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48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
MCF7 NHXkdFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe0eo02yqEQvF2= M{jle|Q5yqCq MoDlZoxw[2u|IEK3MW9JSy2rbnT1Z4VlKGOnbHygdJJwdGmoZYLheIlwdiClb33wZZJi[mynIITvJJRp[XRib3[gZoF{[WxibHX2[Yx{ MkTSNlY{PTB3NkW=
NP69 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\STWM2OD1|MT62PeKyOi53NDFOwG0> NIXYNpQzPjJ3MkW3OS=>
NP460 NEHDRVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTJ{Lki1xtEyNjF6IN88US=> M1T3blI3OjV{NUe1
C666-1 Mkj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTF7Lkm1xtE5Njl|IN88US=> NEfPV3ozPjJ3MkW3OS=>
C666-1 NITWTYZE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NY\y[o5sOTBiwsXN M1z4S|Q5KGh? NGjNUGxFVVOR NF;oSFZ{\W6|aYTpfoV{KEN4Nk[tNUBk\WyuczD0c{B1cGViY4n0c5RwgGmlIHXm[oVkfCCxZjDjbZNxdGG2aX6= M2XNWFI3OjV{NUe1
C666-1  NU[5epJbTnWwY4Tpc44hSXO|YYm= MonPNVAhyrWP MV:yOEBp NXr2OnVjTE2VTx?= NVHJUZNW[WO2aY\heIV{KHSqZTDwOVMheGG2aIfhfUwhfXC{ZXf1cIF1cW6pIIC1N{wheDJzIHHu[EBO\G1{ NWCydoxZOjZ{NUK1O|U>
C666-1 M{jIVWFxd3C2b4Ppd{BCe3OjeR?= M3LxPFExKML3TR?= MXi0PE84OiCq M1TWSmROW09? M4HodZNmdnOrdHn6[ZMhSzZ4Nj2xJINmdGy|IITvJINqe3CuYYTpck1qdmS3Y3XkJIFxd3C2b4Ppdy=> NInKVIIzPjJ3MkW3OS=>
A549 M4nQbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XKbVI1KGh? NVra[ZhxUUN3ME2xO{43QCEEsTC0MlUzKM7:TR?= M1fBTFI3OTJ3MkOw
A549-NTC MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoP3NlQhcA>? NGHYOmRKSzVyPUG5MlQzKMLzIEGuPVYh|ryP M1;XdlI3OTJ3MkOw
A549-920 M3W2dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPmUWFmOjRiaB?= NGXlXlNKSzVyPUOzMlg2KMLzIESuPFQh|ryP Mkn5NlYyOjV{M{C=
CRL-5908 NUW4VoZYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV[yOEBp NF;ET3BKSzVyPUO4MlcyKMLzIEKuOFMh|ryP M3r6OlI3OTJ3MkOw
L6 NWnXc5V6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfGS|ZEOTEEoN88UeKh NHv5[FQzPC92OD:3NkBp M13l[2ROW09? NVjZU2g{cW6qaXLpeJMh[2WubIOgdJJwdGmoZYLheIlwdiCjbnSg[Iln\mW{ZX70bYF1cW:w M{G5VlI2QDdzN{m0
C2C12 NEHNeJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWqxNOKh|ryPwrC= NH63c4QzPC92OD:3NkBp M33SR2ROW09? NFTZOGlqdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? NV\1eotGOjV6N{G3PVQ>
MCF-7  M3\GO2Z2dmO2aX;uJGF{e2G7 NV\DPHdMOTEEoN88US=> Mlj6SG1UVw>? NWPnNmlRcW6qaXLpeJMh[3mlbHnuJGQyKGGwZDDEbYNmesLi NH3BeVYzPTdyMkewNy=>
DU4475  MmXRSpVv[3Srb36gRZN{[Xl? MYC1M|ExNzJyIN88US=> MljzNlTDqGh? NH7sRYRld3ewcnXneYxifGW|IGTvZ4EuOSCmb4PlJIRmeGWwZHXueIx6 M1XkblI2PTR5MUe0
SMMC-7721 M4rUVWZ2dmO2aX;uJGF{e2G7 MmHBNVAh|ryP M2qxb|Q5KGh? MoiySG1UVw>? M1juc4NifXOnczDEUmEhTFOEIHThcYFo\Q>? MnLONlU2PDR|NkG=
SMMC-7721 M17qUGZ2dmO2aX;uJGF{e2G7 MYOxNEDPxE1? M3PPWFQ5KGh? M{\zeGROW09? MXLpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg MYqyOVU1PDN4MR?=
SMMC-7721 NEjtSoZHfW6ldHnvckBCe3OjeR?= MXWxNEDPxE1? M1vqUVQ5KGh? NXH3WphWTE2VTx?= Mn\CbY5kemWjc3XzJJRp\SCneIDy[ZN{cW:wIHzleoVtKG:owrDJSm5DOcLibWLORS=> NYfTZWFoOjV3NESzOlE>
SMMC-7721 NXW3XmxrTnWwY4Tpc44hSXO|YYm= MorJNVAh|ryP Mmr0N|YhcA>? MYTEUXNQ MWnjZZV{\XNidHjlJIVkfG:yaXOg[ZhxemW|c3nvckBw\iCLRlmxOi=> NU\yWnRFOjV3NESzOlE>
MCF-7 MUPGeY5kfGmxbjDBd5NigQ>? NVLMbW9IOTEEoN88US=> NIKxZZExNTJ2IHi= NYjwcow3cW6mdXPld{BxPTNiYX7kJJAzOS:FaYCx NFy0UZMzPTR6MkO3Ny=>
OVCAR10 NHfrfXhHfW6ldHnvckBCe3OjeR?= NHPwOIEyOMLizszN M4nhTVIycMLi M2XNb2ROW09? NWfxRYlQcW6lcnXhd4V{KHB3MzDwdo91\WmwIHzleoVtew>? NVj6RppOOjV2Mk[1OFg>
NCI-H23 M2DwNGZ2dmO2aX;uJGF{e2G7 M4nBb|ExyqEQvF2= M3G0TVIycMLi NVq2VopqTE2VTx?= M4HyRYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> M4jNdFI2PDJ4NUS4
A2780 NV;QbVNITnWwY4Tpc44hSXO|YYm= M{DwVVExyqEQvF2= MWqyNYjDqA>? NFXBfmhFVVOR NHPIcIlqdmO{ZXHz[ZMheDV|IIDyc5RmcW5ibHX2[Yx{ NY\VT29{OjV2Mk[1OFg>
NCI-H23 MVvGeY5kfGmxbjDBd5NigQ>? M4qwPVExyqEQvF2= Mly0NlFpyqB? M{LHb2ROW09? MX7k[YNz\WG|ZYOgeIhmKE[xeF2xJIxmfmWucx?= NW\wXVlIOjV2Mk[1OFg>
A2780 NWfjTpY{TnWwY4Tpc44hSXO|YYm= NGr5UWwyOMLizszN MnvYNlFpyqB? MWPEUXNQ NFPTZYJl\WO{ZXHz[ZMhfGinIF\vfG0yKGyndnXsdy=> NFG0bmYzPTR{NkW0PC=>
HCT116  M{LBN2Z2dmO2aX;uJGF{e2G7 NX7ZdItqOTBiwsXN MVeyOEBp MnTFZ4F2e2W|IHGgdFU{NWSncHXu[IVvfCC2ZYTyZZBtd2mmIFexMYFzemW|dDDpckBlcXCub3nkJGhEXDFzNjDjcI9v\XNiREOgZY5lKER6 NXOzOYd1OjV|OECwOVU>
MCF-10CA1a NUHROml{TnWwY4Tpc44hSXO|YYm= NH7ibHEyOMLizszN MUi0PEBp NEPl[llFVVOR MknrbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? MVSyOVI2Pzd{OR?=
MCF-10A1  NXfOclhHTnWwY4Tpc44hSXO|YYm= NIP2SowyOMLizszN MXSyOE81QCCq MkTkSG1UVw>? NXXqUZpvcW6qaXLpeJMhdWmpcnH0bY9vKG:oIH7vdo1idCCkcnXhd5Qh\XCrdHjlcIlidMLi Mm\LNlUzPTd5Mkm=
MCF-10CA1a M3uwSmZ2dmO2aX;uJGF{e2G7 Mm\jNVDDqM7:TR?= NXi2W3B4OjRiaB?= NVrufno5TE2VTx?= MoDI[IVkemWjc3XzJJRp\SCWR1[t{tI{NWmwZIXj[YQhdVKQQTDs[ZZmdHNib3\NUXAzNMLiTV3QPUwh[W6mwrDpcpRm\3KrbtMg{tLDqDN? NFT0NpozPTJ3N{eyPS=>
MCF-10CA1a Ml\oSpVv[3Srb36gRZN{[Xl? MnPNNVDDqM7:TR?= M4XwOFI1KGh? NWPWTVNQTE2VTx?= M4TGeYlvcGmkaYTzJEBVT0ZvzsKzMYlv\HWlZXSgSXBJSjMEoH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbh?= M1;3XVI2OjV5N{K5
SK-BR-7 NYTTbJV6TnWwY4Tpc44hSXO|YYm= NWraVJA4OTEEoN88US=> NH31eYczPCCq MmTXSG1UVw>? NILtW5ZqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= NV61NFFpOjV{NUe3Nlk>
SUM102PT MULGeY5kfGmxbjDBd5NigQ>? NELiVlQyOMLizszN MWSyOEBp M4LBTGROW09? NXX3WItNcW6qaXLpeJMhKFSJRj5OtlMucW6mdXPl[EBGWEiEMtMgcXJPSSCjbnSgdJJwfGWrbjDlfJBz\XO|aX;u NYHQN2tIOjV{NUe3Nlk>
RAW 264.7 M4jyRmZ2dmO2aX;uJGF{e2G7 MWCxNOKh|ryP MoX4N|AhdWmw M121dZBz\X[nboTzJJRp\SCyNUOgdoVlfWO2aX;uJIlvKHKnc4DvcpNmKHSxIFzQVy=> NEP3b44zPTF5MkW0Oy=>
RAW 264.7 M3iwVWZ2dmO2aX;uJGF{e2G7 M1WzNFExyqEQvF2= Ml7ZN|AhdWmw MmPXdoVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NULTZmNNOjVzN{K1OFc>
RAW 264.7 MXXGeY5kfGmxbjDBd5NigQ>? NVT3V49ROTEEoN88US=> NXv3bHFJOzBibXnu M{Ta[IlvcGmkaYTzJGxRWy2rbnT1Z4VlKE6RIIDyc4R2[3Srb39CpC=> MYOyOVE4OjV2Nx?=
MCF7  M4[wNGNmdGxiVnnhZoltcXS7IFHzd4F6 NUPVOXFKOi53INM1US=> NV7IbVdRPSCm NHf4W|ZFVVOR NFjBWFZ{\W6|aYTpfoV{KE2FRkegeI8hWEGUUDDpcohq[mm2aX;u MWKyOVA5PTlyMh?=
MCF7  NV7BfW9UTnWwY4Tpc44hSXO|YYm= M2\UWFIvPSEEtV2= MnrqOFghcA>? NHXlZWZFVVOR Mo\J[IVkemWjc3XzJJRp\SCqb33vcI9od3W|IFTTRkBz\XCjaYKg[pJmeXWnbnPp[ZM> NXfSVm5ZOjVyOEW5NFI>
ACHN NYS2dJl5S2WubDDWbYFjcWyrdImgRZN{[Xl? NYHWN4FIOC53LUGwJO69VQ>? M2rZSVAuPiCm NEP2cFFFVVOR NGDlfIRqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NHfLXVEzPTB4N{e4Oy=>
Caki-2 NGTwZ3hE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFzOV|QxNjVvMUCg{txO NIH0OIsxNTZiZB?= NUPsb2psTE2VTx?= NHHTdXBqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ MmjnNlUxPjd5OEe=
A498 NVfxPIxRS2WubDDWbYFjcWyrdImgRZN{[Xl? MlXDNE42NTFyIN88US=> M4HGVlAuPiCm MYnEUXNQ NIj1SJJqdmirYnn0d{Bxem:uaX\ldoF1cW:wIHnuJIEh\G:|ZT3k[ZBmdmSnboSgcYFvdmW{ NYPS[HFKOjVyNke3PFc>
115 M1rCe2NmdGxiVnnhZoltcXS7IFHzd4F6 NUfpVmtTOC53LUGwJO69VQ>? M3WySVAuPiCm Mme3SG1UVw>? MXTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NG\v[ZczPTB4N{e4Oy=>
117 M{H3PGNmdGxiVnnhZoltcXS7IFHzd4F6 MUCwMlUuOTBizszN M2D5flAuPiCm MnjKSG1UVw>? MlzYbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{W0elI2ODZ5N{i3
ACHN NYX6WpdwTnWwY4Tpc44hSXO|YYm= NXThdI52OC53L{GvOUDPxE1? M3zS[lQ5KGh? NGHS[HdFVVOR NULhS3BJdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NFKwXHQzPTB4N{e4Oy=>
Caki-2 Mk[1SpVv[3Srb36gRZN{[Xl? MYmwMlUwOS93IN88US=> NGC5PZg1QCCq NEjieZdFVVOR MXrs[YFleyC2bzDpcoNz\WG|ZXSg[ZhxemW|c3nvckBw\iCyNUOgZY5lKHOxbXWgdFU{KHSjcnfleEBo\W6nc{qgUWROOixiYX7kJJAzOQ>? Ml3yNlUxPjd5OEe=
A498 Ml;WSpVv[3Srb36gRZN{[Xl? M{H4fVAvPS9zL{Wg{txO M1nMVFQ5KGh? NViwfYRMTE2VTx?= NGT1RVRt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NFfRZYEzPTB4N{e4Oy=>
115 NIHtdXNHfW6ldHnvckBCe3OjeR?= MnK2NE42NzFxNTFOwG0> MmTKOFghcA>? MnLLSG1UVw>? NVjWTIR{dGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NUHjUY5zOjVyNke3PFc>
ACHN NG\SdYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:x[pk2KM7:TR?= MmLSOFghcA>? NVS1RnQzTE2VTx?= NH;UZ2NqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NXvpZVlpOjVyNke3PFc>
Caki-2 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjzUXJ6PSEQvF2= MkLsOFghcA>? M3u0bmROW09? NWjOU4s2cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NVTVd|JXOjVyNke3PFc>
A498 M2r6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVG1JO69VQ>? MY[0PEBp NXPuTm4xTE2VTx?= MnTibY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg M3jhc|I2ODZ5N{i3
115 NX[0RYdTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\WS|Uh|ryP MYq0PEBp NXrtNI9rTE2VTx?= NGD0SXFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> Mn3lNlUxPjd5OEe=
ACHN MkXPSpVv[3Srb36gRZN{[Xl? NXnSNpJPPSEQvF2= MlP5OFghcA>? MV3EUXNQ MnzibY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= M2XiWVI2ODZ5N{i3
Caki-2 M1nOUWZ2dmO2aX;uJGF{e2G7 NXzHPXJqPSEQvF2= MVy0PEBp Mn\KSG1UVw>? NHe1ZlFqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg M1LqTFI2ODZ5N{i3
A498 MkHGSpVv[3Srb36gRZN{[Xl? MkDoOUDPxE1? MXq0PEBp NUHjbpJETE2VTx?= M4fzSYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= MoTaNlUxPjd5OEe=
115 M3zmNGZ2dmO2aX;uJGF{e2G7 M4jqXVUh|ryP MW[0PEBp MnzpSG1UVw>? MUTpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MXiyOVA3Pzd6Nx?=
MOLM-13 MVXGeY5kfGmxbjDBd5NigQ>? NEfGcIM3yqEQvF2= NFHi[HMxNThiaB?= M{LoZmROW09? M13Hcolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIIC1N{whVUSPMjygdFIyKGGwZDDhZ4V1gWyjdHXkJJA2Ow>? NVLlV2hiOjR6OEWwPFI>
MOLM-13 MkC0SpVv[3Srb36gRZN{[Xl? NF;sd243yqEQvF2= M1TSVVYhcA>? NVrWSJNITE2VTx?= NGL5OGtmdmijbnPld{B1cGViYXPleJlt[XSrb36gc4YhcGm|dH;u[UBJOkJiYX7kJIhm[XRic3jvZ4sheHKxdHXpcpMhUHOyMkegZY5lKEi|cEmw MVmyOFg5PTB6Mh?=
HepG2 M3;2fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPsOng4OiCq NV\tVGpGTE2VTx?= NX3oeGhuUUN3ME2zOU45PiEEsTCyMlkh|ryP MYGyOFg5PDhyOR?=
HepG2/As NXTKc45qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\N[4hoPzJiaB?= NVHkcm5VTE2VTx?= NHnObFVKSzVyPU[4MlE{KMLzIEmuOkDPxE1? M37ze|I1QDh2OEC5
SMMC7721 M1XsSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYLWUoxtPzJiaB?= M2TIZWROW09? MlvnTWM2OD1|MT6yPEDDuSB2LkKg{txO MWSyOFg5PDhyOR?=
SMMC7721/Ac NH\JfVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\5bFczKGh? NIO0VXFFVVOR MXjJR|UxRTV3LkKxJOKyKDVwMEOg{txO M4\zfFI1QDh2OEC5
Huh-7 NXXSW3FRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrDXWkxPzJiaB?= NVu4T2k2TE2VTx?= MXvJR|UxRTN|Lkm2JOKyKDNwOTFOwG0> NIPWeZgzPDh6NEiwPS=>
Hep3B MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmS5O|IhcA>? NWTn[IhsTE2VTx?= MYHJR|UxRTJyLkG4JOKyKDFwOESg{txO MWiyOFg5PDhyOR?=
HepG2 NXfJWZNxSXCxcITvd4l{KEG|c3H5 MUDpcoR2[2W|IHHwc5B1d3Orcx?= NEDkTVUzPDh6NEiwPS=>
SMMC7721 MoPKRZBweHSxc3nzJGF{e2G7 M3jlVIlv\HWlZYOgZZBweHSxc3nz NIDiWXozPDh6NEiwPS=>
Huh-7 MUXBdI9xfG:|aYOgRZN{[Xl? NEHoV|BqdmS3Y3XzJIFxd3C2b4Ppdy=> MXuyOFg5PDhyOR?=
Hep3B NX3IV|FYSXCxcITvd4l{KEG|c3H5 MnTsbY5lfWOnczDhdI9xfG:|aYO= M{C0ZVI1QDh2OEC5
U2OS  NWjRRVRITnWwY4Tpc44hSXO|YYm= MlHyNlAh|ryP Mn;RNlQhcA>? NX[0fldtcW6lcnXhd4V{KHSqZTDtVm5CKGyndnXsd{Bw\sLiQlPMNmEyNCCEQ1zYUOKh[W6mQlPMWy=> NVzDfHBOOjR6NkeyOVk>
AML2 MlG3RZBweHSxc3nzJGF{e2G7 M4W0WVIwOTBizszN MljtNlQwPDhiaB?= M{ezbolv\HWlZYOgZZBweHSxc3nz Mn7GNlQ3PTl5NEm=
MOML13 MY\BdI9xfG:|aYOgRZN{[Xl? NYnKb2plOi9zMDFOwG0> NEHBOJUzPC92ODDo MlH2bY5lfWOnczDhdI9xfG:|aYO= NFf5N4QzPDZ3OUe0PS=>
AML2 NX\XT21JTnWwY4Tpc44hSXO|YYm= MoDhNVDPxE1? NH\uV24zNzRiaB?= M1Xie4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz NX:5e283OjR4NUm3OFk>
AML3 M1fkcmZ2dmO2aX;uJGF{e2G7 M4XWc|Ex|ryP NEXqRnkzNzRiaB?= NIDmbpJqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> M{jsUVI1PjV7N{S5
MOML13 MV3GeY5kfGmxbjDBd5NigQ>? MVmxNO69VQ>? MmnoNk81KGh? M1W2W4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz M4SxO|I1PjV7N{S5
BeWo MUPGeY5kfGmxbjDBd5NigQ>? MmTiN|AhyrWP NXzCU|BJOjRiaB?= NYrK[IU5cW6lcnXhd4V{KHB3MzygUYRuOixicEKxJIFv\CCSdX3hJIF1KHSqZTDwdo91\WmwIHzleoVt NUD4fINQOjR2OUixOVQ>
BeWo MVXBdI9xfG:|aYOgRZN{[Xl? MkHZN|AhyrWP M4faU|I1KGh? NHK2TFlqdmO{ZXHz[ZMh[XCxcITvd4l{ M3HQb|I1PDl6MUW0
OCI MmDPSpVv[3Srb36gRZN{[Xl? MWSxNEDPxE1? MmDSNlQhcA>? MUP1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? NV\OXZVnOjR2N{O1OlI>
MOLM M1jTSWZ2dmO2aX;uJGF{e2G7 M3fzWVExKM7:TR?= NInCcVUzPCCq MVX1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MUWyOFQ4OzV4Mh?=
U2OS  NYnTN5F5TnWwY4Tpc44hSXO|YYm= MXGyNEDPxE1? M3m0VVI1KGh? M1nEPYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? NHKyRXQzPDN4NkCwOy=>
RKO Mn60SpVv[3Srb36gRZN{[Xl? M4jtNlIxKM7:TR?= MYOyOEBp M1G0Uolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBJVy1zIIDyc5RmcW5iYYOge4VtdCCjczD0bIUheDV|IIDyc5RmcW5? MUSyOFM3PjByNx?=
U2OS  NITvcVZHfW6ldHnvckBCe3OjeR?= M1;tWFIxKM7:TR?= M3fSbFI1KGh? MmrLbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= MlL0NlQ{PjZyMEe=
RKO M3vUcmZ2dmO2aX;uJGF{e2G7 NYjZVWZ1OjBizszN NEm4d5kzPCCq MoXMbY5lfWOnczDIU{0yKGW6cILld5Nqd25iYYSgeIhmKGyndnXsJI9nKHS{YX7zZ5JqeHSrb36= NInP[W8zPDN4NkCwOy=>
SMMC-7721  NEO0fVNE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MYOxMlI2NTJyIN88US=> M4jNUlI1NzR6L{eyJIg> M3;Ub2ROW09? NEDabnhqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> NIK3eIEzPDJ6NkOxNi=>
HuH-7 NGTyXFhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M{P4W|EvOjVvMkCg{txO MWCyOE81QC95MjDo MWTEUXNQ M4L1SYlvcGmkaYTzJINmdGxicILvcIln\XKjdHnvckBld3OnIHHu[EB1cW2nIHTldIVv\GWwdHz5 M4e2fVI1Ojh4M{Gy
SMMC-7721  M4\VemFxd3C2b4Ppd{BCe3OjeR?= MVGyNEDPxE1? MV20PEBp M3TwRWROW09? M{fhd4lv\HWlZYOgZZBweHSxc3nz NH;6Z5kzPDJ6NkOxNi=>
HuH-7 MYHBdI9xfG:|aYOgRZN{[Xl? NYXK[YtnOjBizszN MVG0PEBp NXTOc5FiTE2VTx?= MoPHbY5lfWOnczDhdI9xfG:|aYO= MVeyOFI5PjNzMh?=
SMMC-7721  M2WxdmZ2dmO2aX;uJGF{e2G7 NWnPflRkOTBizszN NWjBb3VSOzZiaB?= M{THWGROW09? M4XYfoRwf25vcnXneYxifGW|IITo[UBxem:2ZXnuJIV5eHKnc4Ppc44hdGW4ZXygc4YheGixc4Doc{1U\XJ|OUKtdFU{ MlOzNlQzQDZ|MUK=
HuH-7 MXfGeY5kfGmxbjDBd5NigQ>? M3vRU|ExKM7:TR?= MYqzOkBp MlvRSG1UVw>? Mn3M[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> M3nhV|I1Ojh4M{Gy
AT2 MXnGeY5kfGmxbjDBd5NigQ>? NV;FfmdYPS9zMDFOwG0> M3HlXIxm[WS|IITvJIEhe3Wkc4ThcpRq[WxiYXPjeY12dGG2aX;uJI9nKHSqZTDwOVMheHKxdHXpckBieyC5ZXzsJIF{KHSqZTDlfJBz\XO|aX;uJI9nKGm2czDkbZJm[3RidHHy[4V1eyCyMkGsJG1FVTJiYX7kJJRp\SCycn:tZZBweHSxdHnjJGJCYCCjbnSgVHVOSSCycn;0[Ylve8Li MXuyOFI1ODJyMx?=
REH MnPiSpVv[3Srb36gRZN{[Xl? NV62d3gyPS9zMDFOwG0> NVz4SWxFdGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NUPu[297OjR{NECyNFM>
UoCB6 MV7GeY5kfGmxbjDBd5NigQ>? MVO1M|ExKM7:TR?= MYrs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? MYCyOFI1ODJyMx?=
AT2 NFT1Z|RE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M13ze|AuOjVizszN MUPpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 M{HPRlI1OjRyMkCz
REH NVzoUFRTS2WubDDWbYFjcWyrdImgRZN{[Xl? M33IeVAuOjVizszN MnrJbY5pcWKrdIOgZ4VtdCC4aXHibYxqfHliZH;z[UBl\XCnbnTlcpRtgQ>? NVzUSIo5OjR{NECyNFM>
UoCB6 MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M13ScVAuOjVizszN M4rUWYlvcGmkaYTzJINmdGxidnnhZoltcXS7IHTvd4Uh\GWyZX7k[Y51dHl? MUCyOFI1ODJyMx?=
A2780 M3r0XWZ2dmO2aX;uJGF{e2G7 NXTIbGpLPS9zMD:yNEDPxE1? NEiy[WUzPCCq NFW0fZJ2eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= M2HFXlI1OTN4MUS3
H460 NX;Oc4FXTnWwY4Tpc44hSXO|YYm= NUnYU|NbPS9zMD:yNEDPxE1? MYGyOEBp MnvveZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? MknsNlQyOzZzNEe=
Lovo  MWjGeY5kfGmxbjDBd5NigQ>? NH3kfoQ2NzFyL{KwJO69VQ>? NWTNfXFOOjRiaB?= M2PyWpVxemWpdXzheIV{KHB3MzygUWROOixicEKxJIFv\CCGUkWgdJJwfGWrbjDs[ZZmdHNiZH;z[UBl\XCnbnTlcpRtgcLi M3jyWVI1OTN4MUS3
A2780 M33iTmFxd3C2b4Ppd{BCe3OjeR?= NYLtUI04PS9zMD:yNEDPxE1? M1rmZlI1KGh? Mlvo[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MlPjNlQyOzZzNEe=
H460 NFLEblZCeG:ydH;zbZMhSXO|YYm= MXy1M|ExNzJyIN88US=> M4nKXVI1KGh? MnPa[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> NH7xXoIzPDF|NkG0Oy=>
Lovo  M2nyN2Fxd3C2b4Ppd{BCe3OjeR?= M3;LcFUwOTBxMkCg{txO NYXaR4prOjRiaB?= NV3HXlhE\W6qYX7j[ZMh[XCxcITvd4l{KGmwZIXjeIlwdiCkeTDENlY6UC:HMUm1VkBwfmW{IILoWHJCUUx? M{fzfVI1OTN4MUS3

... 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