Nutlin-3

For research use only. Not for use in humans.

製品コードS1061

Nutlin-3化学構造

分子量(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.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 32700 あり
JPY 20200 あり
JPY 30200 あり
JPY 63400 あり
JPY 163000 あり
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バルク問合せ

文献中Selleckの製品使用例(36)

製品安全説明書

Mdm2阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
Mdm2 [5]
(Cell-free assay)
180 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 NEP1cm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfEN4NqPcLizszN M3vLb|Q5yqCq M2rPNIJtd2OtczCyO{1QUENvaX7keYNm\CClZXzsJJBzd2yrZnXyZZRqd25iY3;tdIFz[WKuZTD0c{B1cGG2IH;mJIJie2GuIHzleoVtew>? NI\UT5UzPjN3MEW2OS=>
NP69 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNzLk[5xtEzNjV2IN88US=> NIfKcYozPjJ3MkW3OS=>
NP460 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLpcFJLUUN3ME2yNk45PcLzMT6xPEDPxE1? MljvNlYzPTJ3N{W=
C666-1 M3HHUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTF7Lkm1xtE5Njl|IN88US=> NF\GWZIzPjJ3MkW3OS=>
C666-1 NYLmXlYyS2WubDDWbYFjcWyrdImgRZN{[Xl? MUixNEDDvU1? NWT3U|FyPDhiaB?= MWfEUXNQ MlvLd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:geIhmKGO7dH;0c5hq[yCnZn\lZ5Qhd2ZiY3nzdIxifGmw Mmq4NlYzPTJ3N{W=
C666-1  NEDrd25HfW6ldHnvckBCe3OjeR?= NXnnenl7OTBiwsXN MlvFNlQhcA>? NFrYeZVFVVOR MmSxZYN1cX[jdHXzJJRp\SCyNUOgdIF1cHejeTygeZBz\We3bHH0bY5oKHB3MzygdFIyKGGwZDDN[I0z NIr6[WwzPjJ3MkW3OS=>
C666-1 MYHBdI9xfG:|aYOgRZN{[Xl? MkOwNVAhyrWP NXz0SWZpPDhxN{KgbC=> MWrEUXNQ MmnNd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:gZ4l{eGyjdHnuMYlv\HWlZXSgZZBweHSxc3nz Mo\SNlYzPTJ3N{W=
A549 NIroSGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHNNlQhcA>? MlG3TWM2OD1zNz62PEDDuSB2LkWyJO69VQ>? MXSyOlEzPTJ|MB?=
A549-NTC M2jBfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLk[lBrOjRiaB?= MWrJR|UxRTF7LkSyJOKyKDFwOU[g{txO NY\3UYk3OjZzMkWyN|A>
A549-920 M2m3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULLR2VlOjRiaB?= NWLzXGRXUUN3ME2zN{45PSEEsTC0Mlg1KM7:TR?= NFuyb5YzPjF{NUKzNC=>
CRL-5908 MmmzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\Ze|I1KGh? MnrFTWM2OD1|OD63NUDDuSB{LkSzJO69VQ>? MYiyOlEzPTJ|MB?=
L6 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jFUVExyqEQvF5CpC=> M1HYd|I1NzR6L{eyJIg> M1jac2ROW09? MVnpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> M3nKZ|I2QDdzN{m0
C2C12 NX\PdFN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH3SlQyOMLizszNxsA> MV2yOE81QC95MjDo M3LUO2ROW09? MYXpcohq[mm2czDj[YxteyCycn;sbYZmemG2aX;uJIFv\CCmaX\m[ZJmdnSrYYTpc44> MmPaNlU5PzF5OUS=
MCF-7  M3:wb2Z2dmO2aX;uJGF{e2G7 NYXHe45yOTEEoN88US=> M{nqRmROW09? M4r4colvcGmkaYTzJIN6[2yrbjDENUBidmRiRHnj[ZLDqA>? NVPDdoFQOjV5MEK3NFM>
DU4475  NV;E[G42TnWwY4Tpc44hSXO|YYm= M2jqZVUwOTBxMkCg{txO MlfpNlTDqGh? NWSxRWxy\G:5boLl[5Vt[XSnczDUc4NiNTFiZH;z[UBl\XCnbnTlcpRtgQ>? MmrVNlU2PDdzN{S=
SMMC-7721 NUPwbWZiTnWwY4Tpc44hSXO|YYm= MnW4NVAh|ryP MWG0PEBp MorVSG1UVw>? MYfjZZV{\XNiRF7BJGRUSiCmYX3h[4U> MojVNlU2PDR|NkG=
SMMC-7721 M3fFVGZ2dmO2aX;uJGF{e2G7 NX;ROow4OTBizszN MlXNOFghcA>? M2\mfWROW09? NYjuT3NVcW6mdXPld{B1cGViY3jyc41ifGmwLXLveY5lKHC{b4TlbY4hUU[LMU[geI8heGG{dHnhcIx6KGyxY3HsbZpmKGmwIITo[UBkgXSxcHzhd43DqA>? MYeyOVU1PDN4MR?=
SMMC-7721 MY\GeY5kfGmxbjDBd5NigQ>? MV2xNEDPxE1? MnzHOFghcA>? NXzHfJBHTE2VTx?= NUf4NVlUcW6lcnXhd4V{KHSqZTDlfJBz\XO|aX;uJIxmfmWuIH;mxsBKTk6EMdMgcXJPSQ>? NXe2RoNEOjV3NESzOlE>
SMMC-7721 NX35W|RnTnWwY4Tpc44hSXO|YYm= NWXzUXpQOTBizszN MV:zOkBp MYPEUXNQ MmezZ4F2e2W|IITo[UBm[3SxcHnjJIV5eHKnc4Ppc44hd2ZiSV\JNVY> NHvINI0zPTV2NEO2NS=>
MCF-7 M4nH[2Z2dmO2aX;uJGF{e2G7 M1PidlExyqEQvF2= NXrXb|VUOC1{NDDo MV\pcoR2[2W|IIC1N{BidmRicEKxM2NqeDF? M1[3TlI2PDh{M{ez
OVCAR10 MlrNSpVv[3Srb36gRZN{[Xl? NVPlPHE4OTEEoN88US=> MkXSNlFpyqB? M{XON2ROW09? NVLWc|d[cW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? NFTGTmEzPTR{NkW0PC=>
NCI-H23 NFjUdlBHfW6ldHnvckBCe3OjeR?= MoLYNVDDqM7:TR?= M3PYelIycMLi NYHZfohOTE2VTx?= NHzSU5dqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ NVrTOGFDOjV2Mk[1OFg>
A2780 MoHqSpVv[3Srb36gRZN{[Xl? M1XFe|ExyqEQvF2= MWiyNYjDqA>? NXLEWXRZTE2VTx?= MkjlbY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> M1n2TlI2PDJ4NUS4
NCI-H23 Mn;lSpVv[3Srb36gRZN{[Xl? NF7v[5UyOMLizszN MlvGNlFpyqB? MVHEUXNQ NIXmZ2pl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> MUCyOVQzPjV2OB?=
A2780 NIrsUZdHfW6ldHnvckBCe3OjeR?= MX[xNOKh|ryP MlW1NlFpyqB? M3j4U2ROW09? NUDpcot{\GWlcnXhd4V{KHSqZTDGc5hOOSCuZY\lcJM> NF20UnYzPTR{NkW0PC=>
HCT116  NEHmTZJHfW6ldHnvckBCe3OjeR?= MoXhNVAhyrWP Ml\UNlQhcA>? Mn3wZ4F2e2W|IHGgdFU{NWSncHXu[IVvfCC2ZYTyZZBtd2mmIFexMYFzemW|dDDpckBlcXCub3nkJGhEXDFzNjDjcI9v\XNiREOgZY5lKER6 MWmyOVM5ODB3NR?=
MCF-10CA1a M2T2d2Z2dmO2aX;uJGF{e2G7 NY\rPJlSOTEEoN88US=> NHK3To01QCCq M4jqcWROW09? Mn;VbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? NXT5b4g6OjV{NUe3Nlk>
MCF-10A1  NFrSR2ZHfW6ldHnvckBCe3OjeR?= M2DCeVExyqEQvF2= NWfkNZd5OjRxNEigbC=> MUHEUXNQ MVrpcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> MlHxNlUzPTd5Mkm=
MCF-10CA1a M3LNe2Z2dmO2aX;uJGF{e2G7 M1fYOlExyqEQvF2= M2jHPFI1KGh? NWr2eXh[TE2VTx?= NYH5Z2d2\GWlcnXhd4V{KHSqZTDUS2Yu|rJ|LXnu[JVk\WRibWLORUBt\X[nbIOgc4ZOVVB{LNMgUW1RQSxiYX7kxsBqdnSnZ4LpcuKh|rMEoEO= NGD3T4szPTJ3N{eyPS=>
MCF-10CA1a NYDyW5NLTnWwY4Tpc44hSXO|YYm= NFuzXmYyOMLizszN MX6yOEBp MYDEUXNQ NXH5NGR6cW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MX2yOVI2Pzd{OR?=
SK-BR-7 Ml;VSpVv[3Srb36gRZN{[Xl? NVjUV|J5OTEEoN88US=> MXuyOEBp NHvTbWdFVVOR M3vlOolvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= M1\PfVI2OjV5N{K5
SUM102PT MWrGeY5kfGmxbjDBd5NigQ>? MXyxNOKh|ryP Mn:zNlQhcA>? MoHESG1UVw>? MWXpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NIXkXJkzPTJ3N{eyPS=>
RAW 264.7 NXfWcHpUTnWwY4Tpc44hSXO|YYm= MVixNOKh|ryP MXqzNEBucW5? MUjwdoV3\W62czD0bIUheDV|IILl[JVkfGmxbjDpckBz\XOyb37z[UB1dyCOUGO= NHvnepgzPTF5MkW0Oy=>
RAW 264.7 NWLS[XVTTnWwY4Tpc44hSXO|YYm= Moj3NVDDqM7:TR?= MVmzNEBucW5? M4Thb5Jm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= MkjzNlUyPzJ3NEe=
RAW 264.7 MWfGeY5kfGmxbjDBd5NigQ>? MYWxNOKh|ryP M{PFclMxKG2rbh?= NVnQNYhEcW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MlrONlUyPzJ3NEe=
MCF7  MWLD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NFLBNlUzNjViwsXN NHjCSIM2KGR? M3TlXGROW09? NHLtcW5{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u M{TUUVI2ODh3OUCy
MCF7  NFLlSlVHfW6ldHnvckBCe3OjeR?= MYGyMlUhyrWP MlHuOFghcA>? NGXwcphFVVOR MXnk[YNz\WG|ZYOgeIhmKGixbX;sc4dwfXNiRGPCJJJmeGGrcjDmdoVyfWWwY3nldy=> MlHMNlUxQDV7MEK=
ACHN NGHuOVhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYOwMlUuOTBizszN NVfyc3VUOC14IHS= MXrEUXNQ NUfBUZdGcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4PHbFI2ODZ5N{i3
Caki-2 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NX21bWp4OC53LUGwJO69VQ>? MmjqNE03KGR? NEHjZpJFVVOR Ml\tbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M2foNFI2ODZ5N{i3
A498 NFLWfolE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NXnubohXOC53LUGwJO69VQ>? M3G3PVAuPiCm NGW4b25FVVOR NVyxUlI{cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MnXoNlUxPjd5OEe=
115 NGXOSnpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M2XPNlAvPS1zMDFOwG0> NEnPTW4xNTZiZB?= NET5dINFVVOR NVf0V3ZTcW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NHXZdVUzPTB4N{e4Oy=>
117 MkW4R4VtdCCYaXHibYxqfHliQYPzZZk> Mn;tNE42NTFyIN88US=> NU\DN|F1OC14IHS= NVG1PXZmTE2VTx?= MoPzbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NH65[FEzPTB4N{e4Oy=>
ACHN MkC5SpVv[3Srb36gRZN{[Xl? NEP4OmcxNjVxMT:1JO69VQ>? MoDuOFghcA>? NEjxbnhFVVOR NXjpeGRydGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NVHMS2hJOjVyNke3PFc>
Caki-2 M1z6S2Z2dmO2aX;uJGF{e2G7 M{f4[FAvPS9zL{Wg{txO M2jxdlQ5KGh? NFnwT5BFVVOR MYjs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? M1e4PVI2ODZ5N{i3
A498 M4fN[mZ2dmO2aX;uJGF{e2G7 NULFVldIOC53L{GvOUDPxE1? NUPtSHQ2PDhiaB?= MWjEUXNQ NYO1eZNVdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NWTIXFY1OjVyNke3PFc>
115 NHuycmRHfW6ldHnvckBCe3OjeR?= MVWwMlUwOS93IN88US=> M3r1T|Q5KGh? NFHzeI5FVVOR NWjrTI1rdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= M2rJU|I2ODZ5N{i3
ACHN M4jwWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jOPFUh|ryP MWe0PEBp MmWwSG1UVw>? M1zGfIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NUDzepl2OjVyNke3PFc>
Caki-2 MonKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLxe|I2KM7:TR?= MmXZOFghcA>? NHvMdnZFVVOR MUTpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NHvucGQzPTB4N{e4Oy=>
A498 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfjfWhIPSEQvF2= MWm0PEBp NV;lfo9UTE2VTx?= M2C2TYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MXWyOVA3Pzd6Nx?=
115 NUDRTG5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PDV|Uh|ryP MWC0PEBp NUXlR41{TE2VTx?= MYHpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= MkXFNlUxPjd5OEe=
ACHN NET6V21HfW6ldHnvckBCe3OjeR?= NVrYeoRYPSEQvF2= NYP6W|NUPDhiaB?= NXTQcFV2TE2VTx?= MlXnbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M3Ha[FI2ODZ5N{i3
Caki-2 NWnxSYNoTnWwY4Tpc44hSXO|YYm= M1vye|Uh|ryP MXK0PEBp MUDEUXNQ MXnpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M{TKXVI2ODZ5N{i3
A498 MnzCSpVv[3Srb36gRZN{[Xl? NYjVdpZRPSEQvF2= NUfiXlM3PDhiaB?= MkfoSG1UVw>? NWLvO5JlcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M{nRZVI2ODZ5N{i3
115 NFzjc29HfW6ldHnvckBCe3OjeR?= M{HzWlUh|ryP NFTqO3Q1QCCq MoPCSG1UVw>? MkfObY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NXi4UZg4OjVyNke3PFc>
MOLM-13 MVzGeY5kfGmxbjDBd5NigQ>? Mn\lOuKh|ryP NH7vWIQxNThiaB?= MoXkSG1UVw>? M1nGZolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? NXHhRWVkOjR6OEWwPFI>
MOLM-13 NXzKVXRWTnWwY4Tpc44hSXO|YYm= MUW2xsDPxE1? MmXoOkBp NIOzNmJFVVOR NI\3eIRmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw M2LYPVI1QDh3MEiy
HepG2 M2n4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2q3fVczKGh? NY\scHZZTE2VTx?= MUDJR|UxRTN3Lki2JOKyKDJwOTFOwG0> MUOyOFg5PDhyOR?=
HepG2/As MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnuV5Y5PzJiaB?= MnvHSG1UVw>? NWXtXY83UUN3ME22PE4yOyEEsTC5MlYh|ryP MmXKNlQ5QDR6MEm=
SMMC7721 NV24VFRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHDVZlIPzJiaB?= Mo\rSG1UVw>? MkHBTWM2OD1|MT6yPEDDuSB2LkKg{txO NUfxSVFnOjR6OES4NFk>
SMMC7721/Ac MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlOxO|IhcA>? Ml\WSG1UVw>? MUfJR|UxRTV3LkKxJOKyKDVwMEOg{txO Mkn6NlQ5QDR6MEm=
Huh-7 M1e2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPp[YV1PzJiaB?= MoXpSG1UVw>? NH3HV3VKSzVyPUOzMlk3KMLzIEOuPUDPxE1? NFrMNlUzPDh6NEiwPS=>
Hep3B MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjBN4k4OiCq MVrEUXNQ M3r1NGlEPTB;MkCuNVghyrFiMT64OEDPxE1? NXvobpI6OjR6OES4NFk>
HepG2 M2WybmFxd3C2b4Ppd{BCe3OjeR?= MWTpcoR2[2W|IHHwc5B1d3Orcx?= MnPQNlQ5QDR6MEm=
SMMC7721 MUXBdI9xfG:|aYOgRZN{[Xl? NXLwVXZbcW6mdXPld{BieG:ydH;zbZM> M1;qdlI1QDh2OEC5
Huh-7 MmDlRZBweHSxc3nzJGF{e2G7 MknrbY5lfWOnczDhdI9xfG:|aYO= MYOyOFg5PDhyOR?=
Hep3B M4\lNmFxd3C2b4Ppd{BCe3OjeR?= NHG5WIxqdmS3Y3XzJIFxd3C2b4Ppdy=> NHnkfnAzPDh6NEiwPS=>
U2OS  M{S5bmZ2dmO2aX;uJGF{e2G7 NGXie5kzOCEQvF2= NY\rUm5wOjRiaB?= MkLVbY5kemWjc3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhSkOOMlGxMEBDS0y[TNMgZY5lSkOOVx?= NVOz[JNyOjR6NkeyOVk>
AML2 M1W5OWFxd3C2b4Ppd{BCe3OjeR?= NXzjNVhPOi9zMDFOwG0> MWmyOE81QCCq M4LFb4lv\HWlZYOgZZBweHSxc3nz Mn\ONlQ3PTl5NEm=
MOML13 NFf2Z41CeG:ydH;zbZMhSXO|YYm= MnPRNk8yOCEQvF2= NITNWWYzPC92ODDo NWDycIxPcW6mdXPld{BieG:ydH;zbZM> MXiyOFY2QTd2OR?=
AML2 M2XSWmZ2dmO2aX;uJGF{e2G7 M{f5eVEx|ryP MVuyM|QhcA>? NV[4RWlpcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MXmyOFY2QTd2OR?=
AML3 M3HScGZ2dmO2aX;uJGF{e2G7 MlvaNVDPxE1? MoD5Nk81KGh? NUHYU4tqcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MVuyOFY2QTd2OR?=
MOML13 MUTGeY5kfGmxbjDBd5NigQ>? NVPESpBiOTEQvF2= NV75[YZtOi92IHi= M4jub4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NYDnPZdNOjR4NUm3OFk>
BeWo NGjDZopHfW6ldHnvckBCe3OjeR?= MnXPN|AhyrWP M37kNFI1KGh? MVzpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= NGfvS|kzPDR7OEG1OC=>
BeWo NXvSOIZmSXCxcITvd4l{KEG|c3H5 MmLEN|AhyrWP NGDYdIMzPCCq MlTFbY5kemWjc3XzJIFxd3C2b4Ppdy=> NYHscIdXOjR2OUixOVQ>
OCI NY\FeHdSTnWwY4Tpc44hSXO|YYm= MoPJNVAh|ryP MUeyOEBp MnjleZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w MmrGNlQ1PzN3NkK=
MOLM NEm0S2hHfW6ldHnvckBCe3OjeR?= M3T2b|ExKM7:TR?= Mk\GNlQhcA>? M1LiS5VxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= M1fIclI1PDd|NU[y
U2OS  M4LmSWZ2dmO2aX;uJGF{e2G7 NFLWTGQzOCEQvF2= NFLofJgzPCCq Mm\xbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? Mny2NlQ{PjZyMEe=
RKO Mk\GSpVv[3Srb36gRZN{[Xl? NHXESGMzOCEQvF2= M2r5dlI1KGh? NIW4[phqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NVTrS2RsOjR|Nk[wNFc>
U2OS  M{fzS2Z2dmO2aX;uJGF{e2G7 MX2yNEDPxE1? NXnl[3IzOjRiaB?= MVvpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= MnzsNlQ{PjZyMEe=
RKO MoWxSpVv[3Srb36gRZN{[Xl? M13WXVIxKM7:TR?= Ml;JNlQhcA>? MWjpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= NWXDephJOjR|Nk[wNFc>
SMMC-7721  NWP0d5ExS2WubDDWbYFjcWyrdImgRZN{[Xl? Mmr2NU4zPS1{MDFOwG0> MUiyOE81QC95MjDo MkXjSG1UVw>? M4LWfYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MUmyOFI5PjNzMh?=
HuH-7 MmL1R4VtdCCYaXHibYxqfHliQYPzZZk> Mn\qNU4zPS1{MDFOwG0> M3fKUlI1NzR6L{eyJIg> M2m2RmROW09? NH;hPZRqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MVeyOFI5PjNzMh?=
SMMC-7721  MWPBdI9xfG:|aYOgRZN{[Xl? NHe2dIQzOCEQvF2= M1HjWlQ5KGh? NFThTXVFVVOR M3nNeYlv\HWlZYOgZZBweHSxc3nz NWXPeYdEOjR{OE[zNVI>
HuH-7 NEfMPZpCeG:ydH;zbZMhSXO|YYm= M1TQOFIxKM7:TR?= MYC0PEBp NVXBPGc3TE2VTx?= M{HWSolv\HWlZYOgZZBweHSxc3nz MlzwNlQzQDZ|MUK=
SMMC-7721  Mm\CSpVv[3Srb36gRZN{[Xl? M3TleFExKM7:TR?= M3;UN|M3KGh? M2TEWWROW09? MkfK[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> M2jHOVI1Ojh4M{Gy
HuH-7 MoS0SpVv[3Srb36gRZN{[Xl? MXmxNEDPxE1? NX3ONW03OzZiaB?= MYnEUXNQ M1\jWoRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ MYCyOFI5PjNzMh?=
AT2 NVLpSItbTnWwY4Tpc44hSXO|YYm= MlHQOU8yOCEQvF2= M4f1doxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MVuyOFI1ODJyMx?=
REH NVrtcnZZTnWwY4Tpc44hSXO|YYm= NILXRnI2NzFyIN88US=> NHXEbHdt\WGmczD0c{BiKHO3YoP0ZY51cWGuIHHjZ5VufWyjdHnvckBw\iC2aHWgdFU{KHC{b4TlbY4h[XNid3XscEBieyC2aHWg[ZhxemW|c3nvckBw\iCrdIOg[Ilz\WO2IIThdodmfHNicEKxMEBOTE1{IHHu[EB1cGVicILvMYFxd3C2b4TpZ{BDSVhiYX7kJHBWVUFicILveIVqdnQEoB?= MU[yOFI1ODJyMx?=
UoCB6 M{jMXGZ2dmO2aX;uJGF{e2G7 Ml7EOU8yOCEQvF2= MXns[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? M{L5TVI1OjRyMkCz
AT2 NWH1eo96S2WubDDWbYFjcWyrdImgRZN{[Xl? MoLTNE0zPSEQvF2= NHnPOYZqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MUSyOFI1ODJyMx?=
REH M3roT2NmdGxiVnnhZoltcXS7IFHzd4F6 M3fueFAuOjVizszN NGfjdFVqdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 NU\tZWJvOjR{NECyNFM>
UoCB6 MX;D[YxtKF[rYXLpcIl1gSCDc4PhfS=> MUiwMVI2KM7:TR?= M{T4PYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MljxNlQzPDB{MEO=
A2780 NF7YelRHfW6ldHnvckBCe3OjeR?= M2WzflUwOTBxMkCg{txO NWHUVXZ{OjRiaB?= M2nkRpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi NGfYNZUzPDF|NkG0Oy=>
H460 NFfifoNHfW6ldHnvckBCe3OjeR?= MVW1M|ExNzJyIN88US=> MUWyOEBp NYX2cppKfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NWH3eHR[OjRzM{[xOFc>
Lovo  NH\Oe5FHfW6ldHnvckBCe3OjeR?= MXG1M|ExNzJyIN88US=> NFzlfJkzPCCq NUPWZmx2fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NH7yOlczPDF|NkG0Oy=>
A2780 NUn5UIpqSXCxcITvd4l{KEG|c3H5 MoDNOU8yOC9{MDFOwG0> M{P4dFI1KGh? MYLlcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MUeyOFE{PjF2Nx?=
H460 NYi4UmVRSXCxcITvd4l{KEG|c3H5 NUG3cZZwPS9zMD:yNEDPxE1? MYeyOEBp MW\lcohidmOnczDhdI9xfG:|aYOgbY5lfWO2aX;uJIJ6KER{NknIM2UyQTWUIH;2[ZIhemiWUlHJUC=> MoO2NlQyOzZzNEe=
Lovo  NY[4N2E4SXCxcITvd4l{KEG|c3H5 NEnlN|E2NzFyL{KwJO69VQ>? MoW1NlQhcA>? NGLiSFFmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? M{PPWFI1OTN4MUS3

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アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

- 合併

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
細胞試験:

[1]

- 合併
  • 細胞株: HCT116, RKO, SJSA-1, SW480, and MDA-MB-435
  • 濃度: Dissolved in DMSO, final concentrations ~ 30 μM
  • 反応時間: 8, 24, and 48 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
  • 投薬量: 200 mg/kg
  • 投与方法: Orally, twice a day
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 100 mg/mL (171.96 mM)
Ethanol 30 mg/mL (51.59 mM)
Water Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 581.5
化学式

C30H30Cl2N4O4

CAS No. 890090-75-2
Storage powder
in solvent
別名 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

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    Is this a racemic mixture of Nutlin-3a and Nutlin-3b or just the Nutlin-3a enantiomer?

  • 回答:

    It is a racemate.

Mdm2シグナル伝達経路

相関Mdm2製品

Tags: Nutlin-3を買う | Nutlin-3 ic50 | Nutlin-3供給者 | Nutlin-3を購入する | Nutlin-3費用 | Nutlin-3生産者 | オーダーNutlin-3 | Nutlin-3化学構造 | Nutlin-3分子量 | Nutlin-3代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID