Nutlin-3

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)  
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(18)

カスタマーフィードバック(5)

  • Ubiquitination of p53 in vivo by BIRC6 in the presence of Nutlin-3. Cells were treated with Nutlin-3 (20 uM, 24 h) before harvest. Cell lysates were immunoprecipitated with anti-p53 antibody and immunoblotted by anti-ubiquitin antibody.

    Int J Oncol 2014 44, 761-8. Nutlin-3 purchased from Selleck.

  •  

    p53 activation in A76T p53-mutated UKF-NB-3’RITA(10 uM) IV cells. Cells were treated with RITA (10 uM) or nutlin-3 (10 uM) for 24 h and investigated by western blot for the expression of p53 target genes

    Cell Death Dis 2012 3, e294. Nutlin-3 purchased from Selleck.

  • Caspase 3/7 activation in UKF-NB-3 or UKF-NB-3rNutlin10 μM cells treated nutlin-3 (10 μM), VCR (10 ng/ml), DOX (20 ng/ml), or CDDP (1000 ng/ml).

    Cell Death Dis 2011 2, e243. Nutlin-3 purchased from Selleck.

  • J Cell Physiol, 2018, 233(9):7424-7434. Nutlin-3 purchased from Selleck.

  • d qPCR evaluation of DKK1 in MSCs exposed to melphalan in combination with increasing concentrations of nutlin-3 for 24 h. Cells were pre-treated with nutlin-3 for 20 min prior to chemotherapy. *Indicates p value<0.05, One-way ANOVA with Holm-Sidak post hoc

    Med Oncol, 2016, 33(10):113. Nutlin-3 purchased from Selleck.

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 MlXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M124[|XDqM7:TR?= MVO0POKhcA>? Mn7WZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ MXKyOlM2ODV4NR?=
NP69 NF3DbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHHZ5RKSzVyPUOxMlY6yrF{LkW0JO69VQ>? MmH4NlYzPTJ3N{W=
NP460 NG\nOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m0S2lEPTB;MkKuPFXDuTFwMUig{txO M3Ps[|I3OjV{NUe1
C666-1 NUTBV49oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTF7Lkm1xtE5Njl|IN88US=> MnrmNlYzPTJ3N{W=
C666-1 M3\UXWNmdGxiVnnhZoltcXS7IFHzd4F6 MoDrNVAhyrWP NW\DRlR{PDhiaB?= MYfEUXNQ MXvz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzD0bIUh[3m2b4TvfIlkKGWoZnXjeEBw\iClaYPwcIF1cW5? NESyZZkzPjJ3MkW3OS=>
C666-1  MnTySpVv[3Srb36gRZN{[Xl? MnTONVAhyrWP MXGyOEBp NULzc2Q3TE2VTx?= M{HTOoFkfGm4YYTld{B1cGVicEWzJJBifGi5YYmsJJVxemWpdXzheIlv\yCyNUOsJJAzOSCjbnSgUYRuOg>? MXmyOlI2OjV5NR?=
C666-1 NWTOSoU3SXCxcITvd4l{KEG|c3H5 M2nVd|ExKML3TR?= MUS0PE84OiCq MUjEUXNQ NF3LOHV{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{BkcXOybHH0bY4ucW6mdXPl[EBieG:ydH;zbZM> NV\OOYVMOjZ{NUK1O|U>
A549 NGD6RWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXuyOEBp NVyyO5ZGUUN3ME2xO{43QCEEsTC0MlUzKM7:TR?= NU\3Wo5NOjZzMkWyN|A>
A549-NTC M3;HW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVeyOEBp M4\IfWlEPTB;MUmuOFIhyrFiMT65OkDPxE1? MUWyOlEzPTJ|MB?=
A549-920 MojrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYWyOEBp M373PWlEPTB;M{OuPFUhyrFiND64OEDPxE1? M4PPPFI3OTJ3MkOw
CRL-5908 Ml;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXeyOEBp MoDyTWM2OD1|OD63NUDDuSB{LkSzJO69VQ>? M1r3fVI3OTJ3MkOw
L6 NG\EZZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3f4PVExyqEQvF5CpC=> M{i4UlI1NzR6L{eyJIg> MlvJSG1UVw>? NF2yVotqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MW[yOVg4OTd7NB?=
C2C12 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXKzTYhIOTEEoN88UeKh M3vme|I1NzR6L{eyJIg> NIHWR2ZFVVOR MkTQbY5pcWKrdIOgZ4VtdHNicILvcIln\XKjdHnvckBidmRiZHnm[oVz\W62aXH0bY9v NV7iPI12OjV6N{G3PVQ>
MCF-7  M1vRTGZ2dmO2aX;uJGF{e2G7 M2nRfFExyqEQvF2= NWTTVJZCTE2VTx?= MojZbY5pcWKrdIOgZ5lkdGmwIFSxJIFv\CCGaXPlduKh NGXZW5AzPTdyMkewNy=>
DU4475  M1fLT2Z2dmO2aX;uJGF{e2G7 M2Dh[lUwOTBxMkCg{txO M2rwS|I1yqCq NGrZS|Fld3ewcnXneYxifGW|IGTvZ4EuOSCmb4PlJIRmeGWwZHXueIx6 NGrrUGUzPTV2N{G3OC=>
SMMC-7721 M3TNUWZ2dmO2aX;uJGF{e2G7 Mnv4NVAh|ryP MnrROFghcA>? MYHEUXNQ NEn4WnRk[XW|ZYOgSG5CKESVQjDkZY1i\2V? NWP2T4JNOjV3NESzOlE>
SMMC-7721 M4\MOWZ2dmO2aX;uJGF{e2G7 MX2xNEDPxE1? M4TDTlQ5KGh? MVXEUXNQ MXrpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg NX3ZcFFZOjV3NESzOlE>
SMMC-7721 NEH0OGlHfW6ldHnvckBCe3OjeR?= MnS4NVAh|ryP M17aUlQ5KGh? NF74RolFVVOR NImweXdqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C MW[yOVU1PDN4MR?=
SMMC-7721 M1frTGZ2dmO2aX;uJGF{e2G7 MnnzNVAh|ryP MV2zOkBp Mm\WSG1UVw>? NXSzdXNR[2G3c3XzJJRp\SCnY4TvdIlkKGW6cILld5Nqd25ib3[gTWZKOTZ? M3zvRlI2PTR2M{[x
MCF-7 NWK3RYo4TnWwY4Tpc44hSXO|YYm= NHnIRngyOMLizszN M4TJcFAuOjRiaB?= NHuzOGVqdmS3Y3XzJJA2OyCjbnSgdFIyN0OrcEG= MV2yOVQ5OjN5Mx?=
OVCAR10 NXvufVgxTnWwY4Tpc44hSXO|YYm= NV65d|R1OTEEoN88US=> MlPhNlFpyqB? M3qzbWROW09? MnzobY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NEmxVGwzPTR{NkW0PC=>
NCI-H23 MV7GeY5kfGmxbjDBd5NigQ>? M1zPPFExyqEQvF2= NX[xcZdEOjGqwrC= NXuxSJVYTE2VTx?= NHzQN4xqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ M2DPXlI2PDJ4NUS4
A2780 M1vCdmZ2dmO2aX;uJGF{e2G7 M1\zbFExyqEQvF2= M2e1NlIycMLi NHvmO25FVVOR MV\pcoNz\WG|ZYOgdFU{KHC{b4TlbY4hdGW4ZXzz NUXFOJhEOjV2Mk[1OFg>
NCI-H23 NVr6[FFoTnWwY4Tpc44hSXO|YYm= M1XYblExyqEQvF2= NXrWSZBkOjGqwrC= MnvCSG1UVw>? M3;rZ4Rm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz M2HzNlI2PDJ4NUS4
A2780 MV;GeY5kfGmxbjDBd5NigQ>? MVmxNOKh|ryP M3X3cFIycMLi NXOwdlhVTE2VTx?= M3ixRYRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz M3fOS|I2PDJ4NUS4
HCT116  MUXGeY5kfGmxbjDBd5NigQ>? M1zUNVExKML3TR?= NYTjXmNpOjRiaB?= NYLpSY1U[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 MmXwNlU{QDByNUW=
MCF-10CA1a M{DhVGZ2dmO2aX;uJGF{e2G7 NFy4O24yOMLizszN MmLnOFghcA>? M1q5emROW09? MmLNbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? MYWyOVI2Pzd{OR?=
MCF-10A1  NGL2UHlHfW6ldHnvckBCe3OjeR?= MX2xNOKh|ryP MkXFNlQwPDhiaB?= NFztbFdFVVOR NULxXZAxcW6qaXLpeJMhdWmpcnH0bY9vKG:oIH7vdo1idCCkcnXhd5Qh\XCrdHjlcIlidMLi MXKyOVI2Pzd{OR?=
MCF-10CA1a MoHUSpVv[3Srb36gRZN{[Xl? MmPGNVDDqM7:TR?= M3jlSlI1KGh? MX7EUXNQ MoTp[IVkemWjc3XzJJRp\SCWR1[t{tI{NWmwZIXj[YQhdVKQQTDs[ZZmdHNib3\NUXAzNMLiTV3QPUwh[W6mwrDpcpRm\3KrbtMg{tLDqDN? MoXQNlUzPTd5Mkm=
MCF-10CA1a MmjHSpVv[3Srb36gRZN{[Xl? MmX1NVDDqM7:TR?= M{HwNlI1KGh? NF;xPHRFVVOR NHyxWmZqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= M1\uSlI2OjV5N{K5
SK-BR-7 MWPGeY5kfGmxbjDBd5NigQ>? NGrucnIyOMLizszN NIrj[XIzPCCq NWH2WIJDTE2VTx?= MUHpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? Mk\qNlUzPTd5Mkm=
SUM102PT NUXy[Hd5TnWwY4Tpc44hSXO|YYm= M{HzeVExyqEQvF2= M3nrd|I1KGh? NHHMW2JFVVOR M1TiXolvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= M17o[lI2OjV5N{K5
RAW 264.7 MnPMSpVv[3Srb36gRZN{[Xl? M3L1NlExyqEQvF2= MYezNEBucW5? NWnnRmY1eHKndnXueJMhfGinIIC1N{Bz\WS3Y4Tpc44hcW5icnXzdI9ve2VidH:gUHBU NHjwZXozPTF5MkW0Oy=>
RAW 264.7 NI\CTlJHfW6ldHnvckBCe3OjeR?= MYSxNOKh|ryP MlnKN|AhdWmw M3:3NZJm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= NYfo[ZhpOjVzN{K1OFc>
RAW 264.7 NHnkS4RHfW6ldHnvckBCe3OjeR?= M2jOU|ExyqEQvF2= NYDGOJAxOzBibXnu NWL2cJRvcW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MnLONlUyPzJ3NEe=
MCF7  M2L1NWNmdGxiVnnhZoltcXS7IFHzd4F6 NYe4WIFJOi53INM1US=> M3H0OFUh\A>? M{TFXWROW09? NULxRms1e2Wwc3n0bZpmeyCPQ1[3JJRwKFCDUmCgbY5pcWKrdHnvci=> NGO3SIYzPTB6NUmwNi=>
MCF7  NUDBe2RXTnWwY4Tpc44hSXO|YYm= NYfEcWJ3Oi53INM1US=> MnzDOFghcA>? NXLFTlQ4TE2VTx?= MknC[IVkemWjc3XzJJRp\SCqb33vcI9od3W|IFTTRkBz\XCjaYKg[pJmeXWnbnPp[ZM> M3f1ZlI2ODh3OUCy
ACHN NGOwcFdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYCwMlUuOTBizszN NXvjfWxtOC14IHS= NUnWNIYyTE2VTx?= NGXMdYtqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NWHpOVZzOjVyNke3PFc>
Caki-2 MlvUR4VtdCCYaXHibYxqfHliQYPzZZk> MmjDNE42NTFyIN88US=> M2TRbFAuPiCm NEOyRWVFVVOR NYDmb2R6cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MV:yOVA3Pzd6Nx?=
A498 NGXrOIdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NHvvcGwxNjVvMUCg{txO NEDQe3kxNTZiZB?= MYnEUXNQ NHXXeJRqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ M4jIVFI2ODZ5N{i3
115 NFnJNIdE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M1vFPVAvPS1zMDFOwG0> NHfDdGcxNTZiZB?= NHG3VHhFVVOR NG\Pe3pqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MnXYNlUxPjd5OEe=
117 MkHlR4VtdCCYaXHibYxqfHliQYPzZZk> MknyNE42NTFyIN88US=> NWi3WW5UOC14IHS= NVH1W3VQTE2VTx?= MnTsbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NFHKbJEzPTB4N{e4Oy=>
ACHN NHvzRWdHfW6ldHnvckBCe3OjeR?= M2\NWFAvPS9zL{Wg{txO NX\GfoRWPDhiaB?= MmHGSG1UVw>? MnHacIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? Mn\3NlUxPjd5OEe=
Caki-2 MlrZSpVv[3Srb36gRZN{[Xl? M2GxUVAvPS9zL{Wg{txO M364T|Q5KGh? Ml;YSG1UVw>? Ml:zcIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MlvZNlUxPjd5OEe=
A498 M3ztZmZ2dmO2aX;uJGF{e2G7 NYLYXVlqOC53L{GvOUDPxE1? NUPCXYkzPDhiaB?= Mn3USG1UVw>? M3u5Z4xm[WS|IITvJIlv[3KnYYPl[EBmgHC{ZYPzbY9vKG:oIIC1N{BidmRic3;t[UBxPTNidHHy[4V1KGenbnXzPkBOTE1{LDDhcoQheDJz MUeyOVA3Pzd6Nx?=
115 M1ixNWZ2dmO2aX;uJGF{e2G7 NIfpTI8xNjVxMT:1JO69VQ>? MY[0PEBp NV7QT4pzTE2VTx?= MV7s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MX:yOVA3Pzd6Nx?=
ACHN M3XIXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF\aO2c2KM7:TR?= Mo\COFghcA>? NV\wfI1NTE2VTx?= NUPkfXBtcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NIPpW5kzPTB4N{e4Oy=>
Caki-2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\QNZNSPSEQvF2= NGDI[m81QCCq MYLEUXNQ NXvvdVFncW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NIn1WWczPTB4N{e4Oy=>
A498 MnvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XFS|Uh|ryP MXO0PEBp MnfpSG1UVw>? MUHpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NVPPZoN[OjVyNke3PFc>
115 NIDNfYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV:1JO69VQ>? MYC0PEBp NWrn[JlDTE2VTx?= MoW3bY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MmLKNlUxPjd5OEe=
ACHN MYfGeY5kfGmxbjDBd5NigQ>? NFzM[JA2KM7:TR?= NWnHW|N4PDhiaB?= MnPiSG1UVw>? MmLBbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MlT0NlUxPjd5OEe=
Caki-2 NGHyc3RHfW6ldHnvckBCe3OjeR?= MknPOUDPxE1? NEPYN2U1QCCq NXLiToF6TE2VTx?= M13OPIlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MXSyOVA3Pzd6Nx?=
A498 M{LSVmZ2dmO2aX;uJGF{e2G7 NFL4S4w2KM7:TR?= Mmj6OFghcA>? MojOSG1UVw>? MVzpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MWiyOVA3Pzd6Nx?=
115 NVTETnlzTnWwY4Tpc44hSXO|YYm= MXe1JO69VQ>? NUDWcYxxPDhiaB?= M{fseGROW09? M3z1eYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= M1;wb|I2ODZ5N{i3
MOLM-13 NGDaVYxHfW6ldHnvckBCe3OjeR?= MkLNOuKh|ryP NIrCS5oxNThiaB?= MmrPSG1UVw>? MofqbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ NF[wTIUzPDh6NUC4Ni=>
MOLM-13 MXXGeY5kfGmxbjDBd5NigQ>? MYe2xsDPxE1? NID4V3g3KGh? NWnVZ4dKTE2VTx?= MWrlcohidmOnczD0bIUh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINmIh[W6mIHjlZZQhe2ixY3ugdJJwfGWrboOgTJNxOjdiYX7kJGh{eDly MU[yOFg5PTB6Mh?=
HepG2 NFW4XVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvmO|IhcA>? NYTXeHhRTE2VTx?= NF\SfWFKSzVyPUO1Mlg3KMLzIEKuPUDPxE1? NY\j[nBNOjR6OES4NFk>
HepG2/As MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYq3NkBp M1L2OmROW09? NWnncI1LUUN3ME22PE4yOyEEsTC5MlYh|ryP MUWyOFg5PDhyOR?=
SMMC7721 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP3O|IhcA>? MXvEUXNQ NEDP[INKSzVyPUOxMlI5KMLzIESuNkDPxE1? Mn;kNlQ5QDR6MEm=
SMMC7721/Ac MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LJflczKGh? M{W4R2ROW09? NXTDbItrUUN3ME21OU4zOSEEsTC1MlA{KM7:TR?= M4DFVlI1QDh2OEC5
Huh-7 M4ntT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXsR4oxPzJiaB?= NYPqWJhNTE2VTx?= MlnPTWM2OD1|Mz65OkDDuSB|Lkmg{txO NHLhdlEzPDh6NEiwPS=>
Hep3B MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonDO|IhcA>? MnPHSG1UVw>? NV;OUoJQUUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= NWGxXmRGOjR6OES4NFk>
HepG2 Ml3HRZBweHSxc3nzJGF{e2G7 MnvKbY5lfWOnczDhdI9xfG:|aYO= M2XlOFI1QDh2OEC5
SMMC7721 NHPDZm1CeG:ydH;zbZMhSXO|YYm= M4H3[olv\HWlZYOgZZBweHSxc3nz NVHkXYsxOjR6OES4NFk>
Huh-7 NYfBV2JkSXCxcITvd4l{KEG|c3H5 NUXrPZVVcW6mdXPld{BieG:ydH;zbZM> NYO5N3VTOjR6OES4NFk>
Hep3B M2jne2Fxd3C2b4Ppd{BCe3OjeR?= NIH3b4xqdmS3Y3XzJIFxd3C2b4Ppdy=> M1T1UFI1QDh2OEC5
U2OS  MXjGeY5kfGmxbjDBd5NigQ>? Mo\6NlAh|ryP M2jOVlI1KGh? M1TnN4lv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= MkHaNlQ5Pjd{NUm=
AML2 MVfBdI9xfG:|aYOgRZN{[Xl? NYTpO|g2Oi9zMDFOwG0> NH30W|czPC92ODDo M4WyfIlv\HWlZYOgZZBweHSxc3nz MXOyOFY2QTd2OR?=
MOML13 Ml3wRZBweHSxc3nzJGF{e2G7 M1nuVVIwOTBizszN MWGyOE81QCCq MYHpcoR2[2W|IHHwc5B1d3Orcx?= MWGyOFY2QTd2OR?=
AML2 M{fWVmZ2dmO2aX;uJGF{e2G7 NXvTbolrOTEQvF2= MYKyM|QhcA>? NYLuVph7cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NVr3XoZrOjR4NUm3OFk>
AML3 NFzxPVVHfW6ldHnvckBCe3OjeR?= NUDYcmczOTEQvF2= NETx[ngzNzRiaB?= Mom5bY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MX[yOFY2QTd2OR?=
MOML13 M{TXbmZ2dmO2aX;uJGF{e2G7 M2PuXlEx|ryP NVPQZVhVOi92IHi= MnSxbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= NFHR[|UzPDZ3OUe0PS=>
BeWo Mlq2SpVv[3Srb36gRZN{[Xl? NX7BbJhiOzBiwsXN NGHre20zPCCq MYLpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= MUCyOFQ6QDF3NB?=
BeWo Ml3XRZBweHSxc3nzJGF{e2G7 NXXuU3B[OzBiwsXN NEjzN4IzPCCq MnXpbY5kemWjc3XzJIFxd3C2b4Ppdy=> M3PFS|I1PDl6MUW0
OCI NIjVZ3hHfW6ldHnvckBCe3OjeR?= M1jiU|ExKM7:TR?= MorlNlQhcA>? NIfG[3d2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= NFe5TY0zPDR5M{W2Ni=>
MOLM MXXGeY5kfGmxbjDBd5NigQ>? Mm\FNVAh|ryP NWT0UYttOjRiaB?= M37FSpVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= Mn25NlQ1PzN3NkK=
U2OS  NEX5bVNHfW6ldHnvckBCe3OjeR?= Mm[xNlAh|ryP M1nxTVI1KGh? M3\kcolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? NHjU[VEzPDN4NkCwOy=>
RKO MorNSpVv[3Srb36gRZN{[Xl? NHy0UIkzOCEQvF2= M1W3dVI1KGh? NFP6W29qdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MV:yOFM3PjByNx?=
U2OS  M4\MdmZ2dmO2aX;uJGF{e2G7 MYKyNEDPxE1? MnvsNlQhcA>? MnjIbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= Mo[yNlQ{PjZyMEe=
RKO MkLBSpVv[3Srb36gRZN{[Xl? NIDheYUzOCEQvF2= MmC2NlQhcA>? NUCxTWJCcW6mdXPld{BJVy1zIHX4dJJme3Orb36gZZQhfGinIHzleoVtKG:oIITyZY5{[3KrcITpc44> MoTUNlQ{PjZyMEe=
SMMC-7721  M{fyPWNmdGxiVnnhZoltcXS7IFHzd4F6 M4f3UFEvOjVvMkCg{txO MXKyOE81QC95MjDo NFX1V|ZFVVOR NE[4[XBqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M2rTT|I1Ojh4M{Gy
HuH-7 MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NYTKfml{OS5{NT2yNEDPxE1? MnLwNlQwPDhxN{KgbC=> M2\Fb2ROW09? M1PQO4lvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MV2yOFI5PjNzMh?=
SMMC-7721  NVvoZoJ1SXCxcITvd4l{KEG|c3H5 NIjH[XUzOCEQvF2= NX;JOW1SPDhiaB?= M{TjRWROW09? NXvIdZlOcW6mdXPld{BieG:ydH;zbZM> NYrpbm5MOjR{OE[zNVI>
HuH-7 M{XRfmFxd3C2b4Ppd{BCe3OjeR?= NInxVWkzOCEQvF2= NEL5OoU1QCCq MXjEUXNQ MlP2bY5lfWOnczDhdI9xfG:|aYO= Mn25NlQzQDZ|MUK=
SMMC-7721  Mn7ySpVv[3Srb36gRZN{[Xl? MnzhNVAh|ryP MkX0N|YhcA>? NVzBNXJqTE2VTx?= NIXMZXpld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? NEf0WJUzPDJ6NkOxNi=>
HuH-7 NYTKblFqTnWwY4Tpc44hSXO|YYm= NXWycYZZOTBizszN NFPGdmI{PiCq Mm[1SG1UVw>? MkHs[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> M4K1R|I1Ojh4M{Gy
AT2 NIWyNXRHfW6ldHnvckBCe3OjeR?= NUjHdmxOPS9zMDFOwG0> MX7s[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MY[yOFI1ODJyMx?=
REH NYXpN5JzTnWwY4Tpc44hSXO|YYm= M4nrWFUwOTBizszN NVe5TnB3dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= M4PZdFI1OjRyMkCz
UoCB6 M{jOXmZ2dmO2aX;uJGF{e2G7 NU\aeIRLPS9zMDFOwG0> NYjtRmZvdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NXvsdIZYOjR{NECyNFM>
AT2 MofJR4VtdCCYaXHibYxqfHliQYPzZZk> Mm\uNE0zPSEQvF2= NUDpNZM4cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MY[yOFI1ODJyMx?=
REH MYXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MnviNE0zPSEQvF2= NW\6PWhCcW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= MV[yOFI1ODJyMx?=
UoCB6 NGHKfoNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGjmV28xNTJ3IN88US=> M4Dod4lvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MoHoNlQzPDB{MEO=
A2780 Mmj3SpVv[3Srb36gRZN{[Xl? NG\rfIk2NzFyL{KwJO69VQ>? MYKyOEBp NF2xUG52eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= M4exR|I1OTN4MUS3
H460 MkXRSpVv[3Srb36gRZN{[Xl? MlfZOU8yOC9{MDFOwG0> NFnHN4QzPCCq MUL1dJJm\3WuYYTld{BxPTNuIF3EUVItKHB{MTDhcoQhTFJ3IIDyc5RmcW5ibHX2[Yx{KGSxc3Wg[IVx\W6mZX70cJnDqA>? Ml61NlQyOzZzNEe=
Lovo  NX\MNlB5TnWwY4Tpc44hSXO|YYm= NW\yNmZKPS9zMD:yNEDPxE1? MX2yOEBp NHP5[lV2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= M2PjNVI1OTN4MUS3
A2780 MojwRZBweHSxc3nzJGF{e2G7 MVK1M|ExNzJyIN88US=> NWXJPFN2OjRiaB?= NGXMb2dmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? MmC5NlQyOzZzNEe=
H460 M4XRZ2Fxd3C2b4Ppd{BCe3OjeR?= MmnlOU8yOC9{MDFOwG0> NHvPclMzPCCq M3G2XYVvcGGwY3XzJIFxd3C2b4Ppd{BqdmS3Y4Tpc44h[nliREK2PWgwTTF7NWKgc5ZmeiC{aGTSRWlN M{j1SFI1OTN4MUS3
Lovo  MWfBdI9xfG:|aYOgRZN{[Xl? MUO1M|ExNzJyIN88US=> NH;jRVIzPCCq Mmn6[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MkXlNlQyOzZzNEe=

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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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 動物モデル： Athymic female nude mice (Nu/Nu-nuBR) injected subcutaneously with SJSA-1 cells
  • 製剤： Formulated in 2% Klucel, 0.5% Tween 80
  • 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
保管 粉
in solvent
別名 N/A

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.

selleck catalog

Mdm2シグナル伝達経路

相関Mdm2製品

  • MI-773 (SAR405838)

    MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

  • A-1210477

    A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family members.

  • NSC 207895

    NSC 207895 suppresses MDMX with IC50 of 2.5 μM, leading to enhanced p53 stabilization/activation and DNA damage, and also regulates MDM2, an E3 ligase.

  • Nutlin-3a

    Nutlin-3a, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM in a cell-free assay.

    Features:Highly selective MDM2 inhibitor with a much lower effect on MDMX. Most effective on tumors with wild type p53.

  • Nutlin-3b

    Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

  • YH239-EE

    YH239-EE, the ethyl ester of YH239, is a potent p53-MDM2 antagonist and an apoptosis inducer.

  • Z-VAD-FMK

    Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

    Features:A key compound for apoptosis studies.

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