Nutlin-3

For research use only. Not for use in humans.

目录号：S1061

Nutlin-3 Chemical Structure

Molecular Weight(MW): 581.5

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39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 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVi1xsDPxE1? MX60POKhcA>? NV;2cGN6[myxY3vzJFI4NU:KQz3pcoR2[2WmIHPlcIwheHKxbHnm[ZJifGmxbjDjc41x[XKjYnzlJJRwKHSqYYSgc4Yh[mG|YXygcIV3\Wy| NUnQZY1{OjZ|NUC1OlU>
NP69 MlPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDKTWM2OD1|MT62PeKyOi53NDFOwG0> MUmyOlI2OjV5NR?=
NP460 M4XuVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoP5TWM2OD1{Mj64OeKyOS5zODFOwG0> MWiyOlI2OjV5NR?=
C666-1 MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnr3TWM2OD1zOT65OeKyQC57MzFOwG0> M2W2V|I3OjV{NUe1
C666-1 MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M4XpOFExKML3TR?= MlnBOFghcA>? MlHrSG1UVw>? MX3z[Y5{cXSrenXzJGM3PjZvMTDj[YxteyC2bzD0bIUh[3m2b4TvfIlkKGWoZnXjeEBw\iClaYPwcIF1cW5? NV;oOGVzOjZ{NUK1O|U>
C666-1  NG\nXYNHfW6ldHnvckBCe3OjeR?= MYmxNEDDvU1? MWeyOEBp M4i0d2ROW09? NHfPZohi[3SrdnH0[ZMhfGinIIC1N{Bx[XSqd3H5MEB2eHKnZ4XsZZRqdmdicEWzMEBxOjFiYX7kJG1ldTJ? M{HSclI3OjV{NUe1
C666-1 NUPYSItISXCxcITvd4l{KEG|c3H5 M1XafFExKML3TR?= NY\KXoh7PDhxN{KgbC=> NUm0W|JwTE2VTx?= NUmyOHdke2Wwc3n0bZpmeyCFNk[2MVEh[2WubIOgeI8h[2m|cHzheIlvNWmwZIXj[YQh[XCxcITvd4l{ NWXnZ5JNOjZ{NUK1O|U>
A549 M3XqW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLsW5IzPCCq MXvJR|UxRTF5Lk[4JOKyKDRwNUKg{txO NIXXfY0zPjF{NUKzNC=>
A549-NTC M{jqd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzOeYkzPCCq MmfkTWM2OD1zOT60NkDDuSBzLkm2JO69VQ>? NF7XNHQzPjF{NUKzNC=>
A549-920 NH3zbVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXX1T49FOjRiaB?= NHOzbY5KSzVyPUOzMlg2KMLzIESuPFQh|ryP NIDVT5IzPjF{NUKzNC=>
CRL-5908 M37ITGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVmyOEBp NYi0[2xWUUN3ME2zPE44OSEEsTCyMlQ{KM7:TR?= NVXvOINUOjZzMkWyN|A>
L6 NYDvXHJ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjIOoxUOTEEoN88UeKh NGjqS3ozPC92OD:3NkBp MVLEUXNQ M2XDXolvcGmkaYTzJINmdGy|IIDyc4xq\mW{YYTpc44h[W6mIHTp[oZmemWwdHnheIlwdg>? NHjucW8zPTh5MUe5OC=>
C2C12 NUfO[nNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO4O2VwOTEEoN88UeKh M4T5UlI1NzR6L{eyJIg> MXTEUXNQ NGXSN25qdmirYnn0d{Bk\WyuczDwdo9tcW[ncnH0bY9vKGGwZDDkbYZn\XKnboTpZZRqd25? MV6yOVg4OTd7NB?=
MCF-7  NHvOXFZHfW6ldHnvckBCe3OjeR?= MXKxNOKh|ryP M1vNdGROW09? M{DqS4lvcGmkaYTzJIN6[2yrbjDENUBidmRiRHnj[ZLDqA>? NGjQNZEzPTdyMkewNy=>
DU4475  M4\pe2Z2dmO2aX;uJGF{e2G7 MW[1M|ExNzJyIN88US=> M1POPVI1yqCq Mn:2[I94dnKnZ4XsZZRmeyCWb3PhMVEh\G:|ZTDk[ZBmdmSnboTsfS=> MXqyOVU1PzF5NB?=
SMMC-7721 NVTacYJyTnWwY4Tpc44hSXO|YYm= NFL1RZMyOCEQvF2= M2fj[VQ5KGh? MXzEUXNQ MUPjZZV{\XNiRF7BJGRUSiCmYX3h[4U> NULDTZh4OjV3NESzOlE>
SMMC-7721 NVfQZ3BrTnWwY4Tpc44hSXO|YYm= NYnzbJI3OTBizszN M2[3[VQ5KGh? NF\XPFZFVVOR MYPpcoR2[2W|IITo[UBkcHKxbXH0bY4u[m:3bnSgdJJwfGWrbjDJSmkyPiC2bzDwZZJ1cWGubImgcI9k[WyrenWgbY4hfGinIHP5eI9xdGG|bdMg NGj6bpEzPTV2NEO2NS=>
SMMC-7721 MX\GeY5kfGmxbjDBd5NigQ>? Mnf5NVAh|ryP NW\KNJpIPDhiaB?= NFfpcYtFVVOR MWXpcoNz\WG|ZYOgeIhmKGW6cILld5Nqd25ibHX2[Ywhd2cEoFnGUmIyyqCvUl7B MV2yOVU1PDN4MR?=
SMMC-7721 MX7GeY5kfGmxbjDBd5NigQ>? MlPnNVAh|ryP M4P1VlM3KGh? MWDEUXNQ M1XKd4NifXOnczD0bIUh\WO2b4DpZ{BmgHC{ZYPzbY9vKG:oIFnGTVE3 MWeyOVU1PDN4MR?=
MCF-7 NYTXeoJSTnWwY4Tpc44hSXO|YYm= M3PQeVExyqEQvF2= M1:5WFAuOjRiaB?= MlW2bY5lfWOnczDwOVMh[W6mIICyNU9EcXBz NI\pcXMzPTR6MkO3Ny=>
OVCAR10 NYfZdXRJTnWwY4Tpc44hSXO|YYm= MnfuNVDDqM7:TR?= M3XHVFIycMLi MUHEUXNQ MlPabY5kemWjc3XzJJA2OyCycn;0[YlvKGyndnXsdy=> MmTwNlU1OjZ3NEi=
NCI-H23 NIXCfVVHfW6ldHnvckBCe3OjeR?= NIPsR2EyOMLizszN MUOyNYjDqA>? NFn5OXRFVVOR M3\QPIlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> M2nZdFI2PDJ4NUS4
A2780 M331dGZ2dmO2aX;uJGF{e2G7 NHjkOpEyOMLizszN MWWyNYjDqA>? NWrEVFMzTE2VTx?= M1KzdYlv[3KnYYPld{BxPTNicILveIVqdiCuZY\lcJM> NYnpZlZnOjV2Mk[1OFg>
NCI-H23 Mm\NSpVv[3Srb36gRZN{[Xl? NF71N4MyOMLizszN NGfNUWszOWkEoB?= NWD0VmVmTE2VTx?= MoLr[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= MlnSNlU1OjZ3NEi=
A2780 MYfGeY5kfGmxbjDBd5NigQ>? M4C3NlExyqEQvF2= M2\ldVIycMLi MXTEUXNQ MmTk[IVkemWjc3XzJJRp\SCIb4jNNUBt\X[nbIO= MnrONlU1OjZ3NEi=
HCT116  NIf5RnBHfW6ldHnvckBCe3OjeR?= M4LldlExKML3TR?= M1G5cFI1KGh? NU\TVY43[2G3c3XzJIEheDV|LXTldIVv\GWwdDD0[ZRz[XCub3nkJGcyNWG{cnXzeEBqdiCmaYDsc4llKEiFVEGxOkBkdG:wZYOgSFMh[W6mIFS4 NGTNNpIzPTN6MEC1OS=>
MCF-10CA1a MlrISpVv[3Srb36gRZN{[Xl? NEH6RXEyOMLizszN MkO0OFghcA>? Ml:wSG1UVw>? MnHQbY5pcWKrdIOgZoF{[WxiaX72ZZNqd25iYX7kJJJm\HWlZXSgWGdHNc7{Mz3pcoR2[2WmIHnueoF{cW:wIITvJIJie2GuIHzleoVtew>? NEe5doIzPTJ3N{eyPS=>
MCF-10A1  NXi0Uo4xTnWwY4Tpc44hSXO|YYm= M3i4ZlExyqEQvF2= MmPZNlQwPDhiaB?= MU\EUXNQ M2XPVolvcGmkaYTzJI1q\3KjdHnvckBw\iCwb4LtZYwh[nKnYYP0JIVxcXSqZXzpZYzDqA>? MYiyOVI2Pzd{OR?=
MCF-10CA1a NVnYOnpHTnWwY4Tpc44hSXO|YYm= M2jid|ExyqEQvF2= NWfZ[4dXOjRiaB?= MVvEUXNQ NH3ZXJdl\WO{ZXHz[ZMhfGinIGTHSk3PujNvaX7keYNm\CCvUl7BJIxmfmWuczDv[m1OWDJuwrDNUXA6NCCjbnVCpIlvfGWpcnnuxsDPusLiMx?= MXiyOVI2Pzd{OR?=
MCF-10CA1a NWXyWG86TnWwY4Tpc44hSXO|YYm= M2L6eVExyqEQvF2= M1H2cFI1KGh? MXTEUXNQ MULpcohq[mm2czCgWGdHNc7{Mz3pcoR2[2WmIFXQTGIzyqCvUl7BJIFv\CCycn;0[YlvKGW6cILld5Nqd25? NUHyOoUzOjV{NUe3Nlk>
SK-BR-7 NGnYZ3BHfW6ldHnvckBCe3OjeR?= MlrvNVDDqM7:TR?= M4raWFI1KGh? MWDEUXNQ NIX6[JhqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= M2C1U|I2OjV5N{K5
SUM102PT NHzTS3VHfW6ldHnvckBCe3OjeR?= NYPlUGJNOTEEoN88US=> NILPTIMzPCCq NYm1[moxTE2VTx?= NFjlSnlqdmirYnn0d{AhXEeILd8yN{1qdmS3Y3XkJGVRUEJ{wrDtVm5CKGGwZDDwdo91\WmwIHX4dJJme3Orb36= MkSxNlUzPTd5Mkm=
RAW 264.7 NITjeJBHfW6ldHnvckBCe3OjeR?= NFXqWWwyOMLizszN NUXhRpQ6OzBibXnu NI\UWnNxemW4ZX70d{B1cGVicEWzJJJm\HWldHnvckBqdiC{ZYPwc45{\SC2bzDMVHM> M4n4XlI2OTd{NUS3
RAW 264.7 MY\GeY5kfGmxbjDBd5NigQ>? MYqxNOKh|ryP MVizNEBucW5? Moj0doVlfWOnczD0bIUhVFCVLXH1[41mdnSnZDD0bIUhVkZvzsrCJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhZ5Rqfmm2eR?= NYHV[ndSOjVzN{K1OFc>
RAW 264.7 Ml;NSpVv[3Srb36gRZN{[Xl? NV7hXHpyOTEEoN88US=> M2DOT|MxKG2rbh?= NX3iU|F{cW6qaXLpeJMhVFCVLXnu[JVk\WRiTl:gdJJw\HWldHnvcuKh MUOyOVE4OjV2Nx?=
MCF7  NUPt[YVVS2WubDDWbYFjcWyrdImgRZN{[Xl? M2PabFIvPSEEtV2= MV[1JIQ> M2\SS2ROW09? MVnz[Y5{cXSrenXzJG1ETjdidH:gVGFTWCCrbnjpZol1cW:w NXzvPXlNOjVyOEW5NFI>
MCF7  NYjvZZo1TnWwY4Tpc44hSXO|YYm= MV6yMlUhyrWP NXPPcJhuPDhiaB?= MnG4SG1UVw>? NILOSm5l\WO{ZXHz[ZMhfGinIHjvcY9td2exdYOgSHNDKHKncHHpdkBnemWzdXXuZ4lmew>? M4THfVI2ODh3OUCy
ACHN MWnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MVywMlUuOTBizszN M{\MPFAuPiCm MX;EUXNQ MVHpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXjnc3ZtOjVyNke3PFc>
Caki-2 MXPD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXOwMlUuOTBizszN M{DHSlAuPiCm NYO0XnNzTE2VTx?= MULpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFPZ[W0zPTB4N{e4Oy=>
A498 NVK4[oY4S2WubDDWbYFjcWyrdImgRZN{[Xl? NYrrcYNDOC53LUGwJO69VQ>? NUfvWpcxOC14IHS= NEnifFhFVVOR MYTpcohq[mm2czDwdo9tcW[ncnH0bY9vKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUKyOVA3Pzd6Nx?=
115 MYnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NGq5RXIxNjVvMUCg{txO MWewMVYh\A>? MoPjSG1UVw>? MoHpbY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NWni[pVROjVyNke3PFc>
117 NVjZPW4xS2WubDDWbYFjcWyrdImgRZN{[Xl? MofDNE42NTFyIN88US=> MY[wMVYh\A>? MVvEUXNQ Ml;1bY5pcWKrdIOgdJJwdGmoZYLheIlwdiCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MoS5NlUxPjd5OEe=
ACHN NIXDSVJHfW6ldHnvckBCe3OjeR?= NEm1epAxNjVxMT:1JO69VQ>? NXq0ZlF[PDhiaB?= MoPTSG1UVw>? NVj3dpRrdGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= NEK5OWQzPTB4N{e4Oy=>
Caki-2 NUO5O5FJTnWwY4Tpc44hSXO|YYm= NFnDZ4MxNjVxMT:1JO69VQ>? NF\mZYI1QCCq NGP4TldFVVOR NV3WW5A2dGWjZIOgeI8hcW6lcnXhd4VlKGW6cILld5Nqd25ib3[gdFU{KGGwZDDzc41mKHB3MzD0ZZJo\XRiZ3Xu[ZM7KE2GTUKsJIFv\CCyMkG= MUWyOVA3Pzd6Nx?=
A498 NHOyfZRHfW6ldHnvckBCe3OjeR?= MYKwMlUwOS93IN88US=> NEXqfpY1QCCq NV3jR2p1TE2VTx?= NETPcIFt\WGmczD0c{BqdmO{ZXHz[YQh\XiycnXzd4lwdiCxZjDwOVMh[W6mIIPvcYUheDV|IIThdodmfCCpZX7ld|ohVUSPMjygZY5lKHB{MR?= NVrkVYtmOjVyNke3PFc>
115 NYjQS21sTnWwY4Tpc44hSXO|YYm= M{fad|AvPS9zL{Wg{txO NXy3R3V[PDhiaB?= M4Dwe2ROW09? MkP5cIVi\HNidH:gbY5kemWjc3XkJIV5eHKnc4Ppc44hd2ZicEWzJIFv\CC|b33lJJA2OyC2YYLn[ZQh\2WwZYO6JG1FVTJuIHHu[EBxOjF? MmK2NlUxPjd5OEe=
ACHN NGrMZ49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLZOUDPxE1? NWmwXJRxPDhiaB?= M4XGcGROW09? MnTzbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MVWyOVA3Pzd6Nx?=
Caki-2 M2H1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXNUWE2KM7:TR?= M4Had|Q5KGh? M2XReWROW09? NGDnZoFqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> MonvNlUxPjd5OEe=
A498 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\3UYk2KM7:TR?= M1XLVlQ5KGh? NVLQ[WZ6TE2VTx?= NX3SN4tjcW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh NHLMXHQzPTB4N{e4Oy=>
115 M3HxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK1JO69VQ>? NXyye45NPDhiaB?= MmnLSG1UVw>? M{DG[Ilv\HWlZYOgZ4VtdCCleXPs[UBienKnc4VCpC=> MYeyOVA3Pzd6Nx?=
ACHN M{mwdGZ2dmO2aX;uJGF{e2G7 MofpOUDPxE1? MYW0PEBp NFWxO5ZFVVOR MYnpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MYSyOVA3Pzd6Nx?=
Caki-2 MnnSSpVv[3Srb36gRZN{[Xl? NInvOIY2KM7:TR?= NEnQ[2U1QCCq NYDR[Y9HTE2VTx?= MlTybY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NG\JTmYzPTB4N{e4Oy=>
A498 MXHGeY5kfGmxbjDBd5NigQ>? M1PFUFUh|ryP MXq0PEBp M3rzTWROW09? MlPWbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= MVmyOVA3Pzd6Nx?=
115 MXLGeY5kfGmxbjDBd5NigQ>? NFLCTnI2KM7:TR?= NXnPTldUPDhiaB?= MojrSG1UVw>? NEjGWIxqdmS3Y3XzJJA2Oy2mZYDlcoRmdnRic3Xu[ZNk\W6lZdMg NEnmVngzPTB4N{e4Oy=>
MOLM-13 NELUfo1HfW6ldHnvckBCe3OjeR?= NUT0Oox4PsLizszN MoLYNE05KGh? MVPEUXNQ MWTpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iCyNUOsJG1FVTJuIICyNUBidmRiYXPleJlt[XSnZDDwOVM> NF\EW48zPDh6NUC4Ni=>
MOLM-13 Mmj3SpVv[3Srb36gRZN{[Xl? MX62xsDPxE1? NVOyW|NUPiCq MUDEUXNQ NXPGTVFQ\W6qYX7j[ZMhfGinIHHj[ZR6dGG2aX;uJI9nKGirc4TvcoUhUDKEIHHu[EBp\WG2IIPoc4NsKHC{b4TlbY5{KEi|cEK3JIFv\CCKc4C5NC=> NWrqeVV4OjR6OEWwPFI>
HepG2 NGT4VohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rPUlczKGh? M3HEe2ROW09? M3K3U2lEPTB;M{WuPFYhyrFiMj65JO69VQ>? MkOxNlQ5QDR6MEm=
HepG2/As NYfOT5B{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVG3NkBp NFjWWldFVVOR NVfmVW9pUUN3ME22PE4yOyEEsTC5MlYh|ryP MX2yOFg5PDhyOR?=
SMMC7721 Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPBSHc4OiCq MXrEUXNQ NFXMcHFKSzVyPUOxMlI5KMLzIESuNkDPxE1? MlzYNlQ5QDR6MEm=
SMMC7721/Ac NHjNcWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWD1bJNnPzJiaB?= NGW1UVdFVVOR MUTJR|UxRTV3LkKxJOKyKDVwMEOg{txO M2rUe|I1QDh2OEC5
Huh-7 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3YXpA4OiCq MlziSG1UVw>? M3vkPGlEPTB;M{OuPVYhyrFiMz65JO69VQ>? MVKyOFg5PDhyOR?=
Hep3B M3nWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWO3NkBp M2jmbGROW09? NYPOc3R{UUN3ME2yNE4yQCEEsTCxMlg1KM7:TR?= MknQNlQ5QDR6MEm=
HepG2 NETr[FhCeG:ydH;zbZMhSXO|YYm= NEmzbY1qdmS3Y3XzJIFxd3C2b4Ppdy=> MkLvNlQ5QDR6MEm=
SMMC7721 NVeyXHR6SXCxcITvd4l{KEG|c3H5 NUDrNpFncW6mdXPld{BieG:ydH;zbZM> MXuyOFg5PDhyOR?=
Huh-7 MkjhRZBweHSxc3nzJGF{e2G7 MXLpcoR2[2W|IHHwc5B1d3Orcx?= NH7TfHEzPDh6NEiwPS=>
Hep3B MlnuRZBweHSxc3nzJGF{e2G7 M1f2VIlv\HWlZYOgZZBweHSxc3nz NX7lSWs4OjR6OES4NFk>
U2OS  NH36TVdHfW6ldHnvckBCe3OjeR?= MUWyNEDPxE1? NYDUNJZGOjRiaB?= MXPpcoNz\WG|ZYOgeIhmKG2UTlGgcIV3\Wy|IH;mxsBDS0x{QUGsJGJEVFiOwrDhcoRDS0yZ NIDwT20zPDh4N{K1PS=>
AML2 NV7EOXZNSXCxcITvd4l{KEG|c3H5 MXiyM|ExKM7:TR?= MWmyOE81QCCq NEXnO|dqdmS3Y3XzJIFxd3C2b4Ppdy=> NFy0dJkzPDZ3OUe0PS=>
MOML13 NYHJTZNGSXCxcITvd4l{KEG|c3H5 NFfY[VgzNzFyIN88US=> NY\WOlBwOjRxNEigbC=> NE\SWHVqdmS3Y3XzJIFxd3C2b4Ppdy=> MXqyOFY2QTd2OR?=
AML2 MYfGeY5kfGmxbjDBd5NigQ>? MmfINVDPxE1? MWSyM|QhcA>? NVHyS2xPcW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NH;Zb5czPDZ3OUe0PS=>
AML3 MlfLSpVv[3Srb36gRZN{[Xl? NYSze4VWOTEQvF2= NF7We3IzNzRiaB?= M1jhO4lv[3KnYYPld{B1cGVibHX2[Ywhd2ZicEWz MoLmNlQ3PTl5NEm=
MOML13 NEnjeXhHfW6ldHnvckBCe3OjeR?= NWiy[pI4OTEQvF2= NGfhfJgzNzRiaB?= NXjoRZNicW6lcnXhd4V{KHSqZTDs[ZZmdCCxZjDwOVM> NEH2bXMzPDZ3OUe0PS=>
BeWo MWfGeY5kfGmxbjDBd5NigQ>? MVmzNEDDvU1? NWTLNnROOjRiaB?= MW\pcoNz\WG|ZYOgdFU{NCCPZH2yMEBxOjFiYX7kJHB2dWFiYYSgeIhmKHC{b4TlbY4hdGW4ZXy= MYqyOFQ6QDF3NB?=
BeWo Mm\sRZBweHSxc3nzJGF{e2G7 NGntcGE{OCEEtV2= NWLUXJd4OjRiaB?= NH\z[5NqdmO{ZXHz[ZMh[XCxcITvd4l{ NHnaNFIzPDR7OEG1OC=>
OCI MkLJSpVv[3Srb36gRZN{[Xl? MnrnNVAh|ryP NG\hWmwzPCCq NImycVJ2eHKnZ4XsZZRmeyC2aHWgV29EWy1zIHX4dJJme3Orb36= M4nmcFI1PDd|NU[y
MOLM NGDVfopHfW6ldHnvckBCe3OjeR?= NXPlXJlJOTBizszN NUPUbYE5OjRiaB?= MWH1dJJm\3WuYYTld{B1cGViU1;DV{0yKGW6cILld5Nqd25? MVmyOFQ4OzV4Mh?=
U2OS  Mn\RSpVv[3Srb36gRZN{[Xl? NH3pPGYzOCEQvF2= MXOyOEBp NHew[5NqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw NGTiVngzPDN4NkCwOy=>
RKO NFeyUZdHfW6ldHnvckBCe3OjeR?= NFziV5czOCEQvF2= MmD3NlQhcA>? MV;pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgTG8uOSCycn;0[YlvKGG|IIflcIwh[XNidHjlJJA2OyCycn;0[Ylv M{PLelI1OzZ4MEC3
U2OS  MVXGeY5kfGmxbjDBd5NigQ>? NHLLRZgzOCEQvF2= NUfSboRYOjRiaB?= MYXpcoR2[2W|IFjPMVEh\XiycnXzd4lwdiCjdDD0bIUhdGW4ZXygc4YhfHKjboPjdolxfGmxbh?= MnLjNlQ{PjZyMEe=
RKO MlviSpVv[3Srb36gRZN{[Xl? M2XTUFIxKM7:TR?= MYqyOEBp NHP2XIpqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MkKwNlQ{PjZyMEe=
SMMC-7721  NGTyOpBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MkXBNU4zPS1{MDFOwG0> MYmyOE81QC95MjDo MYPEUXNQ NF2y[GFqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> M{\VPVI1Ojh4M{Gy
HuH-7 NUO4dIpVS2WubDDWbYFjcWyrdImgRZN{[Xl? MljPNU4zPS1{MDFOwG0> NXPmS2dIOjRxNEivO|IhcA>? Mn\LSG1UVw>? Mn\NbY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MmraNlQzQDZ|MUK=
SMMC-7721  NXjFeVJzSXCxcITvd4l{KEG|c3H5 M4K1cVIxKM7:TR?= MmHrOFghcA>? M3S0[2ROW09? NFrKPVFqdmS3Y3XzJIFxd3C2b4Ppdy=> M3zwPVI1Ojh4M{Gy
HuH-7 NGrhVmRCeG:ydH;zbZMhSXO|YYm= MXyyNEDPxE1? Mo\UOFghcA>? NF3ON5dFVVOR Mn\KbY5lfWOnczDhdI9xfG:|aYO= M2nOVVI1Ojh4M{Gy
SMMC-7721  M3nWXWZ2dmO2aX;uJGF{e2G7 NXG4UZF4OTBizszN MmrHN|YhcA>? MVnEUXNQ MnfG[I94di2{ZXf1cIF1\XNidHjlJJBzd3SnaX6g[ZhxemW|c3nvckBt\X[nbDDv[kBxcG:|cHjvMXNmejN7Mj3wOVM> NELNUZkzPDJ6NkOxNi=>
HuH-7 MVnGeY5kfGmxbjDBd5NigQ>? MUexNEDPxE1? NVPDOHRuOzZiaB?= NGLleJBFVVOR NGizRnBld3ewLYLl[5Vt[XSnczD0bIUheHKxdHXpckBmgHC{ZYPzbY9vKGyndnXsJI9nKHCqb4PwbI8uW2W{M{myMZA2Ow>? NILIbFAzPDJ6NkOxNi=>
AT2 M3LGcmZ2dmO2aX;uJGF{e2G7 M{SyZVUwOTBizszN NXK0T4N2dGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NEXGe4YzPDJ2MEKwNy=>
REH MYPGeY5kfGmxbjDBd5NigQ>? MnHJOU8yOCEQvF2= MUTs[YFleyC2bzDhJJN2[nO2YX70bYFtKGGlY4XteYxifGmxbjDv[kB1cGVicEWzJJBzd3SnaX6gZZMhf2WubDDhd{B1cGViZYjwdoV{e2mxbjDv[kBqfHNiZHny[YN1KHSjcnfleJMheDJzLDDNSG0zKGGwZDD0bIUheHKxLXHwc5B1d3SrYzDCRXgh[W6mIGDVUWEheHKxdHXpcpPDqA>? M4rPRlI1OjRyMkCz
UoCB6 NI\CXoVHfW6ldHnvckBCe3OjeR?= MVy1M|ExKM7:TR?= NYXncYFudGWjZIOgeI8h[SC|dXLzeIFvfGmjbDDhZ4N2dXWuYYTpc44hd2ZidHjlJJA2OyCycn;0[YlvKGG|IIflcIwh[XNidHjlJIV5eHKnc4Ppc44hd2ZiaYTzJIRqemWldDD0ZZJo\XS|IICyNUwhVUSPMjDhcoQhfGinIIDyc{1ieG:ydH;0bYMhSkG[IHHu[EBRXU2DIIDyc5RmcW6|wrC= NFnU[3UzPDJ2MEKwNy=>
AT2 M2XEd2NmdGxiVnnhZoltcXS7IFHzd4F6 M3TmfVAuOjVizszN NV72WVB5cW6qaXLpeJMh[2WubDD2bYFjcWyrdImg[I9{\SCmZYDlcoRmdnSueR?= NYfZZ2pWOjR{NECyNFM>
REH M37aOGNmdGxiVnnhZoltcXS7IFHzd4F6 NXfpc2ZoOC1{NTFOwG0> MVvpcohq[mm2czDj[YxtKH[rYXLpcIl1gSCmb4PlJIRmeGWwZHXueIx6 NGTZTVczPDJ2MEKwNy=>
UoCB6 MWDD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M33rdlAuOjVizszN NH7USG1qdmirYnn0d{Bk\WyuII\pZYJqdGm2eTDkc5NmKGSncHXu[IVvfGy7 MX:yOFI1ODJyMx?=
A2780 NYSxZ|ZuTnWwY4Tpc44hSXO|YYm= NH:yVVk2NzFyL{KwJO69VQ>? NXnBSJFmOjRiaB?= MoL3eZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? NGTzdZAzPDF|NkG0Oy=>
H460 MmfvSpVv[3Srb36gRZN{[Xl? NVHtdoRxPS9zMD:yNEDPxE1? M372bFI1KGh? Ml\heZBz\We3bHH0[ZMheDV|LDDNSG0zNCCyMkGgZY5lKESUNTDwdo91\WmwIHzleoVteyCmb4PlJIRmeGWwZHXueIx6yqB? Mn\zNlQyOzZzNEe=
Lovo  M4e1dGZ2dmO2aX;uJGF{e2G7 MkfyOU8yOC9{MDFOwG0> NGP0S4wzPCCq NFjaVo52eHKnZ4XsZZRmeyCyNUOsJG1FVTJuIICyNUBidmRiRGK1JJBzd3SnaX6gcIV3\Wy|IHTvd4Uh\GWyZX7k[Y51dHoEoB?= NXqwVFZVOjRzM{[xOFc>
A2780 M4HINWFxd3C2b4Ppd{BCe3OjeR?= NFO1cVk2NzFyL{KwJO69VQ>? M3fPfVI1KGh? MoDo[Y5p[W6lZYOgZZBweHSxc3nzJIlv\HWldHnvckBjgSCGMk[5TE9GOTl3UjDveoVzKHKqVGLBTWw> MlzINlQyOzZzNEe=
H460 MojZRZBweHSxc3nzJGF{e2G7 MmXNOU8yOC9{MDFOwG0> NVy0fWpuOjRiaB?= NGnLc|ZmdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? M4jvTFI1OTN4MUS3
Lovo  NEjlW|BCeG:ydH;zbZMhSXO|YYm= NXHGWldDPS9zMD:yNEDPxE1? MlnINlQhcA>? NEXCZW9mdmijbnPld{BieG:ydH;zbZMhcW6mdXP0bY9vKGK7IFSyOllJN0VzOUXSJI93\XJicnjUVmFKVA>? NEHrdIYzPDF|NkG0Oy=>

... 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 只
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.

Selleck产品目录册

Mdm2 Signaling Pathway Map

相关Mdm2产品

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  • MI-773 (SAR405838) New

    MI-773 (SAR405838) 是一种口服生物有效的MDM2拮抗剂，Ki为0.88 nM。Phase 1。

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  • NSC 207895

    NSC 207895抑制MDMX，IC50为2.5 μM，促进p53稳定/激活和DNA损伤，也调节MDM2（E3连接酶）。

  • Nutlin-3a

    Nutlin-3a 是Nutlin-3的活性对映体，抑制p53/MDM2相互作用，无细胞试验中IC50为90 nM。Nutlin-3a 可诱导p53依赖的自噬和细胞凋亡。

  • Nutlin-3b

    Nutlin-3b是一种p53/MDM2拮抗剂或抑制剂，IC50值为13.6μM，是Nutlin-3的（+）-对映体，比(-)-对映体Nutlin-3a作用效果低150倍。

  • YH239-EE

    YH239-EE,YH239乙酯,是一种强效的 p53-MDM2 拮抗剂和细胞凋亡诱导剂。

  • Z-VAD-FMK

    Z-VAD-FMK是一种细胞渗透性的，不可逆泛caspase抑制剂，在THP.1 和 Jurkat T细胞中阻断细胞凋亡的所有特性。

    Features:Z-VAD-FMK是研究细胞凋亡的一种关键化合物。

  • Navitoclax (ABT-263)

    Navitoclax (ABT-263)是一种有效的Bcl-xL，Bcl-2和Bcl-w抑制剂，无细胞试验中Ki分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。Phase 2。

  • Venetoclax (ABT-199)

    Venetoclax (ABT-199, GDC-0199)是一种Bcl-2选择性抑制剂，无细胞试验中Ki为<0.01 nM，比作用于Bcl-xL和Bcl-w选择性高4800倍以上，对Mcl-1没有抑制活性。有研究证明 Venetoclax 在三阴性乳腺癌 MDA-MB-231 细胞中诱导细胞生长抑制，凋亡，细胞周期停滞和自噬。Phase 3。

    Features:ABT-263 (Navitoclax)的重组

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID