Nutlin-3

For research use only. Not for use in humans.

目录号:S1061

Nutlin-3 Chemical Structure

CAS No. 890090-75-2

Nutlin-3是一种有效的,选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1515.15 现货
RMB 900.36 现货
RMB 3026.07 现货
RMB 5298.93 现货
RMB 7939.67 现货
RMB 13243.23 现货
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客户使用Selleck生产的Nutlin-3发表文献68篇:

产品安全说明书

Mdm2抑制剂选择性比较

生物活性

产品描述 Nutlin-3是一种有效的,选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。
靶点
Mdm2 [5]
(Cell-free assay)
180 nM
体外研究

Nutlin-3有效抑制MDM2-p53相互作用,IC50 为 90 nM, 导致p53通路激活。Nutlin-3 处理含野生型p53的细胞,如HCT116, RKO 和SJSA-1,诱导MDM2 和p21表达, 且具有有效的抗增殖活性,IC50 为~1.5 μM, 但是作用于含突变型p53的细胞系 SW480和 MDA-MB-435没有效果。10 μM Nutlin-3处理 SJSA-1细胞48小时,显著诱导caspase依赖的细胞凋亡,凋亡达~45%。虽然Nutlin-3也抑制人皮肤 (1043SK) 和小鼠胚胎 (NIH/3T3) 的生长和活力,IC50分别为2.2 μM 和1.3 μM, 10 μM Nutlin-3处理一周后仍保留细胞活力,而3 μM Nutlin-3 处理SJSA-1细胞后,细胞则无活力。[1] Nutlin-3 不诱导p53在关键丝氨酸残基的磷酸化,在特定DNA结合序列没有区别,且与基因毒性药物Doxorubicin和Etoposide诱导的磷酸化p53相比, 使p53靶点基因转活,说明 p53 在关键丝氨酸残基的磷酸化对转录激活和凋亡是非必需的。[2] 虽然与MDM2相比,Nutlin-3 与MDMX 结合的效率低一点, Nutlin-3作用于视网膜母细胞瘤细胞(Weri1),能抑制MDMX–p53相互作用,且诱导 p53通路,IC50为0.7 μM。[3] 30 μM Nutlin-3作用于无野生型p53的细胞,也扰乱内源性p73-HDM2 相互作用,且增强p73稳定性和促凋亡活性, 导致细胞生长受抑制,和诱导凋亡。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SMMC-7721  MVrGeY5kfGmxbjDBd5NigQ>? NIL4WmEyOCEQvF2= MY[zOkBp NXe0NYt1TE2VTx?= M4P5eYRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ NYrkcZF7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 NH7lRodCeG:ydH;zbZMhSXO|YYm= NX7rTY5SOjBizszN MY[0PEBp NILjS2lFVVOR NFHsdm9qdmS3Y3XzJIFxd3C2b4Ppdy=> MknFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
SMMC-7721  MlTSRZBweHSxc3nzJGF{e2G7 NYLWdGZKOjBizszN NGTmbHg1QCCq MnrkSG1UVw>? MnjFbY5lfWOnczDhdI9xfG:|aYO= M4nB[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
HuH-7 MUnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHHZXHEyNjJ3LUKwJO69VQ>? MVKyOE81QC95MjDo MYPEUXNQ NX\nbW1lcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NHrrb5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
SMMC-7721  MlG2R4VtdCCYaXHibYxqfHliQYPzZZk> NXW3Soc{OS5{NT2yNEDPxE1? M333UlI1NzR6L{eyJIg> NXvjdXY{TE2VTx?= MUfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MnjUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
RKO NXvBSYE{TnWwY4Tpc44hSXO|YYm= NWjl[Ws4OjBizszN M1fCcFI1KGh? M2PXe4lv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NYnQdm1zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlYxODdpPkK0N|Y3ODB5PD;hQi=>
U2OS  MoTMSpVv[3Srb36gRZN{[Xl? NX7JWXY2OjBizszN M{X3U|I1KGh? M2DlVolv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NEXLVmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
RKO NXryOG9pTnWwY4Tpc44hSXO|YYm= MYWyNEDPxE1? MVWyOEBp MYDpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv MlnMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
U2OS  Ml7iSpVv[3Srb36gRZN{[Xl? NFrOfFgzOCEQvF2= M3L5T|I1KGh? NUf5fm4{cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= NHLtOZk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
MOLM NXjSeVJCTnWwY4Tpc44hSXO|YYm= NGL6S2syOCEQvF2= NWHyeWpYOjRiaB?= MXr1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5M{W2Nkc,OjR2N{O1OlI9N2F-
OCI MmXISpVv[3Srb36gRZN{[Xl? MofmNVAh|ryP MoXuNlQhcA>? MUT1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5M{W2Nkc,OjR2N{O1OlI9N2F-
BeWo M2PSW2Fxd3C2b4Ppd{BCe3OjeR?= MXezNEDDvU1? M3PjbFI1KGh? MUPpcoNz\WG|ZYOgZZBweHSxc3nz M4fSVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm4NVU1Lz5{NES5PFE2PDxxYU6=
BeWo M3v2R2Z2dmO2aX;uJGF{e2G7 MUmzNEDDvU1? MXSyOEBp MVTpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR7OEG1OEc,OjR2OUixOVQ9N2F-
MOML13 M1;YNGZ2dmO2aX;uJGF{e2G7 MV6xNO69VQ>? MUiyM|QhcA>? NYjiNY9ncW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OUe0PUc,OjR4NUm3OFk9N2F-
AML3 NFjLUWFHfW6ldHnvckBCe3OjeR?= MV6xNO69VQ>? MkfCNk81KGh? NGn1cphqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NELNXIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 M1nvW2Z2dmO2aX;uJGF{e2G7 NGfwTZAyOM7:TR?= M{DTb|IwPCCq NFHHS3dqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MknrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
MOML13 MoDhRZBweHSxc3nzJGF{e2G7 MmDNNk8yOCEQvF2= MXSyOE81QCCq M3XWXIlv\HWlZYOgZZBweHSxc3nz MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ3OUe0PUc,OjR4NUm3OFk9N2F-
AML2 MkX1RZBweHSxc3nzJGF{e2G7 MUiyM|ExKM7:TR?= NFPO[5YzPC92ODDo M{fpdYlv\HWlZYOgZZBweHSxc3nz Mo[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
U2OS  Mn\USpVv[3Srb36gRZN{[Xl? MWiyNEDPxE1? M1S5W|I1KGh? NX7UNHRucW6lcnXhd4V{KHSqZTDtVm5CKGyndnXsd{Bw\sLiQlPMNmEyNCCEQ1zYUOKh[W6mQlPMWy=> MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K1PUc,OjR6NkeyOVk9N2F-
Hep3B MX7BdI9xfG:|aYOgRZN{[Xl? MXfpcoR2[2W|IHHwc5B1d3Orcx?= NFfLZok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
Huh-7 NIXsPZlCeG:ydH;zbZMhSXO|YYm= MWPpcoR2[2W|IHHwc5B1d3Orcx?= NXn5dpozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
SMMC7721 MnnqRZBweHSxc3nzJGF{e2G7 MYDpcoR2[2W|IHHwc5B1d3Orcx?= NVi0WXRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
HepG2 MWLBdI9xfG:|aYOgRZN{[Xl? M{jJeIlv\HWlZYOgZZBweHSxc3nz NF2xZ2c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
Hep3B M4qyOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3LTGJsPzJiaB?= MlWySG1UVw>? MWHJR|UxRTJyLkG4JOKyKDFwOESg{txO Mm\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
Huh-7 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVu3NkBp NXvoZWxiTE2VTx?= Ml7mTWM2OD1|Mz65OkDDuSB|Lkmg{txO MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721/Ac M13l[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFq3PJU4OiCq MlPOSG1UVw>? Mn\ITWM2OD13NT6yNUDDuSB3LkCzJO69VQ>? NW\mVZZJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
SMMC7721 MknBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\iSVczKGh? MXXEUXNQ MlL1TWM2OD1|MT6yPEDDuSB2LkKg{txO MnnIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
HepG2/As MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3zkO|czKGh? Mn\ZSG1UVw>? NIHwVppKSzVyPU[4MlE{KMLzIEmuOkDPxE1? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
HepG2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jMTVczKGh? NGXsNFFFVVOR Ml25TWM2OD1|NT64OkDDuSB{Lkmg{txO NYriN4R7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
MOLM-13 M{\VWWZ2dmO2aX;uJGF{e2G7 MlHUOuKh|ryP MmTrOkBp NILrOYpFVVOR NVnDO4Q3\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> M1\6TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1NFgzLz5{NEi4OVA5OjxxYU6=
MOLM-13 MV3GeY5kfGmxbjDBd5NigQ>? M3rnb|bDqM7:TR?= MXWwMVghcA>? M3qxVGROW09? NXHZTFFncW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[gdFU{NCCPRF2yMEBxOjFiYX7kJIFk\XS7bHH0[YQheDV| NYLBTYE{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFUxQDJpPkK0PFg2ODh{PD;hQi=>
115 NIL6ZZZHfW6ldHnvckBCe3OjeR?= M3i5SFUh|ryP NVfsV3JiPDhiaB?= MknTSG1UVw>? NHK1[IhqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M3\ZVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 M2HTOmZ2dmO2aX;uJGF{e2G7 Mn;MOUDPxE1? MoT0OFghcA>? NUOwT2hyTE2VTx?= MWPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi NUSzVVZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
Caki-2 NVzrcWpKTnWwY4Tpc44hSXO|YYm= NVmzSmNUPSEQvF2= M{K3c|Q5KGh? NX3yOmZjTE2VTx?= NXz0O4J4cW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
ACHN M4HpRmZ2dmO2aX;uJGF{e2G7 M3HFSFUh|ryP M3juW|Q5KGh? MXXEUXNQ NEeydYJqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MmK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 NHvVbGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIi0[Yo2KM7:TR?= MVm0PEBp MUfEUXNQ NYLlXo5jcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
A498 MmXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnzOUDPxE1? M1PsbVQ5KGh? MW\EUXNQ MWDpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NXu5T3Z5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
Caki-2 M2naVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnW0OUDPxE1? MYK0PEBp MoXtSG1UVw>? M2DtOIlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NWHOTppqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
ACHN NIHCVItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVq1JO69VQ>? MnTROFghcA>? MX7EUXNQ MojObY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
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... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
MDM2 / p53 / ALKBH2 / p21 / PUMA; 

PubMed: 23258843     


CCF-STTG1 cells were treated with the MDM2 antagonist nutlin-3 (0–8 µM) for 24h before cell lysates were collected for western blotting.

RRM1 / RRM2 / p53R2 / p21 / p53 / pS6 / S6; 

PubMed: 28507282     


(A) Rh18 cells were treated with different concentrations of nutlin-3 as indicated for 24 hr. Total proteins were extracted for immunoblotting of RRM1, RRM2, γH2AX, p21, p53R2, p53, S6, pS6-235/6 and 4E-BP1. (B) Rh30 cells were treated with different concentrations of nutlin-3 as indicated for 24 hr. Total proteins were extracted for immunoblotting of RRM1, RRM2, γH2AX, p21, p53R2, p53, S6, pS6-235/6 and 4E-BP1. GAPDH and Actin served as loading controls.

23258843 28507282
Immunofluorescence
Lamin A / Lamin C / p16 / H3K9me3; 

PubMed: 30728349     


c Immunofluorescence images of nuclear deformation and p16 expression after Nutlin-3 treatment for different time period. HCT p53+/− cells were treated with Nutlin-3 (1 μM) for different time (24, 48 h). After treatment, cells were subjected to immunofluorescence staining for Lamin A/C (Red), p16 (Green), and counterstained with DAPI (Blue). dImmunofluorescence images of nuclear deformation and decreased expression of H3K9me3 in HCT p53+/− cells (left). Counting of histone H3K9me3-positive cells (middle) and signal intensities (right) on the basis of IF staining. HCT p53+/− cells were treated with Nutlin-3 (1 μM) for different time (24, 48 h). After treatment, cells were IF stained with Lamin A/C (Red), H3K9me3 (Green), and counterstained with DAPI (Blue). *P < 0.05. 

Merlin / cyclin D1 / p53 / MDM2; 

PubMed: 30274821     


The changes in the subcellular localization of proteins in response to Nutlin-3. Nuclear merlin was indicated with white arrows. Scale bar = 50 μm.

p53; 

PubMed: 24286312     


The subcellular localization of p53 was detected under immunofluorescence microscope (1,000×). The cells were treated as indicated and stained for p53 (red). Nuclei were counterstained with DAPI (blue).

30728349 30274821 24286312
Growth inhibition assay
Cell viability; 

PubMed: 29286113     


Inhibitory effect of nutlin-3 for the cell proliferation after cultivate cells at different concentration for three times (24, 48 and 72 h), respectively.

29286113
体内研究 Nutlin-3 按200 mg/kg 剂量口服处理,每天两次,持续3周,显著抑制SJAS-1移植瘤生长,抑制达90%, 而Doxorubicin抑制81%肿瘤生长。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

Biacore 研究:

在Biacore S51上进行竞争性实验。衍生一系列S传感器芯片CM5,用于固定 PentaHis抗体,为了捕获 His-标记的p53。捕获的水平为~200反应单位(1 反应单位对应于1 pg 蛋白/ mm2)。MDM2蛋白浓度一直维持在300 nM。Nutlin-3 溶于DMSO,浓度为10 mM,然后进一步稀释,在每个MDM2实验样本中产生系列浓度的Nutlin-3。在电泳缓冲液(10 mM Hepes,0.15 M NaCl, 2% DMSO)中25oC下进行实验。在Nutlin-3存在时,计算MDM2-p53结合情况,作为结合百分数, 使用Microsoft Excel计算IC50。
细胞实验:

[1]

- 合并
  • Cell lines: HCT116, RKO, SJSA-1, SW480, 和 MDA-MB-435
  • Concentrations: 溶于DMSO,终浓度为~ 30 μM
  • Incubation Time: 8, 24, 和 48 小时
  • Method:

    使用不同浓度Nutlin-3处理细胞8, 24和 48 小时。通过实时PCR分析p21 和MDM2基因转录水平,通过Western Blotting分析蛋白水平。通过MTT实验测定细胞活力。 通过末端脱氧核苷酸转移酶调节的脱氧尿苷三磷酸缺口末端标记法(TUNEL)染色,使用流式细胞仪和荧光显微镜测定细胞凋亡。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 皮下注射 SJSA-1细胞的雌性无胸腺Nu/Nu-nuBR裸鼠
  • Dosages: 200 mg/kg
  • Administration: 口服处理,每天两次
    (Only for Reference)

溶解度 (25°C)

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

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 581.5
化学式

C30H30Cl2N4O4

CAS号 890090-75-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

相关Mdm2产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID