6ldHnvckBCe3OjeR?= MUCxNOKh|ryP MXyyNYjDqA>? MX\EUXNQ MYPpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz MlrCNlU1OjZ3NEi=
A2780 MYPGeY5kfGmxbjDBd5NigQ>? NFjjV2oyOMLizszN MUKyNYjDqA>? MXHEUXNQ M2PzXIlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> M{i4fVI2PDJ4NUS4
NCI-H23 MWLGeY5kfGmxbjDBd5NigQ>? M3vKTFExyqEQvF2= Mkm1NlFpyqB? MnPuSG1UVw>? MVXk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= NIn0O5EzPTR{NkW0PC=>
A2780 MUHGeY5kfGmxbjDBd5NigQ>? NXy4XWJSOTEEoN88US=> MUSyNYjDqA>? M4faemROW09? NELONXNl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> MonLNlU1OjZ3NEi=
HCT116  MXHGeY5kfGmxbjDBd5NigQ>? Ml7WNVAhyrWP M4jNVFI1KGh? MVPjZZV{\XNiYTDwOVMu\GWyZX7k[Y51KHSndILhdIxwcWRiR{GtZZJz\XO2IHnuJIRqeGyxaXSgTGNVOTF4IHPsc45meyCGMzDhcoQhTDh? NE\2PWIzPTN6MEC1OS=>
MCF-10CA1a NHHPTHVHfW6ldHnvckBCe3OjeR?= M3K5bFExyqEQvF2= NWnGXIt[PDhiaB?= M3u4dmROW09? M4DuXYlvcGmkaYTzJIJie2GuIHnueoF{cW:wIHHu[EBz\WS3Y3XkJHRITi4QskOtbY5lfWOnZDDpcpZie2mxbjD0c{Bj[XOjbDDs[ZZmdHN? M4nSbFI2OjV5N{K5
MCF-10A1  Mnj5SpVv[3Srb36gRZN{[Xl? NHrKRooyOMLizszN NFm0TJgzPC92ODDo NX3MPFVqTE2VTx?= NYjnW5pycW6qaXLpeJMhdWmpcnH0bY9vKG:oIH7vdo1idCCkcnXhd5Qh\XCrdHjlcIlidMLi MlfqNlUzPTd5Mkm=
MCF-10CA1a MknKSpVv[3Srb36gRZN{[Xl? M1TjZ|ExyqEQvF2= M{HDZVI1KGh? NYjGSmJWTE2VTx?= M3\yXIRm[3KnYYPld{B1cGViVFfGMe6zOy2rbnT1Z4VlKG2UTlGgcIV3\Wy|IH;mUW1ROi{EoF3NVFktKGGwZNMgbY51\We{aX9CpO6zyqB| Mk\wNlUzPTd5Mkm=
MCF-10CA1a NF\DPYlHfW6ldHnvckBCe3OjeR?= NEXxeGMyOMLizszN MYWyOEBp NEfHco5FVVOR NXjQVZdzcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MWKyOVI2Pzd{OR?=
SK-BR-7 NHq4fY9HfW6ldHnvckBCe3OjeR?= MVyxNOKh|ryP M2HYNlI1KGh? NUjYO3ZqTE2VTx?= MmH4bY5pcWKrdIOgJHRITi4QskOtbY5lfWOnZDDFVGhDOsLibWLORUBidmRicILveIVqdiCneIDy[ZN{cW:w M2jHRlI2OjV5N{K5
SUM102PT NFToWJdHfW6ldHnvckBCe3OjeR?= M3;JdlExyqEQvF2= MV6yOEBp MV\EUXNQ NF7kNHdqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MVGyOVI2Pzd{OR?=
RAW 264.7 MVLGeY5kfGmxbjDBd5NigQ>? NXfUeFFmOTEEoN88US=> M{TkZVMxKG2rbh?= MnSydJJmfmWwdIOgeIhmKHB3MzDy[YR2[3Srb36gbY4hemW|cH;ud4UhfG9iTGDT MWKyOVE4OjV2Nx?=
RAW 264.7 NYDBdIRuTnWwY4Tpc44hSXO|YYm= NHSxbngyOMLizszN NF\qV2Q{OCCvaX6= MUHy[YR2[2W|IITo[UBNWFNvYYXncYVvfGWmIITo[UBPTi4QulKgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHjeIl3cXS7 MX6yOVE4OjV2Nx?=
RAW 264.7 NIG3c2FHfW6ldHnvckBCe3OjeR?= M1PxSVExyqEQvF2= Mnn6N|AhdWmw NGniTmtqdmirYnn0d{BNWFNvaX7keYNm\CCQTzDwdo9lfWO2aX;uxsA> MVuyOVE4OjV2Nx?=
MCF7  M{L4OmNmdGxiVnnhZoltcXS7IFHzd4F6 M2HoSFIvPSEEtV2= NFPLN5k2KGR? NGrC[2VFVVOR Mkj4d4Vve2m2aYrld{BOS0Z5IITvJHBCWlBiaX7obYJqfGmxbh?= NEftTVEzPTB6NUmwNi=>
MCF7  NEWzTJVHfW6ldHnvckBCe3OjeR?= MUWyMlUhyrWP NU\Mb2VQPDhiaB?= M4LOdWROW09? M3rBSYRm[3KnYYPld{B1cGViaH;tc4xw\2:3czDEV2IhemWyYXnyJIZz\XG3ZX7jbYV{ NWfqbnBNOjVyOEW5NFI>
ACHN NYixeVNGS2WubDDWbYFjcWyrdImgRZN{[Xl? NVjKTWdTOC53LUGwJO69VQ>? MXKwMVYh\A>? M1nDd2ROW09? M{fEO4lvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWPWdFFVOjVyNke3PFc>
Caki-2 M1rTbWNmdGxiVnnhZoltcXS7IFHzd4F6 NF\Gem8xNjVvMUCg{txO NX\nUZRROC14IHS= MUTEUXNQ MmXNbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1noeFI2ODZ5N{i3
A498 MoXnR4VtdCCYaXHibYxqfHliQYPzZZk> M3GxTlAvPS1zMDFOwG0> NEjzPWMxNTZiZB?= NYqyVnI2TE2VTx?= MXTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NIjMZ4kzPTB4N{e4Oy=>
115 NFizOXNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmrZNE42NTFyIN88US=> M17GSVAuPiCm M4WxfWROW09? MWDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXzSTGFmOjVyNke3PFc>
117 NW\TcHFbS2WubDDWbYFjcWyrdImgRZN{[Xl? Mon1NE42NTFyIN88US=> Ml60NE03KGR? M3nvV2ROW09? NIPhO2NqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MkXVNlUxPjd5OEe=
ACHN NIXS[3BHfW6ldHnvckBCe3OjeR?= M2Hl[|AvPS9zL{Wg{txO NU\sbFd4PDhiaB?= NGPNPGJFVVOR NHXBT3Nt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NITBWIozPTB4N{e4Oy=>
Caki-2 MYPGeY5kfGmxbjDBd5NigQ>? NEH0[WwxNjVxMT:1JO69VQ>? Mk\COFghcA>? NWXUemRWTE2VTx?= M2C4eIxm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MVuyOVA3Pzd6Nx?=
A498 NFfqdmFHfW6ldHnvckBCe3OjeR?= M1nRd|AvPS9zL{Wg{txO NEn0cFA1QCCq MV3EUXNQ MULs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MVSyOVA3Pzd6Nx?=
115 NHu4UVFHfW6ldHnvckBCe3OjeR?= M2nacFAvPS9zL{Wg{txO M4XRR|Q5KGh? MmLsSG1UVw>? NFnhZnBt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NI\yN2MzPTB4N{e4Oy=>
ACHN MmWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LR[FUh|ryP NUG1TpN2PDhiaB?= NYHkbYJQTE2VTx?= M1i5T4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MV2yOVA3Pzd6Nx?=
Caki-2 MnPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXDNlk2KM7:TR?= NF;1T5o1QCCq NUL3coVGTE2VTx?= MVPpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MoTzNlUxPjd5OEe=
A498 M2rUOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYP0UnJSPSEQvF2= MVK0PEBp Mmi5SG1UVw>? NGHMWlBqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> MmezNlUxPjd5OEe=
115 NIrhdG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy2fXJqPSEQvF2= MkLFOFghcA>? M{PtfmROW09? NGD4SlFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> M32yRVI2ODZ5N{i3
ACHN Mn3jSpVv[3Srb36gRZN{[Xl? NVLLb2dJPSEQvF2= NGO2W2s1QCCq M1jOTmROW09? NXfMfZk4cW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MnLpNlUxPjd5OEe=
Caki-2 NIq3O3FHfW6ldHnvckBCe3OjeR?= Ml3MOUDPxE1? NVztR5FUPDhiaB?= NILMR2dFVVOR NH3pcZJqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MknNNlUxPjd5OEe=
A498 M1;m[mZ2dmO2aX;uJGF{e2G7 NHj2T3I2KM7:TR?= M3fRdFQ5KGh? NFrXSpNFVVOR NEPYSlNqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MoLpNlUxPjd5OEe=
115 NXfDPXNWTnWwY4Tpc44hSXO|YYm= NY\QR4hRPSEQvF2= NFT0fpQ1QCCq NEfHdVNFVVOR MWjpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NEjyXFIzPTB4N{e4Oy=>
MOLM-13 M4HBd2Z2dmO2aX;uJGF{e2G7 NHi3XlA3yqEQvF2= MlnmNE05KGh? MljLSG1UVw>? M4DJXIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? MkLuNlQ5QDVyOEK=
MOLM-13 NWfyeZJ[TnWwY4Tpc44hSXO|YYm= MlvsOuKh|ryP MUW2JIg> MVrEUXNQ MoH4[Y5p[W6lZYOgeIhmKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFJDKGGwZDDo[YF1KHOqb3PrJJBzd3SnaX7zJGh{eDJ5IHHu[EBJe3B7MB?= MojaNlQ5QDVyOEK=
HepG2 NWP2fppbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjMO|IhcA>? Mn3wSG1UVw>? M3\ON2lEPTB;M{WuPFYhyrFiMj65JO69VQ>? M{LRelI1QDh2OEC5
HepG2/As NFj0NVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmK5O|IhcA>? M3PnSmROW09? NUiwZoVzUUN3ME22PE4yOyEEsTC5MlYh|ryP MWqyOFg5PDhyOR?=
SMMC7721 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXq3NkBp NEixSppFVVOR MkHITWM2OD1|MT6yPEDDuSB2LkKg{txO NVjFZm9EOjR6OES4NFk>
SMMC7721/Ac MlPkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfDTI44OiCq MYLEUXNQ MWHJR|UxRTV3LkKxJOKyKDVwMEOg{txO M{\qclI1QDh2OEC5
Huh-7 M2XERWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnGxO|IhcA>? MkflSG1UVw>? NIfnWWJKSzVyPUOzMlk3KMLzIEOuPUDPxE1? MmTONlQ5QDR6MEm=
Hep3B NH7C[GpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fROlczKGh? MYXEUXNQ MmnpTWM2OD1{MD6xPEDDuSBzLki0JO69VQ>? NYXhR|RDOjR6OES4NFk>
HepG2 NXrJbpV{SXCxcITvd4l{KEG|c3H5 NXvN[o9JcW6mdXPld{BieG:ydH;zbZM> MnPPNlQ5QDR6MEm=
SMMC7721 NF;zRWdCeG:ydH;zbZMhSXO|YYm= Mn\ubY5lfWOnczDhdI9xfG:|aYO= MV:yOFg5PDhyOR?=
Huh-7 Mnq0RZBweHSxc3nzJGF{e2G7 NWTCdG4{cW6mdXPld{BieG:ydH;zbZM> MYWyOFg5PDhyOR?=
Hep3B MkPDRZBweHSxc3nzJGF{e2G7 MWXpcoR2[2W|IHHwc5B1d3Orcx?= NHf5OVAzPDh6NEiwPS=>
U2OS  Mmf6SpVv[3Srb36gRZN{[Xl? MlL3NlAh|ryP NUjLbIVZOjRiaB?= MlfSbY5kemWjc3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhSkOOMlGxMEBDS0y[TNMgZY5lSkOOVx?= MnjXNlQ5Pjd{NUm=
AML2 NYfre|g5SXCxcITvd4l{KEG|c3H5 MmLpNk8yOCEQvF2= MXSyOE81QCCq NGHxUIJqdmS3Y3XzJIFxd3C2b4Ppdy=> NYmyWXBbOjR4NUm3OFk>
MOML13 MXPBdI9xfG:|aYOgRZN{[Xl? NXXLZZplOi9zMDFOwG0> M4TSO|I1NzR6IHi= Ml3PbY5lfWOnczDhdI9xfG:|aYO= Ml:3NlQ3PTl5NEm=
AML2 NELodY1HfW6ldHnvckBCe3OjeR?= MYKxNO69VQ>? NYf6XGJ3Oi92IHi= Mke0bY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MY[yOFY2QTd2OR?=
AML3 Mkn3SpVv[3Srb36gRZN{[Xl? NUHWcYY2OTEQvF2= M3HoOlIwPCCq NVvGeXJzcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> M1\UN|I1PjV7N{S5
MOML13 M13YSGZ2dmO2aX;uJGF{e2G7 MXexNO69VQ>? MoK4Nk81KGh? NVy3clZZcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MkD6NlQ3PTl5NEm=
BeWo MmjLSpVv[3Srb36gRZN{[Xl? MWCzNEDDvU1? MVmyOEBp NFnwbHZqdmO{ZXHz[ZMheDV|LDDN[I0zNCCyMkGgZY5lKFC3bXGgZZQhfGinIIDyc5RmcW5ibHX2[Yw> MWGyOFQ6QDF3NB?=
BeWo NFLOW21CeG:ydH;zbZMhSXO|YYm= MlPFN|AhyrWP MWGyOEBp NHLhVmtqdmO{ZXHz[ZMh[XCxcITvd4l{ MmLGNlQ1QThzNUS=
OCI NWLOV4VvTnWwY4Tpc44hSXO|YYm= MYmxNEDPxE1? M3LXb|I1KGh? NX73W|VufXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NFfkT3IzPDR5M{W2Ni=>
MOLM M{DTO2Z2dmO2aX;uJGF{e2G7 M1G4fVExKM7:TR?= M164NlI1KGh? M1TVVZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= MVKyOFQ4OzV4Mh?=
U2OS  NGXlXm9HfW6ldHnvckBCe3OjeR?= MYeyNEDPxE1? M2PrXVI1KGh? MlzpbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? MmD2NlQ{PjZyMEe=
RKO MkHySpVv[3Srb36gRZN{[Xl? M4PKOFIxKM7:TR?= NYjiVm9XOjRiaB?= NEi5Um9qdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MnTrNlQ{PjZyMEe=
U2OS  NVHuO|NSTnWwY4Tpc44hSXO|YYm= MX6yNEDPxE1? MmfLNlQhcA>? MorTbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MnnRNlQ{PjZyMEe=
RKO MonlSpVv[3Srb36gRZN{[Xl? Mo\2NlAh|ryP MXiyOEBp NInrS3ZqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MXGyOFM3PjByNx?=
SMMC-7721  M1jMUGNmdGxiVnnhZoltcXS7IFHzd4F6 NYO2WGpoOS5{NT2yNEDPxE1? NF3DVm0zPC92OD:3NkBp MnrxSG1UVw>? NX3uZpREcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NXfwb3NnOjR{OE[zNVI>
HuH-7 MmXCR4VtdCCYaXHibYxqfHliQYPzZZk> MlHPNU4zPS1{MDFOwG0> NHvUcpgzPC92OD:3NkBp MoqySG1UVw>? NWnaUlNjcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NYPXWYxSOjR{OE[zNVI>
SMMC-7721  NYXqc4k5SXCxcITvd4l{KEG|c3H5 M1X5[FIxKM7:TR?= NH21Npc1QCCq M{PWPWROW09? NXmzUHFWcW6mdXPld{BieG:ydH;zbZM> MmfrNlQzQDZ|MUK=
HuH-7 MYjBdI9xfG:|aYOgRZN{[Xl? MkDjNlAh|ryP MWq0PEBp NGjtd4hFVVOR M1q1eolv\HWlZYOgZZBweHSxc3nz NYq5PJBOOjR{OE[zNVI>
SMMC-7721  MnrzSpVv[3Srb36gRZN{[Xl? MmryNVAh|ryP MYOzOkBp MY\EUXNQ MXTkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> M3nOU|I1Ojh4M{Gy
HuH-7 NIX4V2JHfW6ldHnvckBCe3OjeR?= NIj3PXQyOCEQvF2= NXnYUVdtOzZiaB?= NY\UblZZTE2VTx?= MV;kc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> NH;w[XczPDJ6NkOxNi=>
AT2 NX;ldGtUTnWwY4Tpc44hSXO|YYm= MV:1M|ExKM7:TR?= MYXs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MnjpNlQzPDB{MEO=
REH M{TOfmZ2dmO2aX;uJGF{e2G7 M1zpOFUwOTBizszN MoHKcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? MWiyOFI1ODJyMx?=
UoCB6 NXvRVYdITnWwY4Tpc44hSXO|YYm= NIrtOIw2NzFyIN88US=> Ml3BcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? NGe4NZMzPDJ2MEKwNy=>
AT2 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MWiwMVI2KM7:TR?= MnvpbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M1nVU|I1OjRyMkCz
REH NVjHV3RGS2WubDDWbYFjcWyrdImgRZN{[Xl? MX:wMVI2KM7:TR?= Mn3qbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MkXKNlQzPDB{MEO=
UoCB6 MkD5R4VtdCCYaXHibYxqfHliQYPzZZk> Mm\BNE0zPSEQvF2= M4nuWYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? M13zVlI1OjRyMkCz
A2780 MW\GeY5kfGmxbjDBd5NigQ>? NIrsUHM2NzFyL{KwJO69VQ>? NVjTd3lCOjRiaB?= MXv1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? NWKyPJg2OjRzM{[xOFc>
H460 NVv2XYFLTnWwY4Tpc44hSXO|YYm= MlLGOU8yOC9{MDFOwG0> M3v1fFI1KGh? MV71dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? MlvPNlQyOzZzNEe=
Lovo  NXLjR3VQTnWwY4Tpc44hSXO|YYm= MoT1OU8yOC9{MDFOwG0> NIj3S3AzPCCq MoPreZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NWK5VIlSOjRzM{[xOFc>
A2780 MYXBdI9xfG:|aYOgRZN{[Xl? M37mR|UwOTBxMkCg{txO NHjjTZozPCCq MkP6[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MmHrNlQyOzZzNEe=
H460 NF;VXoRCeG:ydH;zbZMhSXO|YYm= MUG1M|ExNzJyIN88US=> MlfyNlQhcA>? NIfKdHNmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? Mnf1NlQyOzZzNEe=
Lovo  NXzL[VJUSXCxcITvd4l{KEG|c3H5 NG[xXmQ2NzFyL{KwJO69VQ>? M{\aRlI1KGh? NVizfmNw\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? M{nrR|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]

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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
  • 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
Smiles COC1=CC(=C(C=C1)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(Cl)C=C4)C5=CC=C(Cl)C=C5)OC(C)C

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