Nutlin-3

For research use only. Not for use in humans.

製品コードS1061

Nutlin-3化学構造

CAS No. 890090-75-2

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)  
10mM (1mL in DMSO) JPY 32700
JPY 20200
JPY 30200
JPY 63400
JPY 163000
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バルク問合せ

文献中Selleckの製品使用例(80)

製品安全説明書

MDM2/MDMX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
SMMC-7721  M3;NXmZ2dmO2aX;uJGF{e2G7 MnrZNVAh|ryP M13p[lM3KGh? M1f5W2ROW09? NWHqVopC\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NYXNUJlKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 NVPm[lBVSXCxcITvd4l{KEG|c3H5 NXK4Wm5xOjBizszN MnfxOFghcA>? MUDEUXNQ MVLpcoR2[2W|IHHwc5B1d3Orcx?= NF\XU3M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
SMMC-7721  MoHIRZBweHSxc3nzJGF{e2G7 NXTDdGx[OjBizszN MYi0PEBp NGrlPVBFVVOR NGLJdXJqdmS3Y3XzJIFxd3C2b4Ppdy=> MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 M4DxZWNmdGxiVnnhZoltcXS7IFHzd4F6 NIPRUIcyNjJ3LUKwJO69VQ>? M17XSFI1NzR6L{eyJIg> NUTjUXd1TE2VTx?= M{fSWYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 NUjmVJNxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
SMMC-7721  NVrnW|ljS2WubDDWbYFjcWyrdImgRZN{[Xl? MkHwNU4zPS1{MDFOwG0> Mkn1NlQwPDhxN{KgbC=> MoPCSG1UVw>? NHXKOXdqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M2PUelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
RKO M3LXW2Z2dmO2aX;uJGF{e2G7 M3ywTFIxKM7:TR?= NUjye|hZOjRiaB?= NVfyZWNscW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NkCwO{c,OjR|Nk[wNFc9N2F-
U2OS  NWjkTWJmTnWwY4Tpc44hSXO|YYm= MmjkNlAh|ryP MXiyOEBp M{fZ[Ilv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NG\PUFE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
RKO M1WwNWZ2dmO2aX;uJGF{e2G7 MWCyNEDPxE1? NXPDUmhyOjRiaB?= MWTpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MoTFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
U2OS  MoHXSpVv[3Srb36gRZN{[Xl? NH3ORmEzOCEQvF2= MXqyOEBp M3m3dIlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN4NkCwO{c,OjR|Nk[wNFc9N2F-
MOLM NY\aRnNuTnWwY4Tpc44hSXO|YYm= NYjKVmtjOTBizszN NV;4SXhwOjRiaB?= NYrKU41WfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u MlXHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
OCI NELYVHVHfW6ldHnvckBCe3OjeR?= M37XUlExKM7:TR?= M33YXlI1KGh? MlLmeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5M{W2Nkc,OjR2N{O1OlI9N2F-
BeWo MkSxRZBweHSxc3nzJGF{e2G7 NHGwb4Y{OCEEtV2= NHK0WY4zPCCq MXXpcoNz\WG|ZYOgZZBweHSxc3nz NWXBeo9HRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVgyPTRpPkK0OFk5OTV2PD;hQi=>
BeWo NHLrUYJHfW6ldHnvckBCe3OjeR?= NFKyToU{OCEEtV2= MkC4NlQhcA>? M1X3T4lv[3KnYYPld{BxPTNuIF3kcVItKHB{MTDhcoQhWHWvYTDheEB1cGVicILveIVqdiCuZY\lcC=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7OEG1OEc,OjR2OUixOVQ9N2F-
MOML13 NVOwPFBUTnWwY4Tpc44hSXO|YYm= MnzqNVDPxE1? NGn5dVQzNzRiaB?= M2n2ZYlv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NFLxd4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML3 MVjGeY5kfGmxbjDBd5NigQ>? MYOxNO69VQ>? MVKyM|QhcA>? NE\FN2ZqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NYrUc3dmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML2 M2i2TWZ2dmO2aX;uJGF{e2G7 MV[xNO69VQ>? MkLINk81KGh? NF7uOWJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MoezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
MOML13 MU\BdI9xfG:|aYOgRZN{[Xl? MonzNk8yOCEQvF2= NYT6bIhiOjRxNEigbC=> NICzNpZqdmS3Y3XzJIFxd3C2b4Ppdy=> MljnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
AML2 MYjBdI9xfG:|aYOgRZN{[Xl? Mkj2Nk8yOCEQvF2= NYSzenlnOjRxNEigbC=> NV;O[HJkcW6mdXPld{BieG:ydH;zbZM> NX7iRWs{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
U2OS  MVrGeY5kfGmxbjDBd5NigQ>? NYXNOFdoOjBizszN NUS5NZhGOjRiaB?= M3XLdYlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K1PUc,OjR6NkeyOVk9N2F-
Hep3B M{HhWWFxd3C2b4Ppd{BCe3OjeR?= NIDQNXRqdmS3Y3XzJIFxd3C2b4Ppdy=> M3rlOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
Huh-7 MnHSRZBweHSxc3nzJGF{e2G7 M{e2Z4lv\HWlZYOgZZBweHSxc3nz MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721 NFnYcpRCeG:ydH;zbZMhSXO|YYm= NYDJSGh6cW6mdXPld{BieG:ydH;zbZM> M2rPOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2 MmfaRZBweHSxc3nzJGF{e2G7 NIe4cFFqdmS3Y3XzJIFxd3C2b4Ppdy=> NVn4SWJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
Hep3B NU\UXYszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrIO|IhcA>? MX;EUXNQ Mm\YTWM2OD1{MD6xPEDDuSBzLki0JO69VQ>? NIP0dWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
Huh-7 NI\2eGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[zO|IhcA>? MlLzSG1UVw>? NGDHeGZKSzVyPUOzMlk3KMLzIEOuPUDPxE1? NHrETYI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
SMMC7721/Ac NHnTTG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:2O|IhcA>? MXzEUXNQ NEjoSGNKSzVyPUW1MlIyKMLzIEWuNFMh|ryP NFT6c|U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
SMMC7721 NWj2bGlnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYroW5BUPzJiaB?= M{fNS2ROW09? NIj3ZoFKSzVyPUOxMlI5KMLzIESuNkDPxE1? M3LzXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2/As NYrk[WNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWe3NkBp NYjDOINMTE2VTx?= MYPJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> M2X0PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2 NEjuVJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HwWlczKGh? NFfEZYdFVVOR NV:3NZZUUUN3ME2zOU45PiEEsTCyMlkh|ryP NXPlTGlCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
MOLM-13 Mn\KSpVv[3Srb36gRZN{[Xl? M4DDWFbDqM7:TR?= MnjnOkBp NGjkRpRFVVOR MYHlcohidmOnczD0bIUh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINmIh[W6mIHjlZZQhe2ixY3ugdJJwfGWrboOgTJNxOjdiYX7kJGh{eDly MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NUC4Nkc,OjR6OEWwPFI9N2F-
MOLM-13 MmDhSpVv[3Srb36gRZN{[Xl? MlzWOuKh|ryP MUewMVghcA>? MXvEUXNQ MVLpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> MknsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEWwPFIoRjJ2OEi1NFgzRC:jPh?=
115 M4m2eGZ2dmO2aX;uJGF{e2G7 M3XFeVUh|ryP MkDsOFghcA>? M4\SXmROW09? NXr0U4l4cW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> NGLVXZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
A498 NUXVVZc1TnWwY4Tpc44hSXO|YYm= M1;YR|Uh|ryP NV\DeotuPDhiaB?= MkXwSG1UVw>? NHq5PXhqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MlrOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 M1;2dGZ2dmO2aX;uJGF{e2G7 MmDQOUDPxE1? NFjRWIk1QCCq M{HMemROW09? M2PQ[4lv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= M2jnPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
ACHN MmTpSpVv[3Srb36gRZN{[Xl? NEDETFU2KM7:TR?= Mn3GOFghcA>? MVXEUXNQ MWHpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MoHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 M{LleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDIOJI2KM7:TR?= NVu3cotbPDhiaB?= NGDXO5dFVVOR MXfpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= M3fpdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 MkH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVfsTWtXPSEQvF2= NX\YfpVXPDhiaB?= M37xZmROW09? M4nUd4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> Ml\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrmSI82KM7:TR?= NUnkO2dKPDhiaB?= NFG4eFdFVVOR NFT2TZJqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NXTzTZI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
ACHN NFO2WoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXG1JO69VQ>? MoTzOFghcA>? M3LPXGROW09? NFnUZYlqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> MnL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 M4fjcGZ2dmO2aX;uJGF{e2G7 NXvYe5lJOC53L{GvOUDPxE1? M3nGeVQ5KGh? MXjEUXNQ MY\s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NVzMXXFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
A498 MlOzSpVv[3Srb36gRZN{[Xl? Mn;RNE42NzFxNTFOwG0> NUnlfGlXPDhiaB?= NUD2[W5HTE2VTx?= NIThTHNt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
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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 CC(C)OC1=C(C=CC(=C1)OC)C2=NC(C(N2C(=O)N3CCNC(=O)C3)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl

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SDS/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SDS/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/MDMXシグナル伝達経路

相関MDM2/MDMX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