3-Methyladenine (3-MA)

目录号：S2767 别名： NSC 66389

3-Methyladenine (3-MA) Chemical Structure

Molecular Weight(MW): 149.15

3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。现配现用（加热助溶）。

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产品安全说明书

PI3K抑制剂选择性比较

生物活性

产品描述 3-Methyladenine (3-MA)是一种选择性PI3K抑制剂，作用于Vps34和PI3Kγ，在 HeLa细胞中IC50分别为25 μM和60 μM；永久性抑制I型PI3K，但对III型PI3K的抑制是短暂的，也会阻断自噬体的形成。现配现用（加热助溶）。
靶点
Vps34 [1]
(HeLa cells)		 PI3Kγ [1]
(HeLa cells)
25 μM 60 μM
体外研究

3-MA对Vps34轻微的偏向性可能是由于Vps34中某个特异性的疏水环形结构可以环绕在3-MA的3-甲基基团外面造成的[1] 。据报道对于正常培养和饥饿处理的癌细胞3-MA都能引起细胞死亡。3-MA还可以不通过抑制自吞噬来抑制细胞迁移和入侵，这表明3-MA 除了抑制自吞噬之外还有其它生物功能。3-MA可以造成半胱天冬酶依赖的细胞死亡，这一功能与它对自吞噬的抑制无关。用5mM 3-MA处理葡萄糖饥饿Hela细胞可降低gfp-lc3阳性细胞比例至23%。3-MA处理细胞12到48小时内 LC3-I 的水平上升而LC3-II 水平下降。LC3-I转为为 LC3-II 的过程被3-MA抑制了。 2.5 mM 或5 mM 3-MA 处理HeLa 细胞一天并不影响细胞存活率, 而 10 mM 3-MA 处理一天会造成细胞存活率下降25.0% 。 2.5, 5 或 10 mM 3-MA 处理细胞两天分别使细胞存活率下降 11.5%, 38.0% 和79.4% 。3-MA 降低细胞存活率的作用具有时间和剂量依赖特性。3-MA 明显缩短nocodazole诱导的前中期阻断时间[2]。3-MA 通过抑制自吞噬来抑制SU11274诱导的细胞死亡[3]。 在野生型MEF细胞中延长 3-MA处理时间 (最多 9 小时) 明显造成 LC3 I 到 II 转换。延长 3-MA处理时间会明显增加GFP-LC3的聚集而wortmannin不具有此功能。3-MA介导的LC3 转换和游离 GFP 释放是ATG7依赖的。 3-MA处理会导致 p62 蛋白水平明显升高。即使在Atg5−/− 的MEF细胞中3-MA 也会使p62 水平升高，就像在DOX介导的ATG5缺失的细胞中一样 。3-MA以不同方式抑制 I 型和 III型 PI3K。与野生型细胞相比，在Tsc2−/−细胞中3-MA诱导的 LC3 I 到 LC3 II 转换过程大幅下降。3-MA会破坏mTOR复合物1的拮抗自吞噬功能[4]。
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
95D M2Habmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXLTlE{dU1? NVPafFZxOmh? M{fNe2ROW09? NH23cWZz\WS3Y3XzJIdzd3e2aDDpcohq[mm2b4L5JIVn\mWldDDv[kBDTE2F NW\m[YpbOjV5MU[1OlE>
A549  NI\o[YZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu0XmQ{dU1? NXS0UGNIOmh? NW[xe3JwTE2VTx?= NFLT[3Rz\WS3Y3XzJIdzd3e2aDDpcohq[mm2b4L5JIVn\mWldDDv[kBDTE2F MYOyOVcyPjV4MR?=
95D MVfBdI9xfG:|aYOgRZN{[Xl? MV61cW0> MlqyNog> M3rOSWROW09? NFXHW2ZqdmirYnn0d{BDTE2FLXnu[JVk\WRiYYDvdJRwfGmlIHPlcIwh\GWjdHi= MonvNlU4OTZ3NkG=
A549  M1LaUmFxd3C2b4Ppd{BCe3OjeR?= NHLE[Gs2dU1? M4nBO|Jp MXLEUXNQ MkfhbY5pcWKrdIOgRmROSy2rbnT1Z4VlKGGyb4D0c5Rq[yClZXzsJIRm[XSq MX2yOVcyPjV4MR?=
NBL-W-S  NWDTe|MzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVixcW0> NUCxc5ZGPmh? NFew[pNmdmijbnPld{BISU6WLU[xJJRwgGmlaYT5 MXqyOVMzOzJ{Mh?=
NBL-W-S  NYfJNodySXCxcITvd4l{KEG|c3H5 MlnqNY1O MkDUOog> M374eYlv[3KnYYPld{Bk\WyuIHHwc5B1d3OrczDpcoR2[2WmIHL5JGdCVlRvNkG= NWHZb21vOjV|MkOyNlI>
A2780cp  MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37EVVFuVQ>? M{TEZ|Fp NEP2XGhqdmO{ZXHz[ZMh[2m|cHzheIlvNWmwZIXj[YQh[2WubDDk[YF1cA>? NYi0Vm9EOjV|MkK2PVQ>
A549  NF;oR5RHfW6ldHnvckBCe3OjeR?= NY\DRoxwPW2P NVL2[5k2Omh? Mn7ld5VxeHKnc4Pld{BUWENiaX7keYNm\CCjY3P1cZVt[XSrb36gc4YhVEN|LVnJ MXSyOVI5PTZ{OB?=
H157 MWfGeY5kfGmxbjDBd5NigQ>? NHXvN3o2dU1? MUWybC=> MVHzeZBxemW|c3XzJHNRSyCrbnT1Z4VlKGGlY4XteYxifGmxbjDv[kBNSzNvSVm= M4frN|I2Ojh3NkK4
MDR Mm\ORZBweHSxc3nzJGF{e2G7 MVWxNI1O M{DQbFZp MVfzeJJmdme2aHXud{B1cGVicH;3[ZIhd2ZiYX70bYNidmOncjDkdpVoew>? M3XRXFI2ODF7N{Cx
HT-29  NFLHV2RCeG:ydH;zbZMhSXO|YYm= MVexcW0> NX7DO|VsPDiq M3zBd2ROW09? MWjlcohidmOnczDic5J1\XqxbXniMYlv\HWlZXSgZ4VtdCC4aXHibYxqfHlibH;zdy=> MoPJNlQ5PDJzNUi=
Microglia  M2X0WGFxd3C2b4Ppd{BCe3OjeR?= M4XLe|VuVQ>? NUjCd|RCOjSq MmnM[IVkemWjc3XzJIh6eG:6aXGtbY5lfWOnZDDj[YxtKGSnYYTo NV;FT2pPOjR6MUi2NFE>
A2780cp NE\4fYFCeG:ydH;zbZMhSXO|YYm= NFrMPG0zNjWvTR?= MlOwNYg> NELl[Gll\Eh{Tx?= M1XCd4VvcGGwY3XzJINqe3CuYYTpck1qdmS3Y3XkJINmdGxiZHXheIg> MVmyOFgyPzl2Nh?=
HepG2 M{LBbmZ2dmO2aX;uJGF{e2G7 M3;CcFVuVQ>? NHPpdnM1cA>? MVXpcoNz\WG|ZYOgTGwhemWuZXHz[S=> M{TpTFI1PzF|NUi3
A549 NFrPcotCeG:ydH;zbZMhSXO|YYm= MoLmOY1O MWS0PIg> NHToUopl\WO{ZXHz[ZMhfGinIIDldoNmdnSjZ3Wgc4Yh[2WubDDk[YF1cCCjbnSg[ZhxemW|c3nvckBt\X[nbIOgc4Yh[2G|cHHz[U0{NCCEZXPsbY4uOSCjbnSgUGM{NUmL NEPMcoYzPDdyNkOwNy=>
U2OS MWTBdI9xfG:|aYOgRZN{[Xl? MY[xNI1O NEfsNHkzPGh? NVi4THZYcW62ZX7zbYZq\XNidHjlJIdzd3e2aDDpcohq[mm2aX;uJI9nKHSqZTDVNm9UKGOnbHzzJIlv\HWlZXSgZpkhTG:6 MUmyOFY{QTBzMx?=
Saos-2 NWTtVY9tSXCxcITvd4l{KEG|c3H5 M2Lsb|ExdU1? NH74[4QzPGh? NFjEbWFqdnSnboPp[olmeyC2aHWg[5Jwf3SqIHnubIljcXSrb36gc4YhfGinIGWyU3Mh[2WubIOgbY5lfWOnZDDifUBFd3h? M2exRVI1PjN7MEGz
A549 MYnBdI9xfG:|aYOgRZN{[Xl? NEn6W48yOG2P M4fzZlQ5cA>? Mn3HZYNk\WyncnH0[ZMhfGinIILl[JVkfGmxbjDv[kBk\WyuII\pZYJqdGm2eTDpcoR2[2WmIHL5JHBVYA>? NFPrdm0zPDZ{NkeyNi=>
HCT116  M4[wNmFxd3C2b4Ppd{BCe3OjeR?= M1jyZlVuVQ>? Mo\JNlRp NU\KfI1[\W6qYX7j[ZMhfGinIHHwc5B1d3OrczDpcoR2[2WmIHL5JIFxcWenbnnu M4LF[FI1PjJ4NUKy
HGC-27 MV7GeY5kfGmxbjDBd5NigQ>? NFnpPI8yOG2P NFTW[|QycA>? NWftPFVQcW6qaXLpeJMhfGinIHPlcIwhfmmjYnnsbZR6KGyxc4OgZpkhWkGGMECxJI9zKE2NLUKyNFY> MUSyOFQyPjN2OR?=
U2OS  MVvGeY5kfGmxbjDBd5NigQ>? M4T0fVAvPS9zbV2= MkmyOFhp M{n5fYlv\HWlZYOgd4FtcW6xbYnjbY4ucW6mdXPl[EBk\WyuII\pZYJqdGm2eTDsc5N{ MWGyOFM2QDN2Mh?=
MG-63 Mke4SpVv[3Srb36gRZN{[Xl? M{LBVlAvPS9zbV2= NGLNV4M1QGh? MnHsbY5lfWOnczDzZYxqdm:veXPpck1qdmS3Y3XkJINmdGxidnnhZoltcXS7IHzvd5M> M{XYTlI1OzV6M{Sy
MG-63 NGP1boRCeG:ydH;zbZMhSXO|YYm= MUOwMlUwOW2P NXjCNGZ6OzKq M17EeIVvcGGwY3XzJJNidGmwb335Z4lvNWmwZIXj[YQh[2WubDDhdI9xfG:|aYO= MVWyOFM2QDN2Mh?=
MG-63 M{TyO2Fxd3C2b4Ppd{BCe3OjeR?= MmWxNVBuVQ>? NVjCbFlCOTKq M3PuUoVvcGGwY3XzJGRRNWmwZIXj[YQh[XCxcITvd4l{ MV2yOFM2QDNyMR?=
NTUB1 MXvBdI9xfG:|aYOgRZN{[Xl? M33OUlVuVQ>? NGLWdGMyNjWq M{mwS5BwfGWwdHnheIV{KGOnbHXjc5hq[i2rbnT1Z4VlKGGyb4D0c5Nqew>? M{Sxd|I1OzR7MUe2
T24 NUnr[oltSXCxcITvd4l{KEG|c3H5 M{C3RlVuVQ>? MVyxMlVp M37XWpBwfGWwdHnheIV{KGOnbHXjc5hq[i2rbnT1Z4VlKGGyb4D0c5Nqew>? NVfjR5k{OjR|NEmxO|Y>
SGC-7901  NIq4OpdCeG:ydH;zbZMhSXO|YYm= NUThN5hmOm2P MojQNYg> M4DIZYlv[3KnYYPld{BESS12IHnu[JVk\WRiYYDvdJRwe2m| MkHrNlQ{OjF|NEC=
SMMC-7721 NWTPeGk5SXCxcITvd4l{KEG|c3H5 MnvwNo1O NYXxU2dyOWh? M1KyPYlv[3KnYYPld{BESS12IHnu[JVk\WRiYYDvdJRwe2m| M3y5OVI1OzJzM{Sw
ECSCs  MkXNRZBweHSxc3nzJGF{e2G7 M4O4R|ExdU1? MoH6OIg> MkXL[IVkemWjc3XzJJJieGGveXPpck11emWjdHXkJIFxd3C2b4Ppdy=> M{DKb|I1OzF7MUC5
MCF-7  MYXGeY5kfGmxbjDBd5NigQ>? MlnMNVBuVQ>? MXWyOIg> M{PMZYlvcGmkaYTzJJRp\SCjdYTvdIhi\3liaX7keYNm\CCkeTDjbIVud3SqZYLhdJkh\HK3Z4O= MXGyOFMyPTV5OB?=
UOK257 NEnnZWxCeG:ydH;zbZMhSXO|YYm= M2XibFVuVQ>? NVfJW29ZO2h? NXfBNXo2\W6qYX7j[ZMheGGlbHn0ZZhmdC2vZXTpZZRm\CCjcH;weI9{cXQEoB?= M4D2UVI1OzB3NkC0
ACHN-5968 NIPqcWZCeG:ydH;zbZMhSXO|YYm= M3rZZlVuVQ>? NF;zZ5E{cA>? NIDTZpRmdmijbnPld{Bx[WOuaYThfIVtNW2nZHnheIVlKGGyb4D0c5Nqe8Li NWjaUGNROjR|MEW2NFQ>
Huh7 MXTBdI9xfG:|aYOgRZN{[Xl? M4f1cVJuVQ>? MVGxNog> MnXDSG1UVw>? MnXibY5pcWKrdIOgRXpFQDB3NT3pcoR2[2WmIHPlcIwh\GWjdHi= MlW3NlQzQTd|MEC=
Hep3B NG\NTWVCeG:ydH;zbZMhSXO|YYm= NI\oVFQzdU1? NWPZOopGOTKq MWTEUXNQ NX34bm9tcW6qaXLpeJMhSVqGOEC1OU1qdmS3Y3XkJINmdGxiZHXheIg> NIrmSYQzPDJ7N{OwNC=>
RKO MXvGeY5kfGmxbjDBd5NigQ>? MnXrNo1O MV[xbC=> M4\iZ2ROW09? MkC2[Y5p[W6lZYOgZ4VtdCCmZXH0bEBjgSCpZXzkZY5idXmlaX6= NUjGRWVzOjR{OUG3O|c>
HepG2 E47 NFnMeXFHfW6ldHnvckBCe3OjeR?= M{PFOlIvPW2P M{PMVVQ5cA>? NFW3TYtqdmO{ZXHz[ZMhfGinIITvfIlkcXS7IH;mJGFCNCCEU1:sJIFv\CCFQ3y0 MnT2NlQzPzN5M{i=
LoVo  NGe2ZWJCeG:ydH;zbZMhSXO|YYm= M1:0OlVuVQ>? MV60PIg> NH\vO3hmdmijbnPld{BFS0FvaX7keYNm\CCjcH;weI9{cXNw M{X6O|I1OjBzOEGy
WiDr M3XsbGZ2dmO2aX;uJGF{e2G7 MoLONVBuVQ>? NXGzUFZROWh? MYnpcohq[mm2czDQR2JNNWmwZIXj[YQhVEN|IFnJJIV5eHKnc4Ppc44> MUeyOFE6ODR6OR?=
H1299  M37KfWZ2dmO2aX;uJGF{e2G7 MUmxNI1O MnHpOIg> NG\kUldqdmO{ZXHz[ZMh[2m|cHzheIlvNWmwZIXj[YQh[2WubDDk[YF1cA>? NIqwWoEzPDF5M{KwPC=>
H460 M3XSV2Z2dmO2aX;uJGF{e2G7 MUSxNI1O MnT4OIg> MXLpcoNz\WG|ZYOgZ4l{eGyjdHnuMYlv\HWlZXSgZ4VtdCCmZXH0bC=> NF\uV2EzPDF5M{KwPC=>
A549 MWnGeY5kfGmxbjDBd5NigQ>? NUjwc4FbOTCvTR?= M2rUTFRp MWLpcohq[mm2czDheZRweGijZ4mgbY5lfWOnZDDifUBqenKjZHnheIlwdg>? NYntPVNMOjRzNEK3N|U>
Hep3B M{PwSmFxd3C2b4Ppd{BCe3OjeR?= NFnyTYc2dU1? NUD4NnhQOjSq MnHsZZR1\W63YYTld{BVVkZvzsGgdJJwfGWldHnvckBi\2GrboP0JJNmenWvIIP0ZZJ3[XSrb36tcYVlcWG2ZXSgZZBweHSxc3nz NWTPcFZoOjRyNk[2PVM>
SMMC-7721 MWLBdI9xfG:|aYOgRZN{[Xl? NYTx[npoPW2P NFz4b3MzPGh? MYnheJRmdnWjdHXzJHRPTi4QsTDwdo91\WO2aX;uJIFo[Wmwc4Sgd4VzfW1ic4ThdpZifGmxbj3t[YRq[XSnZDDhdI9xfG:|aYO= NGPESFgzPDB4Nk[5Ny=>
HO8910 M{L3S2Fxd3C2b4Ppd{BCe3OjeR?= NWTZOWlGOTCvTR?= M1rKZ|EzcA>? NXfKfVhw\W6qYX7j[ZMhSjF7LXnu[JVk\WRiYYDvdJRwe2l? NGHtdlMzOzl6M{[xNC=>
MCF7 NWPVfWg3TnWwY4Tpc44hSXO|YYm= MmrXOY1O M3PSRVI1cA>? MoXLbY5kemWjc3XzJGN2VyCrbnT1Z4VlKGOnbHyg[IVifGh? MmPxNlM6PjJ4Mkm=
HONE-1  NVLDZnljTnWwY4Tpc44hSXO|YYm= M2L5elVuVQ>? NHKxN2UycA>? NWLpNplOemWycnXzd4V{KD[{LX3l[IlifGWmIGLPV{Bxem:mdXP0bY9v NIK5ZVczOzh7MkO1PC=>
HeLa MWrGeY5kfGmxbjDBd5NigQ>? NIm0[G0yOG2P M{nySVJp M1vm[JN2eHC{ZYPz[ZMhVEN|IFnJJIV5eHKnc4Ppd49v NFnSS40zOzh4NEezPC=>
HepG2 NIrrcYlHfW6ldHnvckBCe3OjeR?= NGH2TZUyOG2P MYeyOIg> M1PXT4lvcGmkaYTzJJNqXEmJQWKtJIFv\CCKQmPTMYlv\HWlZXSgZZV1d3CqYXf5 MnLxNlM5OTdyNEC=
SH-SY5Y Mor2SpVv[3Srb36gRZN{[Xl? MmfGNY1O MXSyOIg> Ml2wbY5pcWKrdIOgeIhmKGG3dH;wbIFogSCrbnT1Z4VlKGK7IGTPR3A> NGC0VmUzOzd2M{G0PC=>
SH-SY5Y M4HGN2Fxd3C2b4Ppd{BCe3OjeR?= MnOxOY1O NEL5TXEycA>? NU[wXZBU[WKxbHnzbIV{KGOnbHHzeJJwdCCwZYXyc5Bzd3SnY4TpeoUh\W[oZXP0 M2e5TlI{PjF7M{m1
PC12  M4X6OWZ2dmO2aX;uJGF{e2G7 M1W4R|ExdU1? NID3Z5EzPGh? NHHISoh4[XSnch?= MnrlxsBqdmirYnn0d{BkcHmvb4TyfZB{cW5vbHnr[UBxem:2ZXHzc41idCCjY4Tpeol1gS5? MWeyN|YxOzl5OR?=
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A2780 NUfSXFdxSXCxcITvd4l{KEG|c3H5 MkTROY1O M4X0O|I1cA>? NWLPcGZX[2:wdnXyeJMhTlS\N{KwJJdqfGhiQ1TEVEBqdnSxIHHuJIFl\Gm2aY\lJIVn\mWldDD0c5diemS|IHvpcIxqdmdib4\hdolidiClYX7j[ZIh[2WubIO= NF7oUmYzOzV7MkK4NS=>
Saos-2  MXTBdI9xfG:|aYOgRZN{[Xl? Mn36NY1O MmLOPVZp M3zQd4lv[3KnYYPld{Bk\WyuIHTlZZRpKGmwZIXj[YQh[nliUFPY M2W2NlI{PTZ|MUex
1321N1 MVLDfZRwfG:6aXPpeJkhSXO|YYm= M4XRcVVuVQ>? NFW3fpczPGh? MY\wdo91\WO2czDj[YxtKGGpYXnud5QhWEOQLXnu[JVk\WRidH;4bYNqfHl? NXjzeVdHOjN3MkWyOlU>
SH-SY5Y NFqwVnNEgXSxdH;4bYNqfHliQYPzZZk> M1\GeVVuVQ>? NETsNlQzPGh? NUnqUHgycW6lcnXhd4V{KFCFTjD0c5hq[2m2eR?= MV[yN|UzPTJ4NR?=
HT-29  M2HVOmZ2dmO2aX;uJGF{e2G7 Mo\qNY1O NEn3NWs1QC97Nni= MWjpcohq[mm2czDBUXBMKGmwZIXj[ZMh[XW2b4DoZYdq[yClZXzsJIRm[XSq NI\rbnQzOzVyOEK3Ni=>
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Hela  Mm\YSpVv[3Srb36gRZN{[Xl? M{L2VlVuVQ>? NHTKXpMzPGh? NXvJdnYxcW6qaXLpeJMhe3Sjco\heIlwdi2rbnT1Z4VlKGG3dH;wbIFogQ>? NHXPTpUzOzN7NU[3PS=>
MCF-7  Ml2wSpVv[3Srb36gRZN{[Xl? MWO1cW0> NGm4cZQzPGh? NHfWZnFqdmirYnn0d{B{fGG{dnH0bY9vNWmwZIXj[YQh[XW2b4DoZYd6 NWXrR3RqOjN|OUW2O|k>
HUVECs NVTLVmhmTnWwY4Tpc44hSXO|YYm= NF6zZVg{dU1? MXyyOIg> MXTicI9kc3NidHjlJJBzd3SnY4TpeoUh\W[oZXP0JI9nKHKnc4\ldoF1em:uIHL5JIlvcGmkaYTpcoch[XW2b4DoZYd6 NFr4cpUzOzN3OEmyPC=>
T24 M1raZ2Z2dmO2aX;uJGF{e2G7 NIj1W5cyOG2P NUDv[WJqOWh? NYHxXINGemWmdXPld{B1cGViY3zlZZZi\2Vib3[gUGM{KGGodHXyJIJicWOjbHnuJJRz\WG2bXXueC=> MlfBNlM{PTRyOEC=
U251MG  MWTGeY5kfGmxbjDBd5NigQ>? NXvYNZhLO22P MoHINYg> NWjMXHhUe3WycILld5NmeyCOQ{OtTWkheHKxdHXpckBmgHC{ZYPzbY9v M4G3WVI{OzN6NkG4
GTL-16  MneyRZBweHSxc3nzJGF{e2G7 MXm1cW0> MUCyOIg> NVKwR29LemWmdXPld{Bk\WyuII\pZYJqdGm2eTDhd{Bkd22yYYLl[EB1dyClZXzsd{B1emWjdHXkJJdqfGhiTVXUJIlvcGmkaYTvdpM> NVHkNmNjOjN|MUO0PVA>
T-47D M4G0fWZ2dmO2aX;uJGF{e2G7 NGfTZ44yOG2P NUPRbVhzOmh? MkTqbY5pcWKrdIOgZZV1d3CqYXf5JJBzd2Onc4OgZY5lKGmwY4LlZZNmeyC{YYDhcZlkcW5iaX7keYNm\CCjcH;weI9{cXN? NIXGcWszOzNyMECyOi=>
PaCa44 NEPvUppCeG:ydH;zbZMhSXO|YYm= NG\KZXczNjWvTR?= NYTUWIJyOWh? Mor5doVlfWOnc9Mg[4VvcXCrbj3t[YRq[XSnZDDhdI9xfG:|aYO= NFywbZYzOzF{NEGxNi=>
MDA-MB231 NVrvO2hyTnWwY4Tpc44hSXO|YYm= MknCOY1O MXGxbC=> MWDpcoNz\WG|ZYOgdoV{fmW{YYTyc4wudWWmaXH0[YQh[2G|cHHz[UBi[3SrdnH0bY9vKGGwZDDj[YxtKGSnYYTo NYHhdIJEOjNyOEi4OVA>
HeLa NILx[|FCeG:ydH;zbZMhSXO|YYm= Ml;FNVBuVQ>? M{PFTFJp M3u1UYRm[3KnYYPld{Bk\WyuII\pZYJqdGm2eTDjc{11emWjdH3lcpQhf2m2aDDQSWk> Mk\iNlMxODBzM{W=
SK-HEP-1 NGXzWGdCeG:ydH;zbZMhSXO|YYm= NEnUXoUyOG2P NYHmPZBzOWh? MUjwdo91\WO2czDh[4FqdnO2IHH1eI9xcGGpeTDhcoQhcW6mdXPld{BieG:ydH;zbZMhcW5iYoXmZYxqdi22cnXheIVlKGOnbHzz M1f4PVIzQDV6NkS5
HepG2 Ml\iRZBweHSxc3nzJGF{e2G7 MUizcW0> MWe1bC=> MXvy[YR2[2W|IHPlcIwh[XCxcITvd4l{KGmwZIXj[YQh[nliUVTz NVHEbHI3OjJ6M{[1PVU>
MCF-7  M1u2TWZ2dmO2aX;uJGF{e2G7 M1TaPFJuVQ>? MonjNlRp M2nQVolvcGmkaYTzJIF2fG:yaHHnfUBqdmS3Y3XkJIJ6KFSPwrC= MmDhNlQ6PzB4N{[=
MDA-MB-231 M4LP[GZ2dmO2aX;uJGF{e2G7 NVXzZWR5Om2P M{nuUlI1cA>? M1m5XYlvcGmkaYTzJIF2fG:yaHHnfUBqdmS3Y3XkJIJ6KFSPwrC= NILj[YkzPDl5ME[3Oi=>
MCF-7  M3nudGZ2dmO2aX;uJGF{e2G7 NXruNJc4Om2P NEXxWVI1QGh? NWfxSW8xeHKxbX;0[ZMhXE1vaX7keYNm\CClZXzsJIRm[XSq NELMb4gzPDl5ME[3Oi=>
MDA-MB-231 M33FW2Z2dmO2aX;uJGF{e2G7 M3zueVJuVQ>? NIHHXGo1QGh? NFrsTpJxem:vb4Tld{BVVS2rbnT1Z4VlKGOnbHyg[IVifGh? M2\SWVI1QTdyNke2
PANC-1  NFrHWm1CeG:ydH;zbZMhSXO|YYm= MY[xcW0> MlnpOFhp MVXEUXNQ MXHlcohidmOnczDic5J1\XqxbXniMYlv\HWlZXSgZ4VtdCC4aXHibYxqfHlibH;zdy=> MnXSNlQ5PDJzNUi=
MDA-MB 231 NIHYO45CeG:ydH;zbZMhSXO|YYm= NV;vSVNNPW2P M3jXRlAvPWh? NEj2e45ud2S3bHH0[ZMhXG:lb33pcuKvyqCrbnT1Z4VlKGGyb4D0c5Nqew>? Ml;RNlQ5OzB5OEG=
Microglia  MXjBdI9xfG:|aYOgRZN{[Xl? NIfH[Jo2dU1? NIOwN5czPGh? NUew[Y9o\GWlcnXhd4V{KGi7cH;4bYEucW6mdXPl[EBk\WyuIHTlZZRp NXy1RmlvOjR6MUi2NFE>
A2780cp NEnQWllCeG:ydH;zbZMhSXO|YYm= MkLsNk42dU1? MXuxbC=> MojN[IRJOk9? NW[xPWpr\W6qYX7j[ZMh[2m|cHzheIlvNWmwZIXj[YQh[2WubDDk[YF1cA>? MnvpNlQ5OTd7NE[=
HepG2 MUHGeY5kfGmxbjDBd5NigQ>? NGPMbYI2dU1? M2rNSlRp NFvt[ndqdmO{ZXHz[ZMh[2WubIXsZZIhdGW4ZXzzJI9nKEiOwrC= NVHBe|kyOjR5MUO1PFc>
U2OS NIrE[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfhNVBuVQ>? MnjJNlRp NUjWdlJEcW62ZX7zbYZq\XNidHjlJIdzd3e2aDDpcohq[mm2aX;uJIlv\HWlZXSgZpkhTG:6 MkfDNlQ3OzlyMUO=
HCT116 M1jjXmFxd3C2b4Ppd{BCe3OjeR?= MVy1cW0> M1;0VFI1cA>? NFjqWHNFVVOR NWD3c2g3\W6qYX7j[ZMh[XCrZ3XubY4ucW6mdXPl[EBk\WyuIHTlZZRp M3vEZVI1PjJ4NUKy
MCF-7  NIqzNZdCeG:ydH;zbZMhSXO|YYm= M3jH[lAvOW2P NV\pN5N{Pmh? NEPveHhmdmijbnPld{B{cXK2aX7vcE1qdmS3Y3XkJIFxd3C2b4Ppdy=> NVnZcW5wOjJ5NUG5PFk>
PC-3  NVe5WpY1SXCxcITvd4l{KEG|c3H5 NInSPIYzdU1? NUGxPFdiOmh? NEDiU3BqdmO{ZXHz[ZMhV1KLLXnu[JVk\WRiY3XscEBl\WG2aB?= NWH5TlFnOjJ5NEW1PFA>
U251  MVLBdI9xfG:|aYOgRZN{[Xl? M3PoO|VuVQ>? M4P4TVI1cA>? M4HBbIlv[3KnYYPld{BUOS2rbnT1Z4VlKGOnbHyg[IVifGh? M{[1TFIzPTd7N{i4
HeLa  NHvlTWZCeG:ydH;zbZMhSXO|YYm= NH3oR4o2dU1? MV[yOIg> MkXUbY5lfWOnczDjZZNx[XOnLXTldIVv\GWwdDDj[YxtKGSnYYTo MlPLNlI2PDVzMki=
A549 NVToPI9pTnWwY4Tpc44hSXO|YYm= NYXOW4ZrOC5zbV2= NG\kR2YzPGh? NXywZVd[e3WycILld5NmeyCVVUGxNlc1NWmwZIXj[YQh[2WubDDk[YF1cA>? NF\KOnAzOjR4Nkm2NC=>
pDCs NEPNO3pHfW6ldHnvckBCe3OjeR?= M3:1WlExdU1? MUiwMlVp MV|CpJJm\HWlZYOgeIhmKGmwZIXjeIlwdiCxZjDJSm4u|rFiYomgd5NTVkF2MB?= MV[yNlM6PjV7OR?=
BGC-823 MWTGeY5kfGmxbjDBd5NigQ>? NVPhO3NvPW2P M3rMdFJp MmGxbY5pcWKrdIOgeIhmKHKjdHWgc4Yh[XW2b4DoZYdq[yClZXzsdy=> MVGyNlMzOjF3Mh?=
U937 NVT4NoNwTnWwY4Tpc44hSXO|YYm= M2DLRlJuVQ>? MWqxNog> NGjUeJRl\WO{ZXHz[ZMhfGinIHH1eI9xcGGpeTDyZZRqd8Li NV3CS4t7OjJzNUWxOVA>
Marc-145 Ml7CSpVv[3Srb36gRZN{[Xl? NXi0PYJuPW2P MmTzNVIwOjRxM{\o MVHy[YR2[2W|IITo[UBRWlKVVjD0bZRmenNiYX7kJJRp\SCycn;0[YlvKGW6cILld5Nqd25? MY[yNlEyQTlyMB?=
HBx  NGfqOGVCeG:ydH;zbZMhSXO|YYm= MofsNVBuVQ>? MW[0PIg> MVnEUXNQ NVzjS5hqcW6lcnXhd4V{KGOnbHyg[IVifGh? MmTHNlIxOjByN{i=
MCF-7 M2HCSmZ2dmO2aX;uJGF{e2G7 NEDJTWoyOG2P Mlf2OFhp Ml7BZoxw[2u|IHH1eI9xcGGpeTDpcoR2[2WmIHL5JIJwenSnen;tbYI> NVvyd2d3OjF7M{G5N|c>
RMPI8226  M3PtemZ2dmO2aX;uJGF{e2G7 NVq5fYRxPW2P MoXENYg> M4nheZN2eHC{ZYPz[ZMhfGinIHzleoVtKG:oIHH1eI9xcGGpeTD1coRmeiCwdYTybYVvfCCmZYDs[ZRqd25? MYmyNVkyPTZ{MB?=
PC12/TetOn NEHnSoZHfW6ldHnvckBCe3OjeR?= Mlf0NE4yNzGvTR?= MnrlNVhp M4jGXIxm[WS|IITvJO6yNXO7bjjXWEkh[WOldX31cIF1cW:wLDD0c5hq[2m2eTygZY5lKG:uaXfvcYVzKG[xcn3heIlwdsLi NG\1VXczOTlyNk[1PS=>
HeLa  MWHDfZRwfG:6aXPpeJkhSXO|YYm= MUWycW0> NVXhcXk1OjSq NWDNNlIxcW6qaXLpeIV{KHSqZTDjfZRwfG:6aXPpeJkhd2Zic3nsbYJqdmmwIITvJGhmVGFiY3XscJMv MkHZNlE5PzV|OEW=
Jurkat NX\LelV[TnWwY4Tpc44hSXO|YYm= M2PiVFExdU1? MlTNNYg> NIXrV3Nl\WO{ZXHz[ZMhfGinIHX4dJJme3Orb36gc4YhVEN|LVnJJIFv\CC2aHWg[o9zdWG2aX;uJI9nKGG3dH;wbIFod3OxbXXz MlzmNlE5PjRyM{e=
K562 Mn3CSpVv[3Srb36gRZN{[Xl? M1LaUFExdU1? MWKxbC=> Ml3B[IVkemWjc3XzJJRp\SCneIDy[ZN{cW:wIH;mJGxEOy2LSTDhcoQhfGinIH\vdo1ifGmxbjDv[kBifXSxcHjh[49{d22ncx?= NXLOTGZuOjF6NkSwN|c>
Nara-H MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHtOY1O Mn;aOFhp NXqxRmgz\W6qYX7j[ZMhfGWvc3nyc4xqdXW|bXXkbYF1\WRic4XwdJJme3Orb36gc4YhVmG{YT3IJINmdGxicILvcIln\XKjdHnvci=> NXzYOFJ2OjF6MEWwN|M>
HUVECs MmHqSpVv[3Srb36gRZN{[Xl? MkDmNVBuVQ>? NInvXlgxNjWq M12wboRm[3KnYYPld{B1cGViQVfFMWJUSWmwZIXj[YQh[XW2b4DoZYd6KGyndnW= M{O5XlIyPDZ6NUmy
HepG2 NU\xTIdTSXCxcITvd4l{KEG|c3H5 NHv0ZZUzdU1? NYrlUVIxOWh? M1\aeIVvcGGwY3XzJJJi\GmjdHnvck1qdmS3Y3XkJINmdGxiZHXheIg> MVyyNVQ2OzZ7MR?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
α-SMA / TGF-β / LC-3BI / LC-3B II / Beclin-1 / NF-κB p65; 

PubMed: 29296191     


Western blotting analysed expression of α-SMA, TGF-β, LC-3B, Beclin-1, NF-κB and NF-κBp65 in hepatic stellate cells.

caspase-3 / caspase-9 / PARP; 

PubMed: 25891159     


EC9706 cell lysates were prepared and subjected to immunoblotting with antibodies against caspase-3, caspase-9 and PARP. The expression ratios in each experiment were determined densitometrically. The results are the averages of triplicate samples. Error bars represent the standard error.*P<0.05 vs. IR alone. 3-MA, 3-methyladenine; IR, ionizing radiation; PI, propidum iodide; PARP, poly(ADP ribose) polymerase.

VEGF; 

PubMed: 25891159     


Effects of autophagy inhibition on the protein expression levels of VEGF. Western blot analysis demonstrated that VEGF protein expression levels were decreased when the EC9706 human esophageal squamous cell carcinoma cells were treated with 3-MA. The results are the averages of triplicate samples. Error bars represent the standard error.*P<0.05 vs. IR alone. 3-MA, 3-methyladenine; IR, ionizing radiation; VEGF, vascular endothelial growth factor.

APP / BACE1 / ADAM17 / Presenilin 1 / Presenilin 2 / Nicastrin / APH-1 / Pen-2 / LC3-1 / LC3-2; 

PubMed: 26316755     


Presenilin 1, Nicastrin, and Pen-2 were increased with the 3-MA treatment (*P<0.001) while the other component of the γ-secretase complex (APH-1 and Presenilin 2) has no difference. 3-MA, 3-methyladenine; Con, control; APP, amyloid protein precursor.

29296191 25891159 26316755
Immunofluorescence
LC3 / Hif-α / COX2; 

PubMed: 29039446     


Chemical interventions of autophagy and ischemic-hypoxic injury, assessed using immunochemical double labeling. Compared with the control group, expression levels of HIF-α and COX2 were altered by chemical intervention. (A) Chemical intervention altered the expression of HIF-α and autophagosmes. Following autophagy antagonist (3-MA) intervention, expression of HIF-α was enhanced, compared with that in the OGD group, and was decreased by the autophagy agonist, rapamycin. In the MHY treatment group, expression of HIF-α was similar to that in the 3-MA group. (B) Chemical intervention showed changes in the expression of COX2 and autophagosomes. Changes in the expression of COX2 were similar to changes in HIF-α. Scale bar, 30 µm. OGD, oxygen-glucose deprivation; HIF-α, hypoxia-inducible factor-α; COX2, cyclooxygenase 2; 3-MA, 3-methyladenine; RP, rapamycin; MHY, MHY1485.

29039446
Growth inhibition assay
Cell viability; 

PubMed: 26934124     


KYSE 180 cells were co-treated with EDHB (40 μg/ml) and various concentrations of 3-MA for 24 h (left) or 48 h (right), and cell viability was determined by WST-8 assays.

26934124
体内研究 3-Methyladenine (3-MA)可以通过对磷酸肌醇3磷酸激酶(PI3K) 的作用来阻断自吞噬, 而PI3K的活性对于自噬体形成早期膜池的成核和组装是必须的。与SAH 处理组相比3-MA并不会改变出血的程度。与SAH +对照成分组相比经过3-MA预处理后会明显加重神经病学症状。3-MA处理会减少自吞噬发生[5]。 相反地,在SAH + 3-MA组里 断裂的半胱天冬酶表达量明显上调，与此一致的是与SAH + 对照成分组相比，SAH + 3-MA组中右脑皮层里原位末端标记阳性细胞数量明显增多[5]。

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：[4]
- 合并

Protein degradation assay:

HeLa cells are radiolabeled for 24 hours with 0.05 mCi/mL l-[U- 14C]valine. At the end of the labeling period, cells are rinsed three times with PBS. Cells are incubated for the designated times in either full medium or EBSS with or without the presence of 10 mM 3-Methyladenine.
细胞实验：[2]
- 合并
  • Cell lines: HeLa 细胞系
  • Concentrations: 1-10 mM
  • Incubation Time: 3 分钟
  • Method: 用台盼蓝染色法分析细胞存活率（如HeLa细胞）。简言之, 经过3-MA处理后将贴壁的与漂浮的细胞都用PBS( pH 7.4)重悬，密度控制在每毫升1-2×106。加入等体积的0.4% 台盼蓝并彻底混匀。室温孵育3分钟后用血细胞计数器对细胞计数分析。
    (Only for Reference)
动物实验：[5]
- 合并
  • Animal Models: 体重 300-350 g 的成年雄性Sprague–Dawley 大鼠
  • Formulation: 生理盐水配制
  • Dosages: 400 nM
  • Administration: 脑室给药
    (Only for Reference)

溶解度 (25°C)

体外 Water 10 mg/mL warmed (67.04 mM)
Ethanol 4 mg/mL (26.81 mM)
DMSO 3 mg/mL warmed (20.11 mM)

* 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 149.15
化学式

C6H7N5
CAS号 5142-23-4
储存条件 粉状
溶于溶剂
别名 NSC 66389

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：

    I'm also wondering whether it can be dissolved in water,or maybe something like culture medium,normal saline solution to form 10mM solution

  • 回答：

    As the reference (http://www.plosone.org/article/info%3Adoi%2F10.1371%2Fjournal. pone.0035665), 3-MA, which was found to inhibit autophagy at concentrations ranging from 1 to 10 mM was directly dissolved into the culture medium at the indicated concentrations. And we tested the solubility of S2767, and found the solubility of 3-MA in DMEM is 31 mg/mL at about 40°C.

Selleck产品目录册

PI3K Signaling Pathway Map

PI3K Inhibitors with Unique Features

相关PI3K产品

  • Taselisib (GDC 0032) New

    Taselisib (GDC 0032)是一种有效，下一代的β亚型PI3K抑制剂，作用于PI3Kα/δ/γ， IC50分别为0.29 nM/0.12 nM/0.97nM，比作用于PI3Kβ选择性高10倍以上。

  • Pilaralisib (XL147) New

    Pilaralisib (XL147)是一种选择性的可逆I型PI3K抑制剂，作用于PI3Kα/δ/γ，在无细胞试验中IC50为 39 nM/36 nM/23 nM，对PI3Kβ作用较低。Phase 1/2。

  • GNE-317 New

    GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。

  • LY294002

    LY294002 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。

    Features:LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。

  • Idelalisib (CAL-101, GS-1101)

    Idelalisib (CAL-101, GS-1101) 是选择性p110δ抑制剂，在无细胞试验中IC50为 2.5 nM；对 p110δ 表现出的选择性是对 p110α/β/γ 的 40 到 300 倍，对p110δ的选择性是对 C2β，hVPS34，DNA-PK 和 mTOR的400到4000倍。

    Features:Calistoga 暗示 CAL-101治疗血液恶性肿瘤可能有更广泛的应用价值。

  • Wortmannin

    Wortmannin是一种首次命名的PI3K抑制剂，在无细胞试验中IC50为3 nM，对 PI3K 家族的选择性较低。也会抑制自噬体的形成，并有效抑制DNA-PK/ATM，在无细胞试验中IC50为16 nM和150 nM。

  • Dactolisib (BEZ235)

    Dactolisib (BEZ235, NVP-BEZ235) 是一种双重ATP竞争性 PI3K 和 mTOR 抑制剂，在无细胞试验中，抑制 p110α/γ/δ/β 和 mTOR(p70S6K) 的 IC50 分别为 4 nM /5 nM /7 nM /75 nM /6 nM。 在 3T3TopBP1-ER 细胞中抑制 ATR，IC50 为 21 nM，而对 Akt 和 PDK1 的抑制作用很弱。Phase 2。

  • Buparlisib (BKM120)

    Buparlisib (BKM120, NVP-BKM120) 是一种选择性 PI3K 抑制剂，在无细胞试验中作用于p110α/β/δ/γ的IC50分别为 52 nM/166 nM/116 nM/262 nM。对 VPS34，mTOR，DNAPK 的作用效果下降，而对 PI4Kβ几乎没有活性。Phase 2。

    Features:BKM120是可用于口服的生物有效的PI3K抑制剂。

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941) 是一种有效的PI3Kα/δ抑制剂，在无细胞试验中IC50为 3 nM，对p110β (11倍)和p110γ (25倍)具有适度的选择性。Phase 2。

  • Alpelisib (BYL719)

    Alpelisib (BYL719) 是一种有效的选择性PI3Kα抑制剂，在无细胞试验中IC50为 5 nM，对PI3Kβ/γ/δ具有极弱的作用。Phase 2。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID