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 1407.13 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59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  NGezTmRHfW6ldHnvckBCe3OjeR?= MW[xNEDPxE1? M3nz[|M3KGh? MVXEUXNQ MYjkc5dvNXKnZ4XsZZRmeyC2aHWgdJJwfGWrbjDlfJBz\XO|aX;uJIxmfmWuIH;mJJBpd3OyaH:tV4VzOzl{LYC1Ny=> NFP4dHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
HuH-7 MnizRZBweHSxc3nzJGF{e2G7 NX7tbJl7OjBizszN MYe0PEBp Mm\2SG1UVw>? NWrBTJFEcW6mdXPld{BieG:ydH;zbZM> NHn4dXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK4OlMyOid-MkSyPFY{OTJ:L3G+
SMMC-7721  NEjlVVZCeG:ydH;zbZMhSXO|YYm= MXmyNEDPxE1? M1LXcFQ5KGh? NHzpXGhFVVOR MYfpcoR2[2W|IHHwc5B1d3Orcx?= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 NXm2NVZWS2WubDDWbYFjcWyrdImgRZN{[Xl? MWOxMlI2NTJyIN88US=> MUmyOE81QC95MjDo NHnC[XNFVVOR NXLCPXRQcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGSxc3WgZY5lKHSrbXWg[IVx\W6mZX70cJk> NXmzUXh[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
SMMC-7721  MXvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mn3QNU4zPS1{MDFOwG0> MVuyOE81QC95MjDo MXrEUXNQ MX;pcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= MnjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
RKO NYD4cXNqTnWwY4Tpc44hSXO|YYm= MnTQNlAh|ryP MlThNlQhcA>? M3:5d4lv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NIXUXmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  M2HsNmZ2dmO2aX;uJGF{e2G7 NVX1VHByOjBizszN MUGyOEBp MnrCbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= NXq3VJB2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzOlYxODdpPkK0N|Y3ODB5PD;hQi=>
RKO MlvoSpVv[3Srb36gRZN{[Xl? NG\JNlAzOCEQvF2= MkfMNlQhcA>? NGLBfY5qdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MojFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
U2OS  MnfNSpVv[3Srb36gRZN{[Xl? NW\jdlZtOjBizszN M3TINVI1KGh? M1jvRolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? NHvq[o49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
MOLM NF;aZXFHfW6ldHnvckBCe3OjeR?= NHq0WGsyOCEQvF2= M4X4WlI1KGh? MmTSeZBz\We3bHH0[ZMhfGinIGPPR3MuOSCneIDy[ZN{cW:w M{W4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEezOVYzLz5{NES3N|U3OjxxYU6=
OCI MmHrSpVv[3Srb36gRZN{[Xl? MonvNVAh|ryP M361blI1KGh? NIDic4x2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= MkG4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
BeWo NGXTc29CeG:ydH;zbZMhSXO|YYm= NUHGSGdrOzBiwsXN Mne3NlQhcA>? MkD2bY5kemWjc3XzJIFxd3C2b4Ppdy=> NVXDSoU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVgyPTRpPkK0OFk5OTV2PD;hQi=>
BeWo MlXuSpVv[3Srb36gRZN{[Xl? M37PTVMxKML3TR?= M3jISFI1KGh? MVjpcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= M3vPbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm4NVU1Lz5{NES5PFE2PDxxYU6=
MOML13 MnHUSpVv[3Srb36gRZN{[Xl? NWXLUGV4OTEQvF2= M2nCT|IwPCCq MlWwbY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= NU\wVW93RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML3 NXfJZVdITnWwY4Tpc44hSXO|YYm= NVnHV5VXOTEQvF2= NIXHPWUzNzRiaB?= NHzPVZNqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NEDSVIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 MlXjSpVv[3Srb36gRZN{[Xl? Mk\PNVDPxE1? M{DEbFIwPCCq NUXxeJgycW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> MlqyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
MOML13 Mm\MRZBweHSxc3nzJGF{e2G7 NYn6V3d1Oi9zMDFOwG0> NF3mWI0zPC92ODDo NFXoWoNqdmS3Y3XzJIFxd3C2b4Ppdy=> NXflR5dORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2OVk4PDlpPkK0OlU6PzR7PD;hQi=>
AML2 MYHBdI9xfG:|aYOgRZN{[Xl? MnqyNk8yOCEQvF2= NYniSXAxOjRxNEigbC=> NX;WXYdTcW6mdXPld{BieG:ydH;zbZM> NFrY[mU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
U2OS  NIXRcIFHfW6ldHnvckBCe3OjeR?= NUnme3ZmOjBizszN M1T5N|I1KGh? MoDGbY5kemWjc3XzJJRp\SCvUl7BJIxmfmWuczDv[uKhSkOOMlGxMEBDS0y[TNMgZY5lSkOOVx?= MnG3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6NkeyOVkoRjJ2OE[3NlU6RC:jPh?=
Hep3B M2jzRmFxd3C2b4Ppd{BCe3OjeR?= Mn3PbY5lfWOnczDhdI9xfG:|aYO= NYDn[|FKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
Huh-7 MYLBdI9xfG:|aYOgRZN{[Xl? MWPpcoR2[2W|IHHwc5B1d3Orcx?= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
SMMC7721 NX\zd5dNSXCxcITvd4l{KEG|c3H5 MlT3bY5lfWOnczDhdI9xfG:|aYO= NWHtVZkxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
HepG2 MVLBdI9xfG:|aYOgRZN{[Xl? NGnrTmtqdmS3Y3XzJIFxd3C2b4Ppdy=> MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Hep3B MonhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvKO|IhcA>? Mo\DSG1UVw>? M3PaO2lEPTB;MkCuNVghyrFiMT64OEDPxE1? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Huh-7 M37jUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nsUFczKGh? NXL3dlZwTE2VTx?= MWnJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> MmDuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
SMMC7721/Ac MnS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrT[nE4OiCq M4HPOWROW09? NIfpeYJKSzVyPUW1MlIyKMLzIEWuNFMh|ryP M{fGPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
SMMC7721 MoHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;DO|IhcA>? NELrS|RFVVOR M2nBbmlEPTB;M{GuNlghyrFiND6yJO69VQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
HepG2/As NUezVmVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWK3NkBp MnfXSG1UVw>? NF\JNWJKSzVyPU[4MlE{KMLzIEmuOkDPxE1? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
HepG2 NFX1UGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTmeFU4OiCq NFOxSFVFVVOR MV7JR|UxRTN3Lki2JOKyKDJwOTFOwG0> NUHmUFV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
MOLM-13 MmjuSpVv[3Srb36gRZN{[Xl? MYq2xsDPxE1? MYW2JIg> MlnTSG1UVw>? M3G5SYVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= M2TaSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1NFgzLz5{NEi4OVA5OjxxYU6=
MOLM-13 MXXGeY5kfGmxbjDBd5NigQ>? NEnweoU3yqEQvF2= NIXtXYMxNThiaB?= NFPsUY5FVVOR MXPpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> NG\1Xmw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OVA5Oid-MkS4PFUxQDJ:L3G+
115 NFTTPZFHfW6ldHnvckBCe3OjeR?= NHjDO|I2KM7:TR?= M1\MV|Q5KGh? NXvJb5pZTE2VTx?= Ml3KbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NInHNnc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
A498 MnrUSpVv[3Srb36gRZN{[Xl? MYe1JO69VQ>? MkXyOFghcA>? MkfDSG1UVw>? NY\FSJpvcW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> M4Tk[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
Caki-2 MlTOSpVv[3Srb36gRZN{[Xl? Mn7ROUDPxE1? MnT4OFghcA>? M2jIS2ROW09? MVjpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M2[0[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
ACHN MUTGeY5kfGmxbjDBd5NigQ>? MXq1JO69VQ>? NE\abpc1QCCq MYPEUXNQ Ml[zbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M2rWUFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
115 M1fySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVS1JO69VQ>? MW[0PEBp MlGwSG1UVw>? NEPsfYtqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NELq[pg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
A498 M33WTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWK1JO69VQ>? MljNOFghcA>? MWLEUXNQ M1Lh[Ilv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NWDpPVRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
Caki-2 NYPHco1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\lV|c2KM7:TR?= NGDkUIQ1QCCq NHnvSGpFVVOR MljRbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg NIHnVVg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
ACHN M{DxUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm1JO69VQ>? NGTXblI1QCCq M3rMUWROW09? M2jwb4lv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> NYKzUZFpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
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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、MSDS / 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、MSDS / 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