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
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