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)  
JPY 30710.00
JPY 18260.00
JPY 28220.00
JPY 61420.00
JPY 161020.00
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文献中Selleckの製品使用例(12)

カスタマーフィードバック(5)

  • 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.

     

    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.

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

    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.

  • 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 Ml35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXy1xsDPxE1? MnLHOFjDqGh? NYDnTlE6[myxY3vzJFI4NU:KQz3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbjDjc41x[XKjYnzlJJRwKHSqYYSgc4Yh[mG|YXygcIV3\Wy| NGTsZ|kzPjN3MEW2OS=>
NP69 NHjSNJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTNzLk[5xtEzNjV2IN88US=> NW\iVms{OjZ{NUK1O|U>
NP460 M2DSNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XseGlEPTB;MkKuPFXDuTFwMUig{txO MkOwNlYzPTJ3N{W=
C666-1 NETWbXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7wR3JLUUN3ME2xPU46PcLzOD65N{DPxE1? MkPqNlYzPTJ3N{W=
C666-1 MnGzR4VtdCCYaXHibYxqfHliQYPzZZk> MX2xNEDDvU1? NHj2SHc1QCCq M1fuO2ROW09? MUPz[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzD0bIUh[3m2b4TvfIlkKGWoZnXjeEBw\iClaYPwcIF1cW5? MXqyOlI2OjV5NR?=
C666-1  M1jiZmZ2dmO2aX;uJGF{e2G7 M2fqWVExKML3TR?= M2G1T|I1KGh? MV7EUXNQ MmnvZYN1cX[jdHXzJJRp\SCyNUOgdIF1cHejeTygeZBz\We3bHH0bY5oKHB3MzygdFIyKGGwZDDN[I0z MkTmNlYzPTJ3N{W=
C666-1 MWrBdI9xfG:|aYOgRZN{[Xl? NHq4RlMyOCEEtV2= MXm0PE84OiCq M3nmbmROW09? MkXvd4Vve2m2aYrld{BEPjZ4LUGgZ4VtdHNidH:gZ4l{eGyjdHnuMYlv\HWlZXSgZZBweHSxc3nz NVTrdlJ5OjZ{NUK1O|U>
A549 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1LOelI1KGh? MX;JR|UxRTF5Lk[4JOKyKDRwNUKg{txO M1PQU|I3OTJ3MkOw
A549-NTC Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYSyOEBp NHfxUG9KSzVyPUG5MlQzKMLzIEGuPVYh|ryP NFnPWYIzPjF{NUKzNC=>
A549-920 M2DsT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm[2NlQhcA>? NEfQTIFKSzVyPUOzMlg2KMLzIESuPFQh|ryP MnfDNlYyOjV{M{C=
CRL-5908 MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnX1NlQhcA>? M3f2bGlEPTB;M{iuO|EhyrFiMj60N{DPxE1? NFLwfYczPjF{NUKzNC=>
L6 MkTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTrNVDDqM7:TdMg M2Lpb|I1NzR6L{eyJIg> NFrwTXZFVVOR M{DVb4lvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NHTHOVMzPTh5MUe5OC=>
C2C12 NITm[4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfrNVDDqM7:TdMg Ml7oNlQwPDhxN{KgbC=> NIHPcXJFVVOR NGLoPHFqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? M3nNdFI2QDdzN{m0
MCF-7  MVHGeY5kfGmxbjDBd5NigQ>? M4XKN|ExyqEQvF2= Mnu3SG1UVw>? NXL5VGducW6qaXLpeJMh[3mlbHnuJGQyKGGwZDDEbYNmesLi NXfqVZFqOjV5MEK3NFM>
DU4475  MXPGeY5kfGmxbjDBd5NigQ>? MVK1M|ExNzJyIN88US=> M{nObVI1yqCq MlfG[I94dnKnZ4XsZZRmeyCWb3PhMVEh\G:|ZTDk[ZBmdmSnboTsfS=> MUOyOVU1PzF5NB?=
SMMC-7721 MWrGeY5kfGmxbjDBd5NigQ>? MUGxNEDPxE1? MnTmOFghcA>? M{nLfGROW09? NWrGflB7[2G3c3XzJGRPSSCGU1Kg[IFu[Wen MWeyOVU1PDN4MR?=
SMMC-7721 MXHGeY5kfGmxbjDBd5NigQ>? NHW2dYkyOCEQvF2= Mm\HOFghcA>? NGrJbm9FVVOR MmCwbY5lfWOnczD0bIUh[2i{b33heIlvNWKxdX7kJJBzd3SnaX6gTWZKOTZidH:gdIFzfGmjbHz5JIxw[2GuaYrlJIlvKHSqZTDjfZRweGyjc35CpC=> NIfyfXQzPTV2NEO2NS=>
SMMC-7721 MYTGeY5kfGmxbjDBd5NigQ>? M1uzR|ExKM7:TR?= NFXNSmw1QCCq MoT3SG1UVw>? NHzzWJBqdmO{ZXHz[ZMhfGinIHX4dJJme3Orb36gcIV3\Wxib3dCpGlHVkJzwrDtVm5C MU[yOVU1PDN4MR?=
SMMC-7721 NVW0VIJKTnWwY4Tpc44hSXO|YYm= NWH6SoNCOTBizszN MnnmN|YhcA>? MkHNSG1UVw>? NIL4VnVk[XW|ZYOgeIhmKGWldH;wbYMh\XiycnXzd4lwdiCxZjDJSmkyPg>? M2X5TVI2PTR2M{[x
MCF-7 MojnSpVv[3Srb36gRZN{[Xl? MUixNOKh|ryP NX2wR3JWOC1{NDDo MYPpcoR2[2W|IIC1N{BidmRicEKxM2NqeDF? MkfMNlU1QDJ|N{O=
OVCAR10 NVfDSoZnTnWwY4Tpc44hSXO|YYm= M2Ph[lExyqEQvF2= NGXSepEzOWkEoB?= Mnn3SG1UVw>? NWDRd3pLcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? NW\tcolROjV2Mk[1OFg>
NCI-H23 MnPUSpVv[3Srb36gRZN{[Xl? MVexNOKh|ryP MnnyNlFpyqB? NVvFeXJmTE2VTx?= Mon2bY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> NGH6NZQzPTR{NkW0PC=>
A2780 MXnGeY5kfGmxbjDBd5NigQ>? MnXiNVDDqM7:TR?= M3[0U|IycMLi NFjud21FVVOR NXrZVlJpcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? M4j0Z|I2PDJ4NUS4
NCI-H23 NIDkeo9HfW6ldHnvckBCe3OjeR?= NFf5d3UyOMLizszN NVKxOIMyOjGqwrC= NEnkWFdFVVOR M2[5[YRm[3KnYYPld{B1cGViRn;4UVEhdGW4ZXzz NHXiR5UzPTR{NkW0PC=>
A2780 MX7GeY5kfGmxbjDBd5NigQ>? NHrPeHAyOMLizszN NG\wUYszOWkEoB?= M{j5NGROW09? MYfk[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= NYXXeVkyOjV2Mk[1OFg>
HCT116  MoDWSpVv[3Srb36gRZN{[Xl? NGn0cVAyOCEEtV2= M1TrO|I1KGh? MnnNZ4F2e2W|IHGgdFU{NWSncHXu[IVvfCC2ZYTyZZBtd2mmIFexMYFzemW|dDDpckBlcXCub3nkJGhEXDFzNjDjcI9v\XNiREOgZY5lKER6 NXXhOm1zOjV|OECwOVU>
MCF-10CA1a NIHKS3JHfW6ldHnvckBCe3OjeR?= NEi2SYIyOMLizszN MVO0PEBp M3PzZ2ROW09? M2PSSYlvcGmkaYTzJIJie2GuIHnueoF{cW:wIHHu[EBz\WS3Y3XkJHRITi4QskOtbY5lfWOnZDDpcpZie2mxbjD0c{Bj[XOjbDDs[ZZmdHN? NVn5fFdzOjV{NUe3Nlk>
MCF-10A1  MkHQSpVv[3Srb36gRZN{[Xl? M1jJRlExyqEQvF2= NVi2b2FROjRxNEigbC=> NUDLVnRoTE2VTx?= MV7pcohq[mm2czDtbYdz[XSrb36gc4Yhdm:{bXHsJIJz\WG|dDDldIl1cGWuaXHsxsA> M3L4UFI2OjV5N{K5
MCF-10CA1a MYHGeY5kfGmxbjDBd5NigQ>? NX7sUFNDOTEEoN88US=> MkfLNlQhcA>? NWHFOXlqTE2VTx?= Mnmz[IVkemWjc3XzJJRp\SCWR1[t{tI{NWmwZIXj[YQhdVKQQTDs[ZZmdHNib3\NUXAzNMLiTV3QPUwh[W6mwrDpcpRm\3KrbtMg{tLDqDN? NILMU|kzPTJ3N{eyPS=>
MCF-10CA1a NV7BU5l4TnWwY4Tpc44hSXO|YYm= MnzvNVDDqM7:TR?= MUCyOEBp NUPvOogxTE2VTx?= M{PwXYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= MUSyOVI2Pzd{OR?=
SK-BR-7 MoPzSpVv[3Srb36gRZN{[Xl? MlfMNVDDqM7:TR?= Mk\INlQhcA>? MWfEUXNQ M{ThZolvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= NYXGZ4w1OjV{NUe3Nlk>
SUM102PT M3O2XmZ2dmO2aX;uJGF{e2G7 NILUXo4yOMLizszN NGXFeJgzPCCq NIeyNJVFVVOR NV22bnVocW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u MXmyOVI2Pzd{OR?=
RAW 264.7 NUDYeYhZTnWwY4Tpc44hSXO|YYm= NV;0WJlZOTEEoN88US=> M3;uW|MxKG2rbh?= NEfKVGZxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> NWLWcIRYOjVzN{K1OFc>
RAW 264.7 MXXGeY5kfGmxbjDBd5NigQ>? NFjnUXMyOMLizszN NXnTOIRbOzBibXnu M4S2RpJm\HWlZYOgeIhmKEySUz3heYdu\W62ZXSgeIhmKE6ILd86RkBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZYN1cX[rdIm= MVSyOVE4OjV2Nx?=
RAW 264.7 NYLqcZVETnWwY4Tpc44hSXO|YYm= NGDJZ4wyOMLizszN M1PQ[VMxKG2rbh?= MlzHbY5pcWKrdIOgUHBUNWmwZIXj[YQhVk9icILv[JVkfGmxbtMg M{jYeFI2OTd{NUS3
MCF7  M37mWmNmdGxiVnnhZoltcXS7IFHzd4F6 MoXoNk42KML3TR?= M3TScVUh\A>? MonRSG1UVw>? MV3z[Y5{cXSrenXzJG1ETjdidH:gVGFTWCCrbnjpZol1cW:w M1vrXVI2ODh3OUCy
MCF7  MlLLSpVv[3Srb36gRZN{[Xl? MVSyMlUhyrWP NIK2Voo1QCCq MUPEUXNQ NXHlZW1X\GWlcnXhd4V{KHSqZTDoc41wdG:pb4XzJGRUSiC{ZYDhbZIh\nKncYXlcoNq\XN? MWCyOVA5PTlyMh?=
ACHN MYHD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVqwMlUuOTBizszN NHruTnUxNTZiZB?= NUnqNGp3TE2VTx?= M36yXYlvcGmkaYTzJJBzd2yrZnXyZZRqd25iaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M1:0bVI2ODZ5N{i3
Caki-2 M1LuUGNmdGxiVnnhZoltcXS7IFHzd4F6 NHnaS3IxNjVvMUCg{txO MlTZNE03KGR? MVnEUXNQ NVX1OIo{cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= M4TRcVI2ODZ5N{i3
A498 Ml\yR4VtdCCYaXHibYxqfHliQYPzZZk> Mnr2NE42NTFyIN88US=> NVGyT|hxOC14IHS= M2XuV2ROW09? NV\aVId1cW6qaXLpeJMheHKxbHnm[ZJifGmxbjDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MVuyOVA3Pzd6Nx?=
115 NIPv[YpE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M334WlAvPS1zMDFOwG0> MUOwMVYh\A>? NGTq[mlFVVOR MW\pcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NY[0NlBIOjVyNke3PFc>
117 MlXYR4VtdCCYaXHibYxqfHliQYPzZZk> MYqwMlUuOTBizszN MWSwMVYh\A>? M4HW[WROW09? NFHuNnhqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ Mlj3NlUxPjd5OEe=
ACHN NY\EbYp3TnWwY4Tpc44hSXO|YYm= MXOwMlUwOS93IN88US=> MVi0PEBp NEL0SIdFVVOR NFTRb4tt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= MkD5NlUxPjd5OEe=
Caki-2 M4rOeWZ2dmO2aX;uJGF{e2G7 NYDKNnFlOC53L{GvOUDPxE1? MlTLOFghcA>? MmfjSG1UVw>? MWDs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MkK5NlUxPjd5OEe=
A498 M4LBOmZ2dmO2aX;uJGF{e2G7 NHXs[48xNjVxMT:1JO69VQ>? M12yVlQ5KGh? NFzIXlBFVVOR MX3s[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? MU[yOVA3Pzd6Nx?=
115 NEW0RndHfW6ldHnvckBCe3OjeR?= NELEN|QxNjVxMT:1JO69VQ>? MUK0PEBp NXrYXpJPTE2VTx?= MVTs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? NUTtWHNQOjVyNke3PFc>
ACHN M{\MeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVu1JO69VQ>? M13r[|Q5KGh? M2T6XmROW09? M1nNbYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MnXrNlUxPjd5OEe=
Caki-2 MkKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW[1N2pQPSEQvF2= M1O2UVQ5KGh? M2rMRWROW09? NUfVdZNUcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MXSyOVA3Pzd6Nx?=
A498 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP0[482KM7:TR?= MUK0PEBp MUnEUXNQ M2XISIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NVztW4c5OjVyNke3PFc>
115 M3vl[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml3wOUDPxE1? NWLNUY01PDhiaB?= MYDEUXNQ NIP4RlFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NFKyV20zPTB4N{e4Oy=>
ACHN MmT6SpVv[3Srb36gRZN{[Xl? MnSzOUDPxE1? M4jqOlQ5KGh? M33uZmROW09? MnrYbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MofCNlUxPjd5OEe=
Caki-2 NX64V251TnWwY4Tpc44hSXO|YYm= MV61JO69VQ>? NYjTUGdwPDhiaB?= NVLz[2Z2TE2VTx?= MWHpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi Mm\yNlUxPjd5OEe=
A498 M1LI[GZ2dmO2aX;uJGF{e2G7 M2DlWFUh|ryP NYDxcWhCPDhiaB?= NFPHbWdFVVOR MmjWbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M2fjNlI2ODZ5N{i3
115 MV7GeY5kfGmxbjDBd5NigQ>? NXfLOnRpPSEQvF2= MnLIOFghcA>? M2PsUWROW09? NIrTZ45qdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MYOyOVA3Pzd6Nx?=
MOLM-13 NGWzdHBHfW6ldHnvckBCe3OjeR?= Mon3OuKh|ryP NFrpVYExNThiaB?= MmnzSG1UVw>? NY\oZpV[cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| NFzqcmwzPDh6NUC4Ni=>
MOLM-13 M{O3RmZ2dmO2aX;uJGF{e2G7 MUC2xsDPxE1? NF3BeW03KGh? NETQ[mxFVVOR NFq2R4FmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw MkGxNlQ5QDVyOEK=
HepG2 NHSzeXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmjTO|IhcA>? NXPZbm04TE2VTx?= M1vB[mlEPTB;M{WuPFYhyrFiMj65JO69VQ>? NEDPPGczPDh6NEiwPS=>
HepG2/As MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkG4O|IhcA>? M3fkcGROW09? NEHuU29KSzVyPU[4MlE{KMLzIEmuOkDPxE1? Ml34NlQ5QDR6MEm=
SMMC7721 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjVdZg4OiCq MYTEUXNQ NUnQR4xoUUN3ME2zNU4zQCEEsTC0MlIh|ryP NIfYN44zPDh6NEiwPS=>
SMMC7721/Ac NFXmcYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW[3NkBp M4DaWWROW09? MVHJR|UxRTV3LkKxJOKyKDVwMEOg{txO Ml3rNlQ5QDR6MEm=
Huh-7 MkLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HxTlczKGh? NXXueZZVTE2VTx?= MYjJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> MlPqNlQ5QDR6MEm=
Hep3B NGW1TJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYm3NkBp MoDKSG1UVw>? M4XndGlEPTB;MkCuNVghyrFiMT64OEDPxE1? MXSyOFg5PDhyOR?=
HepG2 M2LIXWFxd3C2b4Ppd{BCe3OjeR?= NXLXOJd2cW6mdXPld{BieG:ydH;zbZM> MmHqNlQ5QDR6MEm=
SMMC7721 NFrDUGhCeG:ydH;zbZMhSXO|YYm= M1zscolv\HWlZYOgZZBweHSxc3nz MnfnNlQ5QDR6MEm=
Huh-7 MkLtRZBweHSxc3nzJGF{e2G7 M1fWUYlv\HWlZYOgZZBweHSxc3nz NFjBOY0zPDh6NEiwPS=>
Hep3B MV7BdI9xfG:|aYOgRZN{[Xl? NX\KXopscW6mdXPld{BieG:ydH;zbZM> NFTQPFEzPDh6NEiwPS=>
U2OS  M2DrSWZ2dmO2aX;uJGF{e2G7 M1K3TVIxKM7:TR?= Mn;zNlQhcA>? M4nwRYlv[3KnYYPld{B1cGVibWLORUBt\X[nbIOgc4bDqEKFTELBNUwhSkOOWF|CpIFv\EKFTGe= NXfTWllbOjR6NkeyOVk>
AML2 NV7HNolOSXCxcITvd4l{KEG|c3H5 M3TB[|IwOTBizszN MkfWNlQwPDhiaB?= NUHldJkzcW6mdXPld{BieG:ydH;zbZM> M2fwWFI1PjV7N{S5
MOML13 NXnXZnJwSXCxcITvd4l{KEG|c3H5 MljFNk8yOCEQvF2= MYeyOE81QCCq M3ni[Ilv\HWlZYOgZZBweHSxc3nz MYCyOFY2QTd2OR?=
AML2 MnvhSpVv[3Srb36gRZN{[Xl? MVyxNO69VQ>? NV[1N29kOi92IHi= MlLGbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= Ml3RNlQ3PTl5NEm=
AML3 M2\STmZ2dmO2aX;uJGF{e2G7 MlvwNVDPxE1? NUnsWo44Oi92IHi= NFnTUmpqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MmLBNlQ3PTl5NEm=
MOML13 NWHPV5JTTnWwY4Tpc44hSXO|YYm= NFmze4IyOM7:TR?= M4L5NFIwPCCq NX\iWoU4cW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MXKyOFY2QTd2OR?=
BeWo M1u5XGZ2dmO2aX;uJGF{e2G7 Mmf4N|AhyrWP MlLnNlQhcA>? Mln0bY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs NEL0TpkzPDR7OEG1OC=>
BeWo MlP6RZBweHSxc3nzJGF{e2G7 MVSzNEDDvU1? MXuyOEBp MULpcoNz\WG|ZYOgZZBweHSxc3nz MV[yOFQ6QDF3NB?=
OCI NILRS41HfW6ldHnvckBCe3OjeR?= MmHxNVAh|ryP M{naV|I1KGh? M1K5dZVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= M1TQN|I1PDd|NU[y
MOLM NFe5[2tHfW6ldHnvckBCe3OjeR?= M4noPFExKM7:TR?= MXuyOEBp M{LnZ5VxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= M1P5NlI1PDd|NU[y
U2OS  MYjGeY5kfGmxbjDBd5NigQ>? MkTrNlAh|ryP NV23Onl4OjRiaB?= M4PtU4lv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? M2XUWFI1OzZ4MEC3
RKO MYLGeY5kfGmxbjDBd5NigQ>? MX2yNEDPxE1? NYLpN3VwOjRiaB?= MVLpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NVuzcHJiOjR|Nk[wNFc>
U2OS  NXuy[nBqTnWwY4Tpc44hSXO|YYm= M33LPVIxKM7:TR?= M1\leFI1KGh? M2H0bolv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u M4HW[VI1OzZ4MEC3
RKO NH3B[2JHfW6ldHnvckBCe3OjeR?= NFjnRYczOCEQvF2= MUOyOEBp MWPpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= MX6yOFM3PjByNx?=
SMMC-7721  MUXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MmXZNU4zPS1{MDFOwG0> M4TMTFI1NzR6L{eyJIg> MmjNSG1UVw>? MVnpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MYSyOFI5PjNzMh?=
HuH-7 MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NI\FOlQyNjJ3LUKwJO69VQ>? MUSyOE81QC95MjDo M{LscWROW09? MXTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M4O1U|I1Ojh4M{Gy
SMMC-7721  M4nkXWFxd3C2b4Ppd{BCe3OjeR?= NHLDTnUzOCEQvF2= NEjhbok1QCCq NGf6TGNFVVOR NGL2WmtqdmS3Y3XzJIFxd3C2b4Ppdy=> NVzPSopDOjR{OE[zNVI>
HuH-7 Ml\nRZBweHSxc3nzJGF{e2G7 MUiyNEDPxE1? NVHobI5QPDhiaB?= MWPEUXNQ NFPzUZpqdmS3Y3XzJIFxd3C2b4Ppdy=> NYHrUXA4OjR{OE[zNVI>
SMMC-7721  NHnWUlVHfW6ldHnvckBCe3OjeR?= MXqxNEDPxE1? MYezOkBp NXy5coFuTE2VTx?= MXfkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> NH33bVczPDJ6NkOxNi=>
HuH-7 M{jNVWZ2dmO2aX;uJGF{e2G7 M{D3SlExKM7:TR?= M2mwblM3KGh? MkD6SG1UVw>? NUDMdWxv\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? MkPrNlQzQDZ|MUK=
AT2 MlqySpVv[3Srb36gRZN{[Xl? M2OzfFUwOTBizszN MXTs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MkHWNlQzPDB{MEO=
REH MlLqSpVv[3Srb36gRZN{[Xl? NFz3ZVY2NzFyIN88US=> MVjs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? NInhe2gzPDJ2MEKwNy=>
UoCB6 MmDrSpVv[3Srb36gRZN{[Xl? NYjiTldvPS9zMDFOwG0> MlPCcIVi\HNidH:gZUB{fWK|dHHueIlidCCjY3P1cZVt[XSrb36gc4YhfGinIIC1N{Bxem:2ZXnuJIF{KHenbHygZZMhfGinIHX4dJJme3Orb36gc4YhcXS|IHTpdoVkfCC2YYLn[ZR{KHB{MTygUWROOiCjbnSgeIhmKHC{bz3hdI9xfG:2aXOgRmFZKGGwZDDQWW1CKHC{b4TlbY5{yqB? MnP1NlQzPDB{MEO=
AT2 MnuxR4VtdCCYaXHibYxqfHliQYPzZZk> MYOwMVI2KM7:TR?= MlGybY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? MVGyOFI1ODJyMx?=
REH MXfD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NUDKZXZ[OC1{NTFOwG0> NXPBRnV1cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NWPWUpF3OjR{NECyNFM>
UoCB6 NYrKe4tqS2WubDDWbYFjcWyrdImgRZN{[Xl? MY[wMVI2KM7:TR?= NXXsc4gycW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYjiZpltOjR{NECyNFM>
A2780 NGHYSnJHfW6ldHnvckBCe3OjeR?= NVy1cmtbPS9zMD:yNEDPxE1? MXWyOEBp M4jMWJVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi M2LufFI1OTN4MUS3
H460 NFK4R5dHfW6ldHnvckBCe3OjeR?= MWS1M|ExNzJyIN88US=> MoPuNlQhcA>? NX25fmdUfXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= NHTKS5UzPDF|NkG0Oy=>
Lovo  M4X1OWZ2dmO2aX;uJGF{e2G7 NEXGWZA2NzFyL{KwJO69VQ>? MViyOEBp NWru[nR7fXC{ZXf1cIF1\XNicEWzMEBOTE1{LDDwNlEh[W6mIFTSOUBxem:2ZXnuJIxmfmWuczDkc5NmKGSncHXu[IVvfGy7wrC= MYKyOFE{PjF2Nx?=
A2780 NVvDdHc1SXCxcITvd4l{KEG|c3H5 NXHySIE3PS9zMD:yNEDPxE1? NYGy[VNpOjRiaB?= NG\mUmdmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? NXz3ZpBXOjRzM{[xOFc>
H460 Ml7ZRZBweHSxc3nzJGF{e2G7 MoD6OU8yOC9{MDFOwG0> MmDXNlQhcA>? NXj6N4FN\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? NV7PVnFJOjRzM{[xOFc>
Lovo  M17vUGFxd3C2b4Ppd{BCe3OjeR?= MknoOU8yOC9{MDFOwG0> NX70OWF3OjRiaB?= NHvUdodmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? NEXVem0zPDF|NkG0Oy=>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい
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 (g) = 濃度 (mol/L) x 体積 (L) 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