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 MmTyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Wz[|XDqM7:TR?= MlXoOFjDqGh? NWDYU4lV[myxY3vzJFI4NU:KQz3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbjDjc41x[XKjYnzlJJRwKHSqYYSgc4Yh[mG|YXygcIV3\Wy| M4DzeFI3OzVyNU[1
NP69 NXvZSXB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHHTWM2OD1|MT62PeKyOi53NDFOwG0> NHrUWGgzPjJ3MkW3OS=>
NP460 NYrlTWF5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3f0T2lEPTB;MkKuPFXDuTFwMUig{txO MVmyOlI2OjV5NR?=
C666-1 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\JTHZyUUN3ME2xPU46PcLzOD65N{DPxE1? M3\CeFI3OjV{NUe1
C666-1 NWjUfIFYS2WubDDWbYFjcWyrdImgRZN{[Xl? NUOwRWs4OTBiwsXN M{W1eFQ5KGh? NVHGbZI6TE2VTx?= MmXDd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw NWnCXo06OjZ{NUK1O|U>
C666-1  MUXGeY5kfGmxbjDBd5NigQ>? M2DZeFExKML3TR?= Mmn1NlQhcA>? MojlSG1UVw>? MVHhZ5RqfmG2ZYOgeIhmKHB3MzDwZZRpf2G7LDD1dJJm\3WuYYTpcocheDV|LDDwNlEh[W6mIF3kcVI> NHLGe4kzPjJ3MkW3OS=>
C666-1 NHK4bVJCeG:ydH;zbZMhSXO|YYm= MUexNEDDvU1? NWTjUm9EPDhxN{KgbC=> Ml25SG1UVw>? MWnz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzDjbZNxdGG2aX6tbY5lfWOnZDDhdI9xfG:|aYO= M2iyOlI3OjV{NUe1
A549 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITCR3MzPCCq Ml3nTWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? Mlm2NlYyOjV{M{C=
A549-NTC MmjQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPrNlQhcA>? NYDLe3hNUUN3ME2xPU41OiEEsTCxMlk3KM7:TR?= M1nES|I3OTJ3MkOw
A549-920 NILsW2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nHS|I1KGh? M1nIZWlEPTB;M{OuPFUhyrFiND64OEDPxE1? MWGyOlEzPTJ|MB?=
CRL-5908 NVXZelBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\vR|I1KGh? NYXXdIpJUUN3ME2zPE44OSEEsTCyMlQ{KM7:TR?= MmDzNlYyOjV{M{C=
L6 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33PZ|ExyqEQvF5CpC=> M{nR[VI1NzR6L{eyJIg> MX\EUXNQ Mof6bY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v NXj3XHdKOjV6N{G3PVQ>
C2C12 NGezU4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWC5bIwxOTEEoN88UeKh NEj5ZpIzPC92OD:3NkBp MX;EUXNQ M2DBWolvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NH7JZpczPTh5MUe5OC=>
MCF-7  NGDXNINHfW6ldHnvckBCe3OjeR?= M{faSlExyqEQvF2= MWLEUXNQ MmXUbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh MmTuNlU4ODJ5MEO=
DU4475  NXnKZ5l{TnWwY4Tpc44hSXO|YYm= NWD6[WJFPS9zMD:yNEDPxE1? NVPw[lBlOjUEoHi= M3PT[4Rwf26{ZXf1cIF1\XNiVH;jZU0yKGSxc3Wg[IVx\W6mZX70cJk> M13WNVI2PTR5MUe0
SMMC-7721 MWTGeY5kfGmxbjDBd5NigQ>? NEjpTlMyOCEQvF2= NITqSZQ1QCCq NXzRPJR3TE2VTx?= M1LRdINifXOnczDEUmEhTFOEIHThcYFo\Q>? NWLPRXRGOjV3NESzOlE>
SMMC-7721 NXz1cVJTTnWwY4Tpc44hSXO|YYm= M{DnS|ExKM7:TR?= NF3TOI41QCCq NY\pRWtGTE2VTx?= M{TaZ4lv\HWlZYOgeIhmKGOqcn;tZZRqdi2kb4Xu[EBxem:2ZXnuJGlHUTF4IITvJJBienSrYXzsfUBtd2OjbHn6[UBqdiC2aHWgZ5l1d3CuYYPtxsA> MUiyOVU1PDN4MR?=
SMMC-7721 Mnr6SpVv[3Srb36gRZN{[Xl? NXm3WVNFOTBizszN M3zI[lQ5KGh? Ml71SG1UVw>? NHnTWWFqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C MmLXNlU2PDR|NkG=
SMMC-7721 M4K3e2Z2dmO2aX;uJGF{e2G7 NGrIXIsyOCEQvF2= NIX4WpY{PiCq MYHEUXNQ MUHjZZV{\XNidHjlJIVkfG:yaXOg[ZhxemW|c3nvckBw\iCLRlmxOi=> NXP2SnZjOjV3NESzOlE>
MCF-7 NXewfVBuTnWwY4Tpc44hSXO|YYm= NV\QS5R6OTEEoN88US=> NELubmgxNTJ2IHi= NHfaWoxqdmS3Y3XzJJA2OyCjbnSgdFIyN0OrcEG= MmjLNlU1QDJ|N{O=
OVCAR10 NEjhOIFHfW6ldHnvckBCe3OjeR?= NUTZeVRYOTEEoN88US=> M1Tx[|IycMLi NEnzXnNFVVOR NHfPXY9qdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ MXGyOVQzPjV2OB?=
NCI-H23 NF3kdmZHfW6ldHnvckBCe3OjeR?= NYO5WmhNOTEEoN88US=> NW\mfWJyOjGqwrC= M3q0XmROW09? NIrV[o9qdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ M2q1bVI2PDJ4NUS4
A2780 MVvGeY5kfGmxbjDBd5NigQ>? M{njfVExyqEQvF2= NF\0[|kzOWkEoB?= MWXEUXNQ MXfpcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz MlrVNlU1OjZ3NEi=
NCI-H23 MmrMSpVv[3Srb36gRZN{[Xl? NETQelUyOMLizszN MX6yNYjDqA>? NWjpOnBoTE2VTx?= NHP0[|ll\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> M2XueFI2PDJ4NUS4
A2780 M1rWdWZ2dmO2aX;uJGF{e2G7 M{fYbVExyqEQvF2= MmDlNlFpyqB? MYnEUXNQ M{fBPIRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NGr1UWozPTR{NkW0PC=>
HCT116  Mn3OSpVv[3Srb36gRZN{[Xl? MnG0NVAhyrWP MUSyOEBp NEL2PGNk[XW|ZYOgZUBxPTNvZHXw[Y5l\W62IITleJJieGyxaXSgS|Eu[XK{ZYP0JIlvKGSrcHzvbYQhUEOWMUG2JINtd26nczDEN{BidmRiREi= NXnw[mY{OjV|OECwOVU>
MCF-10CA1a MnjWSpVv[3Srb36gRZN{[Xl? NHH3Z2wyOMLizszN NEWycIY1QCCq MmTrSG1UVw>? MVLpcohq[mm2czDiZZNidCCrbo\hd4lwdiCjbnSgdoVlfWOnZDDUS2Yu|rJ|LXnu[JVk\WRiaX72ZZNqd25idH:gZoF{[WxibHX2[Yx{ MoHWNlUzPTd5Mkm=
MCF-10A1  NXu1VJBbTnWwY4Tpc44hSXO|YYm= M3fB[FExyqEQvF2= MmSwNlQwPDhiaB?= NYnUTVllTE2VTx?= MYDpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> MW[yOVI2Pzd{OR?=
MCF-10CA1a NYHKVYt6TnWwY4Tpc44hSXO|YYm= MlvlNVDDqM7:TR?= NIXFVo0zPCCq NUPabI5tTE2VTx?= MoO4[IVkemWjc3XzJJRp\SCWR1[t{tI{NWmwZIXj[YQhdVKQQTDs[ZZmdHNib3\NUXAzNMLiTV3QPUwh[W6mwrDpcpRm\3KrbtMg{tLDqDN? NU[wdYVNOjV{NUe3Nlk>
MCF-10CA1a NHm2[lFHfW6ldHnvckBCe3OjeR?= MYCxNOKh|ryP M1L2TFI1KGh? NIP0WXNFVVOR M3nkWYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NF62ZXAzPTJ3N{eyPS=>
SK-BR-7 NXLsfXJiTnWwY4Tpc44hSXO|YYm= MkfKNVDDqM7:TR?= MVSyOEBp MmrGSG1UVw>? MWXpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? M3XKbVI2OjV5N{K5
SUM102PT MV;GeY5kfGmxbjDBd5NigQ>? NF;FN2MyOMLizszN MoK2NlQhcA>? NGnuSmpFVVOR M1;sdYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= MUiyOVI2Pzd{OR?=
RAW 264.7 MXnGeY5kfGmxbjDBd5NigQ>? MX:xNOKh|ryP NIW3SJU{OCCvaX6= NX7qWWlReHKndnXueJMhfGinIIC1N{Bz\WS3Y4Tpc44hcW5icnXzdI9ve2VidH:gUHBU MX[yOVE4OjV2Nx?=
RAW 264.7 MVHGeY5kfGmxbjDBd5NigQ>? M2\tblExyqEQvF2= M3SyS|MxKG2rbh?= MnfOdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= MVeyOVE4OjV2Nx?=
RAW 264.7 M1nqbGZ2dmO2aX;uJGF{e2G7 NIHwV|gyOMLizszN M1\QXlMxKG2rbh?= NIrGd|JqdmirYnn0d{BNWFNvaX7keYNm\CCQTzDwdo9lfWO2aX;uxsA> NF7xOXUzPTF5MkW0Oy=>
MCF7  MlvQR4VtdCCYaXHibYxqfHliQYPzZZk> M{C3NlIvPSEEtV2= M{X1SVUh\A>? NYTNdGlnTE2VTx?= M17ZOZNmdnOrdHn6[ZMhVUOINzD0c{BRSVKSIHnubIljcXSrb36= MkfDNlUxQDV7MEK=
MCF7  NYXlW|RSTnWwY4Tpc44hSXO|YYm= NYPBfJNVOi53INM1US=> NGLud|c1QCCq NWfqZlZPTE2VTx?= NILZWYpl\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? NGSzN5YzPTB6NUmwNi=>
ACHN MoH3R4VtdCCYaXHibYxqfHliQYPzZZk> NH7PU3kxNjVvMUCg{txO M3rFZlAuPiCm NIDOUo1FVVOR MXfpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MU[yOVA3Pzd6Nx?=
Caki-2 NVXnd2lUS2WubDDWbYFjcWyrdImgRZN{[Xl? MVGwMlUuOTBizszN NUfPW|dsOC14IHS= NHj4TJVFVVOR NFnLXZZqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M3uwNFI2ODZ5N{i3
A498 Mn35R4VtdCCYaXHibYxqfHliQYPzZZk> NIXpcpIxNjVvMUCg{txO NIrteZkxNTZiZB?= NG\nRmRFVVOR MY\pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWeyOVA3Pzd6Nx?=
115 NIfV[ppE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mm[2NE42NTFyIN88US=> M37aVFAuPiCm MYTEUXNQ NWLrbWhEcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M1HEOlI2ODZ5N{i3
117 NX:3XWUxS2WubDDWbYFjcWyrdImgRZN{[Xl? M{LYOFAvPS1zMDFOwG0> NHraPZExNTZiZB?= Mn;ZSG1UVw>? MUDpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUSyOVA3Pzd6Nx?=
ACHN NHvYO2dHfW6ldHnvckBCe3OjeR?= MVuwMlUwOS93IN88US=> MoLkOFghcA>? M1XaTWROW09? M{fTW4xm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz M3nH[|I2ODZ5N{i3
Caki-2 Mmr0SpVv[3Srb36gRZN{[Xl? M3SwSFAvPS9zL{Wg{txO NIGxWIc1QCCq MX\EUXNQ MlGycIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MUGyOVA3Pzd6Nx?=
A498 NXnp[pp6TnWwY4Tpc44hSXO|YYm= NYjYSHNLOC53L{GvOUDPxE1? NYSxflNkPDhiaB?= MVzEUXNQ M4DJS4xm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz M3rOZ|I2ODZ5N{i3
115 M{ixOmZ2dmO2aX;uJGF{e2G7 NVr5W2ZvOC53L{GvOUDPxE1? NHnTOmQ1QCCq MmXOSG1UVw>? NHfvPJpt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MWqyOVA3Pzd6Nx?=
ACHN MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vUflUh|ryP NIjKUXM1QCCq NGHDPHRFVVOR M17jc4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NIHnSWQzPTB4N{e4Oy=>
Caki-2 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXP1UZlMPSEQvF2= NETMfZU1QCCq MkDMSG1UVw>? NGfuUnJqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> MVyyOVA3Pzd6Nx?=
A498 NUDp[mdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGq1NYc2KM7:TR?= NG\kbnE1QCCq M4q3TmROW09? NXvvT4pscW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NXn4WplFOjVyNke3PFc>
115 NGTrWJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVK1JO69VQ>? M1my[|Q5KGh? Mk\qSG1UVw>? NVryU2RYcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh M3fEPFI2ODZ5N{i3
ACHN Mn\uSpVv[3Srb36gRZN{[Xl? NIjCTIc2KM7:TR?= MYO0PEBp MXvEUXNQ NUDmV45GcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M3KyPVI2ODZ5N{i3
Caki-2 NFXjNG5HfW6ldHnvckBCe3OjeR?= MVS1JO69VQ>? M1rEWlQ5KGh? M{j3RWROW09? MV;pcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M1ewW|I2ODZ5N{i3
A498 M{X4OGZ2dmO2aX;uJGF{e2G7 NXvTRlBwPSEQvF2= M2KzeFQ5KGh? M2\yVmROW09? NUflXmltcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MVSyOVA3Pzd6Nx?=
115 MnHXSpVv[3Srb36gRZN{[Xl? M2e5VFUh|ryP M2K0b|Q5KGh? NFW2RlRFVVOR NHXnVHpqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MXqyOVA3Pzd6Nx?=
MOLM-13 MXrGeY5kfGmxbjDBd5NigQ>? M{mwTVbDqM7:TR?= NHOzT|kxNThiaB?= MWDEUXNQ MmjWbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ MXqyOFg5PTB6Mh?=
MOLM-13 NEG0UG1HfW6ldHnvckBCe3OjeR?= MV:2xsDPxE1? MX:2JIg> MVzEUXNQ MmrN[Y5p[W6lZYOgeIhmKGGlZYT5cIF1cW:wIH;mJIhqe3SxbnWgTFJDKGGwZDDo[YF1KHOqb3PrJJBzd3SnaX7zJGh{eDJ5IHHu[EBJe3B7MB?= NFzCTmkzPDh6NUC4Ni=>
HepG2 NHnwPI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{Lob|czKGh? M1T1UWROW09? MlLtTWM2OD1|NT64OkDDuSB{Lkmg{txO MXeyOFg5PDhyOR?=
HepG2/As M1zSUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\oPHQ4OiCq NXP6XmV6TE2VTx?= MX\JR|UxRTZ6LkGzJOKyKDlwNjFOwG0> MnfxNlQ5QDR6MEm=
SMMC7721 M1rofGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vVbVczKGh? MorjSG1UVw>? MkXOTWM2OD1|MT6yPEDDuSB2LkKg{txO NYnJXHFtOjR6OES4NFk>
SMMC7721/Ac MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTDO|IhcA>? MmS3SG1UVw>? Ml7WTWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? MmfvNlQ5QDR6MEm=
Huh-7 NVXNUWU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWW3NkBp NFrOXG9FVVOR NXzsbYVXUUN3ME2zN{46PiEEsTCzMlkh|ryP Mny3NlQ5QDR6MEm=
Hep3B NYnrOGdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\DbFczKGh? NGjUWmpFVVOR MV\JR|UxRTJyLkG4JOKyKDFwOESg{txO Ml;3NlQ5QDR6MEm=
HepG2 MlXtRZBweHSxc3nzJGF{e2G7 M3HQ[Ylv\HWlZYOgZZBweHSxc3nz MV2yOFg5PDhyOR?=
SMMC7721 M1TL[WFxd3C2b4Ppd{BCe3OjeR?= M1m3U4lv\HWlZYOgZZBweHSxc3nz NHz1SnczPDh6NEiwPS=>
Huh-7 M3jYNmFxd3C2b4Ppd{BCe3OjeR?= MV7pcoR2[2W|IHHwc5B1d3Orcx?= NWPRN|NSOjR6OES4NFk>
Hep3B MXPBdI9xfG:|aYOgRZN{[Xl? MoO4bY5lfWOnczDhdI9xfG:|aYO= NWO2fIxOOjR6OES4NFk>
U2OS  MV7GeY5kfGmxbjDBd5NigQ>? NWL1cGRxOjBizszN M4PuTlI1KGh? MnvjbY5kemWjc3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhSkOOMlGxMEBDS0y[TNMgZY5lSkOOVx?= MkXNNlQ5Pjd{NUm=
AML2 NF7JSlNCeG:ydH;zbZMhSXO|YYm= MlfENk8yOCEQvF2= NIG5S5EzPC92ODDo NXHSOXljcW6mdXPld{BieG:ydH;zbZM> NWjKTVVSOjR4NUm3OFk>
MOML13 MX7BdI9xfG:|aYOgRZN{[Xl? NWTX[WhZOi9zMDFOwG0> NVPwWXRxOjRxNEigbC=> MXjpcoR2[2W|IHHwc5B1d3Orcx?= NVrnfHJxOjR4NUm3OFk>
AML2 NF3pSYpHfW6ldHnvckBCe3OjeR?= NF;yW2EyOM7:TR?= MX2yM|QhcA>? MlixbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MX6yOFY2QTd2OR?=
AML3 M1;XO2Z2dmO2aX;uJGF{e2G7 NYf0bFR7OTEQvF2= NEDJc4szNzRiaB?= NEXRNHZqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MWKyOFY2QTd2OR?=
MOML13 MXfGeY5kfGmxbjDBd5NigQ>? NYPyTZdXOTEQvF2= NWfWb|R3Oi92IHi= NUeyOXhjcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MX[yOFY2QTd2OR?=
BeWo MUPGeY5kfGmxbjDBd5NigQ>? Mk\VN|AhyrWP NGW5dnEzPCCq MX7pcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= MmDWNlQ1QThzNUS=
BeWo NXjTPY1JSXCxcITvd4l{KEG|c3H5 M1jRW|MxKML3TR?= M{nDeFI1KGh? MoTZbY5kemWjc3XzJIFxd3C2b4Ppdy=> NH\qS3kzPDR7OEG1OC=>
OCI MlraSpVv[3Srb36gRZN{[Xl? MV:xNEDPxE1? MYWyOEBp NETjWHl2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MV[yOFQ4OzV4Mh?=
MOLM NHnYUm5HfW6ldHnvckBCe3OjeR?= MVmxNEDPxE1? MoTwNlQhcA>? MV\1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? NFnuXmgzPDR5M{W2Ni=>
U2OS  NGX0VZJHfW6ldHnvckBCe3OjeR?= M1vYWlIxKM7:TR?= MVKyOEBp MYfpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MYWyOFM3PjByNx?=
RKO NGP2NWNHfW6ldHnvckBCe3OjeR?= NGDmZYszOCEQvF2= NVHYd2JoOjRiaB?= NIXDVYxqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw Mk\JNlQ{PjZyMEe=
U2OS  NE\aS|ZHfW6ldHnvckBCe3OjeR?= M1izSlIxKM7:TR?= NFLYXmIzPCCq NXe1bG5PcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> M3zG[VI1OzZ4MEC3
RKO MXvGeY5kfGmxbjDBd5NigQ>? MX6yNEDPxE1? NF3MVmwzPCCq MUnpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= M3rjRVI1OzZ4MEC3
SMMC-7721  MkLkR4VtdCCYaXHibYxqfHliQYPzZZk> MYWxMlI2NTJyIN88US=> M3TGUlI1NzR6L{eyJIg> NHq5RWRFVVOR M4nKSYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NIDOOokzPDJ6NkOxNi=>
HuH-7 MnTMR4VtdCCYaXHibYxqfHliQYPzZZk> NXXZcFlUOS5{NT2yNEDPxE1? MnjBNlQwPDhxN{KgbC=> MWjEUXNQ MnzubY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= M2TafFI1Ojh4M{Gy
SMMC-7721  M2DRfWFxd3C2b4Ppd{BCe3OjeR?= MUKyNEDPxE1? MmP1OFghcA>? MnPkSG1UVw>? NVHkT|R{cW6mdXPld{BieG:ydH;zbZM> MkT6NlQzQDZ|MUK=
HuH-7 M2T4bmFxd3C2b4Ppd{BCe3OjeR?= M4r0SlIxKM7:TR?= MUi0PEBp NYPYXVROTE2VTx?= M2jQSIlv\HWlZYOgZZBweHSxc3nz M{nWd|I1Ojh4M{Gy
SMMC-7721  M37LcmZ2dmO2aX;uJGF{e2G7 NEfEToMyOCEQvF2= MWSzOkBp MV7EUXNQ MUnkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> MWOyOFI5PjNzMh?=
HuH-7 MXzGeY5kfGmxbjDBd5NigQ>? NV;6OoM6OTBizszN NXXFN2JuOzZiaB?= Mlm4SG1UVw>? MX;kc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> MUiyOFI5PjNzMh?=
AT2 NGjMVXlHfW6ldHnvckBCe3OjeR?= NH\HXlY2NzFyIN88US=> NWXWVlg{dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= MnrDNlQzPDB{MEO=
REH M1HXb2Z2dmO2aX;uJGF{e2G7 NHnIbZY2NzFyIN88US=> NXj2bIxidGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= M1fGbFI1OjRyMkCz
UoCB6 NX;jU25iTnWwY4Tpc44hSXO|YYm= NILHNmQ2NzFyIN88US=> M3n6eYxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li NITHU4EzPDJ2MEKwNy=>
AT2 Mnf3R4VtdCCYaXHibYxqfHliQYPzZZk> Mk[1NE0zPSEQvF2= MkHDbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NYqxVZM6OjR{NECyNFM>
REH M3uyeGNmdGxiVnnhZoltcXS7IFHzd4F6 NWD6VVgxOC1{NTFOwG0> MnXYbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? M13JSVI1OjRyMkCz
UoCB6 NXHVfVVmS2WubDDWbYFjcWyrdImgRZN{[Xl? NWXDWIFzOC1{NTFOwG0> M4TpTYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? NHG2SGIzPDJ2MEKwNy=>
A2780 NUO3eVRETnWwY4Tpc44hSXO|YYm= M4LlN|UwOTBxMkCg{txO MWGyOEBp M{\S[JVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NH65fGczPDF|NkG0Oy=>
H460 MlWwSpVv[3Srb36gRZN{[Xl? MVi1M|ExNzJyIN88US=> MXeyOEBp NF20V5J2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= Mlm5NlQyOzZzNEe=
Lovo  MmfRSpVv[3Srb36gRZN{[Xl? NEnvb402NzFyL{KwJO69VQ>? Mn7aNlQhcA>? MkDoeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MkDhNlQyOzZzNEe=
A2780 M{fQOWFxd3C2b4Ppd{BCe3OjeR?= M2KzbFUwOTBxMkCg{txO M3;iclI1KGh? M1HJcoVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN NVmzc2tCOjRzM{[xOFc>
H460 MWPBdI9xfG:|aYOgRZN{[Xl? MYO1M|ExNzJyIN88US=> MoC1NlQhcA>? NGjuS5BmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? MXKyOFE{PjF2Nx?=
Lovo  NVvpZ|RsSXCxcITvd4l{KEG|c3H5 NIPud2g2NzFyL{KwJO69VQ>? Mlu0NlQhcA>? M2DsRYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN NELjUZAzPDF|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
  • 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