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65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  Mli0SpVv[3Srb36gRZN{[Xl? MnrlNVAh|ryP NV\GN3RpOzZiaB?= NXj5XWZxTE2VTx?= NWixV2lY\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NWHCTJNwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 M4npNWFxd3C2b4Ppd{BCe3OjeR?= NEHN[FIzOCEQvF2= M2njblQ5KGh? M3TSUmROW09? MnPQbY5lfWOnczDhdI9xfG:|aYO= MlHiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
SMMC-7721  NEnQTpFCeG:ydH;zbZMhSXO|YYm= Mni3NlAh|ryP M3j6WFQ5KGh? M{foPWROW09? MlHFbY5lfWOnczDhdI9xfG:|aYO= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 NHnaVnVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MUWxMlI2NTJyIN88US=> NVq3SmdsOjRxNEivO|IhcA>? M2HFNWROW09? M2G1WYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 MlXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
SMMC-7721  MlvNR4VtdCCYaXHibYxqfHliQYPzZZk> M1vkV|EvOjVvMkCg{txO NGHkcnUzPC92OD:3NkBp MXLEUXNQ MUTpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36g[I9{\SCjbnSgeIlu\SCmZYDlcoRmdnSueR?= M1PZNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mki2N|EzLz5{NEK4OlMyOjxxYU6=
RKO MlzSSpVv[3Srb36gRZN{[Xl? NEXl[GozOCEQvF2= NWDIdWxwOjRiaB?= MWPpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= NIjReZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  M4Hk[2Z2dmO2aX;uJGF{e2G7 MnPwNlAh|ryP NVPzR5V7OjRiaB?= M2THS4lv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u NFnQclA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
RKO MoD3SpVv[3Srb36gRZN{[Xl? MlnUNlAh|ryP NXTpT5l4OjRiaB?= MYrpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv NFqyT2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  MoXaSpVv[3Srb36gRZN{[Xl? NF3OW5kzOCEQvF2= NXX4UHZwOjRiaB?= Mnv0bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJGhQNTFicILveIVqdiCjczD3[YxtKGG|IITo[UBxPTNicILveIVqdg>? MkPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
MOLM NVe1XFhbTnWwY4Tpc44hSXO|YYm= NYXicYdxOTBizszN NHXtd4YzPCCq M1LnOpVxemWpdXzheIV{KHSqZTDTU2NUNTFiZYjwdoV{e2mxbh?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDR5M{W2Nkc,OjR2N{O1OlI9N2F-
OCI MlvTSpVv[3Srb36gRZN{[Xl? NXu4VFVrOTBizszN MlLXNlQhcA>? NVXXVZpDfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NXn3VVFkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O|M2PjJpPkK0OFc{PTZ{PD;hQi=>
BeWo MVLBdI9xfG:|aYOgRZN{[Xl? M4DrelMxKML3TR?= NFjybnIzPCCq M17OUIlv[3KnYYPld{BieG:ydH;zbZM> M1jEUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm4NVU1Lz5{NES5PFE2PDxxYU6=
BeWo M3G0Z2Z2dmO2aX;uJGF{e2G7 M37VUFMxKML3TR?= MmG0NlQhcA>? NYjsd|Z3cW6lcnXhd4V{KHB3MzygUYRuOixicEKxJIFv\CCSdX3hJIF1KHSqZTDwdo91\WmwIHzleoVt MmC1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2OUixOVQoRjJ2NEm4NVU1RC:jPh?=
MOML13 M2\JRmZ2dmO2aX;uJGF{e2G7 MWmxNO69VQ>? Mk\ONk81KGh? MYXpcoNz\WG|ZYOgeIhmKGyndnXsJI9nKHB3Mx?= M2LncFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NkW5O|Q6Lz5{NE[1PVc1QTxxYU6=
AML3 M1;JOGZ2dmO2aX;uJGF{e2G7 MnO2NVDPxE1? MofFNk81KGh? NHLPT4RqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NFz0eHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 MVXGeY5kfGmxbjDBd5NigQ>? M4T3N|Ex|ryP NYrONW9JOi92IHi= MkS5bY5kemWjc3XzJJRp\SCuZY\lcEBw\iCyNUO= MlT5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
MOML13 M3jpPGFxd3C2b4Ppd{BCe3OjeR?= NVHxfHREOi9zMDFOwG0> MmX6NlQwPDhiaB?= MkfTbY5lfWOnczDhdI9xfG:|aYO= MlW5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
AML2 MUHBdI9xfG:|aYOgRZN{[Xl? NW\kXmhROi9zMDFOwG0> NWK3T3JYOjRxNEigbC=> MlnSbY5lfWOnczDhdI9xfG:|aYO= NELHUmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
U2OS  NUPEO|ZITnWwY4Tpc44hSXO|YYm= NEe4[FEzOCEQvF2= MUSyOEBp NFy2WHBqdmO{ZXHz[ZMhfGinIH3SUmEhdGW4ZXzzJI9nyqCEQ1yyRVEtKEKFTGjMxsBidmSEQ1zX MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K1PUc,OjR6NkeyOVk9N2F-
Hep3B M4jLSWFxd3C2b4Ppd{BCe3OjeR?= NFS1NJlqdmS3Y3XzJIFxd3C2b4Ppdy=> NFz5UlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
Huh-7 M1XWTWFxd3C2b4Ppd{BCe3OjeR?= MoHlbY5lfWOnczDhdI9xfG:|aYO= NXjJdW9{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
SMMC7721 MXnBdI9xfG:|aYOgRZN{[Xl? NWjxOFFGcW6mdXPld{BieG:ydH;zbZM> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
HepG2 NX7hS5FTSXCxcITvd4l{KEG|c3H5 MnLZbY5lfWOnczDhdI9xfG:|aYO= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Hep3B MnTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEG0SnA4OiCq NXPkfnhVTE2VTx?= NXHjeXpDUUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Huh-7 M3y3cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TvNVczKGh? M1v5bGROW09? MWLJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> M1Htd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
SMMC7721/Ac MkfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:3NkBp NHPGUlRFVVOR NUTiemhmUUN3ME21OU4zOSEEsTC1MlA{KM7:TR?= MkXCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
SMMC7721 MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1\uXlczKGh? Mk\QSG1UVw>? MnruTWM2OD1|MT6yPEDDuSB2LkKg{txO NXTvWIQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
HepG2/As M1qxUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUO3NkBp NHTieWlFVVOR MYnJR|UxRTZ6LkGzJOKyKDlwNjFOwG0> NELFbZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
HepG2 NXjyPFVET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVT6SGx7PzJiaB?= MYrEUXNQ MVLJR|UxRTN3Lki2JOKyKDJwOTFOwG0> M1H5WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
MOLM-13 MXPGeY5kfGmxbjDBd5NigQ>? NG\LXFg3yqEQvF2= NGjNdlE3KGh? MYLEUXNQ M1fEZoVvcGGwY3XzJJRp\SCjY3X0fYxifGmxbjDv[kBpcXO2b37lJGgzSiCjbnSgbIVifCC|aH;jb{Bxem:2ZXnud{BJe3B{NzDhcoQhUHOyOUC= NVz6UYNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFUxQDJpPkK0PFg2ODh{PD;hQi=>
MOLM-13 M1S4WmZ2dmO2aX;uJGF{e2G7 NIXzXFg3yqEQvF2= M1fkRVAuQCCq MkKySG1UVw>? NFvlR5FqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjDwOVMtKE2GTUKsJJAzOSCjbnSgZYNmfHmuYYTl[EBxPTN? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NUC4Nkc,OjR6OEWwPFI9N2F-
115 NEX2WlRHfW6ldHnvckBCe3OjeR?= NFXjfGo2KM7:TR?= NXnLeppiPDhiaB?= M3vmfWROW09? MWPpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi M3vKSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[3O|g4Lz5{NUC2O|c5PzxxYU6=
A498 NXHjdW9tTnWwY4Tpc44hSXO|YYm= NYLDSoh1PSEQvF2= NFTqeJg1QCCq M4\4VWROW09? NGThfmZqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
Caki-2 MVXGeY5kfGmxbjDBd5NigQ>? M4rCW|Uh|ryP M4\HSFQ5KGh? MV7EUXNQ NU\vSVQ1cW6mdXPld{BxPTNvZHXw[Y5l\W62IIPlcoV{[2WwY3ZCpC=> NEHXVFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
ACHN MnftSpVv[3Srb36gRZN{[Xl? MXK1JO69VQ>? Mn;kOFghcA>? NFrmTGJFVVOR MULpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MlnNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
115 MkLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn:yOUDPxE1? NGK1Zok1QCCq NVnoUHNETE2VTx?= M{fPPYlv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
A498 Mnj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;Ve|Uh|ryP NELheHA1QCCq MVPEUXNQ NV;IbXFRcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MnS5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNke3PFcoRjJ3ME[3O|g4RC:jPh?=
Caki-2 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVy1JO69VQ>? NVHQO25MPDhiaB?= NE[zSGNFVVOR NIf0WnFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NFTRVZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
ACHN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH6yO2U2KM7:TR?= NFLhV5E1QCCq MnHiSG1UVw>? NF3pd4hqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NUHHT5Q4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
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Lovo  NFfaXIJHfW6ldHnvckBCe3OjeR?= M2f6O|UwOTBxMkCg{txO NUX3dplvOjRiaB?= MoXFeZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NWS5Z3RURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxN|YyPDdpPkK0NVM3OTR5PD;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