LY294002

For research use only.

Catalog No.S1105 Synonyms: SF 1101, NSC 697286

1102 publications

LY294002 Chemical Structure

Molecular Weight(MW): 307.34

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.

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Selleck's LY294002 has been cited by 1102 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Description LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Targets
p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)		 DNA-PK [6]
(Cell-free)
0.5 μM 0.57 μM 0.97 μM 1.4 μM
In vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells MXvD[YxtKGmwdnHzbY9vKGG|c3H5 MkDTNlQhcA>? NEHrdGFKdmirYnn0bY9vKG:oIHXwbZRp\WyrYXyg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGOnbHygcYloemG2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgdJJmNWmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JINmdGxiaX72ZZNqd25iYYPzZZktKEmFNUC9NE4{QCEQvF2u NWX5S4ZCOjJ6MESxNFg>
Sf21 cells NGjNd5lHfW6ldHnvckBie3OjeR?= NEPuU3dKdmirYnn0bY9vKG:oIH3veZNmKHerbHSgeJlx\SCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnOjFiY3XscJMh[29vZYjwdoV{e2mwZzDOMZRmem2rbnHsJGhqey22YXfn[YQhcHWvYX6gdFg2[SC3c3nu[{BNNWGucHjhMZBpd3OyaHH0bYR6dGmwb4PpeI9tKHO3YoP0doF1\SCkeTDUUGMh[mG|ZXSgdIhwe3Cqb4KgbY1i\2mwZzygTWM2OD1yLkWg{txO NH7scI8zOjV{ME[zNC=>
Sf21 cells MV7GeY5kfGmxbjDhd5NigQ>? M4rHXmlvcGmkaYTpc44hd2ZibX;1d4UhemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkKxJINmdGy|LDDJR|UxRTBwNTFOwG0v MV[xPVc1QDJ4OR?=
Sf9 cells NIj5VHlHdHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? NGD1[ohKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeTygTWM2OD1yLkW1JO69VS5? MlHJNlEyOjF4M{G=
THP1 cells NHrWR3pHfW6ldHnvckBie3OjeR?= M3v1bmlvcGmkaYTpc44hd2ZiU1PGNU1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJHRJWDFiY3XscJMtKEmFNUC9NU4xOSEQvF2u M4q0PFE3Pzh7N{Sy
human PC3 cells MlzvSpVv[3Srb36gZZN{[Xl? M{LsdVMxKG2rbh?= MmrHTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KHOncnnu[UA1PzNiYX\0[ZIhOzBibXnud{BjgSCHTFnTRUwhUUN3ME2xMlPPxE1w MlztNlM1OTByMEW=
HeLa (human carcinoma) cells. MYPGeY5kfGmxbjDhd5NigQ>? NXrXdYp[UW5idnn0do8hcW6qaXLpeIlwdiCxZjDEUmEu\GWyZX7k[Y51KHC{b4TlbY4hc2mwYYPlLGRPSS2SSzmg[pJwdSCKZVzhJEhpfW2jbjDjZZJkcW6xbXGpJINmdGy|LDDJR|UxRTFwNDFOwG0v MXixOVY2QDh5MB?=
THP1 cells Mn\FSpVv[3Srb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKE2FUEGtbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDUTHAyKGOnbHzzMEBKSzVyPUGuOlUh|ryPLh?= MYWxOlc5QTd2Mh?=
HeLa cells NFS2eG5HfW6ldHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKG2WT2KgdJJwfGWrbjDpd49t[XSnZDDmdo9uKEinTHGgZ4VtdHNuIFnDOVA:Oi53IN88UU4> MYmxOVY2QDh5MB?=
human MCF7 cells MkP0R5l1d3SxeHnjxsBie3OjeR?= MmHlR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVIvPjNizszNMi=> MWCxPFY6OTh7NB?=
HeLa cells MVvGeY5kfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKEG[LUe1NFMh[mmwZHnu[{B1dyC{ZXPvcYJqdmGwdDDQcIs{KGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIJ6KFenc4Tldo4h[myxdDygTWM2RTNizszNMi=> M1;QVFE4OTN3MkS4
human MCF7 cells MUfDfZRwfG:6aXRCpIF{e2G7 M{jk[WN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMhcW5icILld4Vv[2Vib3[gNVAhfU1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVMvODhizszNMi=> NV;jXXhOOTh4OUG4PVQ>
human MCF7 cells MUHDfZRwfG:6aXRCpIF{e2G7 NH7WO45EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k:Oy5zNjFOwG0v NGXXT2UyQDZ7MUi5OC=>
human MDA-MB-231 cells Mk\zR5l1d3SxeHnjxsBie3OjeR?= M3S1R2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMkCg{txOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l;Mz6zNkDPxE1w MUOxPFY6OTh7NB?=
human MDA-MB-231 cells NX3GXZFyS3m2b4TvfIlkyqCjc4PhfS=> MXvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD12LkO1JO69VS5? NFTvbmcyQDZ7MUi5OC=>
human MDA-MB-468 cells NEHsbm1EgXSxdH;4bYPDqGG|c3H5 NEPxdnNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4Phfg+9lCCLQ{WwQVQvPzZizszNMi=> M1K1dFE5PjlzOEm0
human HCT116 cells MoXpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGeyRm81QCCq NXnrUpk6T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT6zJO69VQ>? MWSyNlIyOjd{MR?=
human HCT116 cells NX;0TFM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYLsRmg2PDhiaB?= NVLFUphwT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IN88UU4> NVLw[mFJOjJ{MUK3NlE>
HeLa cells NEfiPWhDcW6maX7nJIFn\mmwaYT5JIF{e2G7 MkXpRolv\GmwZzDh[oZqdmm2eTDmc5IhWEl|LXvpcoF{\SCrc3;sZZRm\CCocn;tJGhmVGFiY3XscJMtKEurPU[g{txO M{[1bVE2PjV6OEew
human HCT116 cells M3jLPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnzZOFghcA>? MYrHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMhd3[ncnX4dJJme3OrbnegVGk{U2GucHjhJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63JO69VS5? NXPvcZk3OjJ{MUK3NlE>
MDA-MB-231 cells MYLDfZRwfG:6aXRCpIF{e2G7 M2jYU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvPzFizszNMi=> NXPBbHJYOTh4OUG4PVQ>
Sf9 cells M{XJXmZ2dmO2aX;uJIF{e2G7 M3vuZWlvcGmkaYTpc44hd2ZiQ1uyJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:Pi57IN88UU4> NXf0dGRVOTh|MkG3NVY>
human U87MG cells NHzz[oJHfW6ldHnvckBie3OjeR?= MnnJTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iVUi3UWch[2WubIOgZpkhTUyLU1GsJGlEPTB;OD6xJO69VS5? MX6xPFM1PTZyOR?=
human MDA-MB-468 cells NFfRZoJEgXSxdH;4bYPDqGG|c3H5 NYPzOIF2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{BqdiCycnXz[Y5k\SCxZjCxNEB2VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLNUC9PE4zKM7:TT6= NIfP[I8yQDZ7MUi5OC=>
human A375 cells MoHqVJJwdGmoZYLheIlwdiCjc4PhfS=> NH;re201PiCq NFW4VXlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiNE[gbJJ{NCCLQ{WwQVgvPCEQvF2u NH;RZ28yPzB2OUK0PC=>
human A375 cells Mm[4VJJwdGmoZYLheIlwdiCjc4PhfS=> NF3UZ4JKdmirYnn0bY9vKG:oIIPldpVuNWmwZIXj[YQheHKxbHnm[ZJifGmxbjDv[kBpfW2jbjDBN|c2KGOnbHzzMEBKSzVyPUiuOEDPxE1w MlTmNVc3ODF5M{m=
human HL60 cells NVPnOZFES3m2b4TvfIlkyqCjc4PhfS=> NX30c2k{PzJiaB?= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;OT65OEDPxE1w NEXWeHYzOjR6MEi1NS=>
mouse Raw264 macrophage MVvGeY5kfGmxbjDhd5NigQ>? Mln6TY5pcWKrdHnvckBw\iCFNXGtcYVlcWG2ZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gcY92e2ViUnH3NlY1KG2jY4LvdIhi\2VuIFnDOVA:OTBizszNMi=> NFvZc4syPjd6OUe0Ni=>
Sf9 cells MnHOSpVv[3Srb36gZZN{[Xl? M3vNO2lvcGmkaYTpc44hd2ZiSHnzMZRi\2enZDDic5ZqdmViUFmzT{BmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTFyIN88UU4> M4D2c|ExQTl6M{Wx
human MDA-MB-468 cells Mn7tR5l1d3SxeHnjxsBie3OjeR?= Mlf2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDifUBUWkJiYYPzZZktKEmFNUC9NVAvPCEQvF2u NXXFUG5YOTh4OUG4PVQ>
human PC3 cell MYTQdo9tcW[ncnH0bY9vKGG|c3H5 M3HLU|czKGh? NXj1U2xDUW6qaXLpeIlwdiCxZjDoeY1idiCSQ{OgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MUKuNUDPxE1w M1v2W|I{PDFyMEC1
human HL60 cells Mo\SVJJwdGmoZYLheIlwdiCjc4PhfS=> NEfFW2w4OiCq NWXuUnh2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUG4MlQ{KM7:TT6= MonvNlU3QTN5OEe=
human BT474 cell MmrTVJJwdGmoZYLheIlwdiCjc4PhfS=> M4HSb|czKGh? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGJVPDd2IHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nlic4DlZ5Rzd3Cqb4TvcYV1emmlIHHuZYx6e2m|78{MJGlEPTB;MkCuO{DPxE1w MofFNlM1OTByMEW=
THP1 cells MlLzSpVv[3Srb36gZZN{[Xl? NELpS4ZKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KG:oIGTIVFEh[2WubIOsJGlEPTB;M{eg{txONg>? MVKxOlc5QTd2Mh?=
human 184B5 cells NWHCcIlkS3m2b4TvfIlkyqCjc4PhfS=> MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxPFRDPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OzlwM{eg{txONg>? MWGxPFY6OTh7NB?=
human KB cells MnTpR5l1d3SxeHnjxsBie3OjeR?= NET0VY44OiCq NXPWZpBnS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20OE44PiEQvF2u M1PFUlIyQTR3MkWw
mouse RAW264.7 cells M4DOV2Z2dmO2aX;uJIF{e2G7 M{XvZ|I2KM7:TR?= NW\IfXFlOjBiaB?= M4\zU2lvcGmkaYTpc44hd2ZiUFmzT{9CU1RiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCrTl;TJJBzd3SnaX6g[ZhxemW|c3nvckBifCB{NTFOwG0h[W[2ZYKgNlAhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MWeyOFI6QTZzNh?=
human A2780 cells NWX6c2I4SXCxcITvd4l{KGG|c3H5 NV24XXRoOiEQvF2= MnzHNVIhcA>? NFzkRoRKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJINqe3CuYYTpck1z\XOrc4ThcpQhcHWvYX6gRVI4QDBiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1\WRiQXv0JIxmfmWuIHH0JFIhfU1iYX\0[ZIhOTJiaILzJIJ6KGmvbYXuc4Jtd3RiYX7hcJl{cXNw NEPjTo0yPzZ6NECxPC=>
human SW480 cells MXfGeY5kfGmxbjDhd5NigQ>? NWi2PFBLOjBizszN M1fkXFI1KGh? MkHJSIVkemWjc3WgbY4he3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCVV{S4NEBk\WyuczDheEAzOCC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= M3jrO|E4PDd{OU[y
mouse mast cells NEH0RYJHfW6ldHnvckBie3OjeR?= NGW5fpYzOCEQvF2= MXvJcohq[mm2aX;uJI9nKFOFRj3pcoR2[2WmIGDLRk9Cc3RicHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKG2jc4SgZ4VtdHNiYYSgNlAh|ryP M3PUTFE3Pzh7N{Sy
human BJ cells M2LBN2Z2dmO2aX;uJIF{e2G7 NFfLNo4zPSEQvF2= M3mwRlIhcA>? M2P6R2lvcGmkaYTpc44hd2ZiUFmzT{B{cWewYXzpcochcW5iUFTHSk1{fGmvdXzheIVlKHOncoXtJJN1[XK4ZXSgbJVu[W5iQlqgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCybHHzcYllKEWJRmCvVGgh\G:vYXnuJI9nKEGtdDDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDQTE1GT0[SIILl[Il{fHKrYoX0bY9vKHSxIIDsZZNu[SCvZX3idoFv\SCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDjc45nd2OjbDDtbYNzd3Olb4D5 MmnhNVY4PjdyOEW=
human IGROV1 cells NG\VRXFHfW6ldHnvckBie3OjeR?= NYnrfXp{OjRxNEigbC=> M2LpfGlvcGmkaYTpc44hd2ZiUFmzT{9Cc3RiaX6gbJVu[W5iSVfSU3YyKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDoc5NxcG:{eXzheIVlKEGNVDDs[ZZmdCCjdDCxJJRwKDVidHnt[ZMhUUN3MDDh[pRmeiB{NDD0c{A1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| M3TQdlIyOjF4MUWx
human IGROV1 cells Mn3MSpVv[3Srb36gZZN{[Xl? M3fZcVI1NzR6IHi= NH21TmZKdmirYnn0bY9vKG:oIGDJN2swSWu2IHnuJIh2dWGwIFnHVm9XOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDjfYNtcW5iREGgcIV3\WxiYYSgNUB1dyB3IITpcYV{KEmFNUCgZYZ1\XJiMkSgeI8hPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M2XtTFIyOjF4MUWx
rat RBL2H3 cells MmTvSpVv[3Srb36gZZN{[Xl? M{DnV2lvcGmkaYTpc44hd2ZiQUKzNVg4NWmwZIXj[YQh\GWpcnHueYxifGmxbjDpckBz[XRiUlLMNmg{KGOnbHzz NWLxWpZCOTh|Mki3NVY>
human BJ cells MmHISpVv[3Srb36gZZN{[Xl? MU[yOUDPxE1? NXLSRWxmOiCq NYXsbFE5SWO2aY\heIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFSqckOwPEBqdiCSRFfGMZN1cW23bHH0[YQhe2W{dX2gd5Rien[nZDDoeY1idiCESjDj[YxteyCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDpcY12dm:kbH;0eIlv\w>? NVjYPFBoOTZ5NkewPFU>
human HCT116 cells M4fRc2Z2dmO2aX;uJIF{e2G7 NUfsXJc4OTBizszN MXKxNEBucW5? Mlm1TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJJV{cW6pIGuzNnBeSVSSIHH0JFExKHWPIHHmeIVzKDFyIH3pcpM> M3m5fFIzOjF{N{Kx
human HCT116 cells MlLHSpVv[3Srb36gZZN{[Xl? NF3jSJQyOCEQvF2= NE[xTGgyOCCvaX6= NXizWG81UW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgTFExPDeUIH31eIFvfCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgeZNqdmdiW{OyVH1CXFBiYYSgNVAhfU1iYX\0[ZIhOTBibXnudy=> MX[yNlIyOjd{MR?=
human HCT116 cells MXzGeY5kfGmxbjDhd5NigQ>? NVexW4pyOTBizszN MXvJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDifUBqdW23bn;icI91KGGwYXz5d4l{ NWHFN3VOOjJ{MUK3NlE>
human HCT116 cells Mlv3SpVv[3Srb36gZZN{[Xl? MVuxNEDPxE1? NEfFXVdKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDINVA1P1JibYX0ZY51KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHH0JFExKHWPIHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> M1m2cVIzOjF{N{Kx
human PC3 cells MkPBSpVv[3Srb36gZZN{[Xl? NV[5bZRZPTBizszN NGTDS2E5KGh? MULJcoR2[3Srb36gc4YheDJzIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBpfW2jbjDQR|Mh[2WubIOgZZQhPTBidV2gbY5kfWKjdHXkJIZweiB6IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKHKnbHH0bZZmKHSxIIXueJJm[XSnZDDjc451em:u MYeyNlk6QDR5Mh?=
human LNCAP cells NIm3VphHfW6ldHnvckBie3OjeR?= MVuwMlEuOzBizszN MmnyN|AhdWmw Mki0TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFzOR2FRKGOnbHzzJIF1KDBwMTD0c{A{OCC3TTDh[pRmeiB|MDDtbY5{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> Mo\TNlI5OzJ|MU[=
human LNCAP cells MXvGeY5kfGmxbjDhd5NigQ>? NFjobo4xNjFvM{Cg{txO NHi3NWszPCCq M2TOd2Rwf26{ZXf1cIF1cW:wIH;mJJN2en[rdnnuJIV5eHKnc4Ppc44hcW5iaIXtZY4hVE6FQWCgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NYjsRYVsOjJ6M{KzNVY>
HUVEC NFnDUWFHfW6ldHnvckBie3OjeR?= NYSw[2d3OTBvMkWg{txO MkTHNVYhcA>? NX3vemtTUW6qaXLpeIlwdiCxZjDUUmZidHCqYT3zeIlufWyjdHXkJGlESU1vMTDtVm5CKGW6cILld5Nqd25iaX6gTHVXTUNiYYSgNVAhfG9iMkWgeW0heHKndILlZZRm\CCob4KgNVYhcHK|IHLl[o9z\SCWTl\hcJBp[SClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPiCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz MX:yNlAzPjRzMB?=
HUVEC MoDwSpVv[3Srb36gZZN{[Xl? NEewPIMyOC1{NTFOwG0> MkT2N|AhdWmw MXrJcohq[mm2aX;uJI9nKFSQRnHsdIhiNXO2aX31cIF1\WRiaIXtZY4hUUODTT2xJJBzd22xdHXyJIFkfGm4aYT5JIV5eHKnc4Pl[EBqdiCKVW\FR{Bie3Onc4Pl[EBieyCkZYThMYdidGGldH;zbYRie2ViYXP0bZZqfHliYYSgNVAhfG9iMkWgeW0heHKndILlZZRm\CCob4KgN|AhdWmwczDi[YZwemViVF7GZYxxcGFiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MVWyNlAzPjRzMB?=
human H1299 cells NUf1OVZXTnWwY4Tpc44h[XO|YYm= M1y5NlAvOS1|MDFOwG0> MoTtNlQhcA>? NEjueHFFd3ewIILl[5Vt[XSrb36gc4Yh[0mDUEKg[ZhxemW|c3nvckBqdiCqdX3hckBJOTJ7OTDj[YxteyCjdDCwMlEhfG9iM{CgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NYL1[pZLOjJ4MkKwOlk>
human H1299 cells M3XT[2Z2dmO2aX;uJIF{e2G7 NXPsUZhZOC5zLUOwJO69VQ>? NH3RPYMzPCCq M{DocGRwf25icnXneYxifGmxbjDv[kBkUUGSMjDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJFExOCC3Zz;tcEBVWkGLTDDhcoQhWEl|SzDpcohq[mm2b4KgUHkzQTRyMEK= MVmyNlYzOjB4OR?=
human H1299 cells NIrjelFHfW6ldHnvckBie3OjeR?= MVGwMlEuOzBizszN NX3t[lF{OjRiaB?= NFX4WpZKdmS3Y4Tpc44hd2ZiRGK1JIV5eHKnc4Ppc44hcW5iaIXtZY4hUDF{OUmgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NYHFXINOOjJ4MkKwOlk>
human H1299 cells Mn\BSpVv[3Srb36gZZN{[Xl? MmP1NE4yNTNyIN88US=> MUKyOEBp M3nrc2lv\HWldHnvckBw\iCMTlutcYVlcWG2ZXSgR2hQWCCneIDy[ZN{cW:wIHnuJIh2dWGwIFixNlk6KGOnbHzzJIF1KDBwMTD0c{A{OCC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MVKyNlYzOjB4OR?=
HEK293 cells NV;6dG1WTnWwY4Tpc44h[XO|YYm= NXzneG5tOS53IHi= MX7EbZNxdGGlZX3lcpQhd2ZiW{PIYWxUTCCocn;tJIh2dWGwIEXIWFYhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bi\nSncjCxMlUhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o NELySXUzOjV|N{G1Ny=>
human U251HRE cells MmC1SpVv[3Srb36gZZN{[Xl? NXnTUZRVUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKFV{NUHIVmUh[2WubIOgZpkh[2WubDDiZZNm\CC{ZYDvdpRmeiCpZX7lJIF{e2G7 NFziSWoyQDVyMU[wNS=>
human HCT116 cells MXLGeY5kfGmxbjDhd5NigQ>? MVGxNEDPxE1? M2fRUWlvcGmkaYTpc44hd2ZiQXv0JIV5eHKnc4Ppc44hcW5iaIXtZY4hUEOWMUG2JINmdGy|IHH0JFExKHWPIHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> MYqyNlIyOjd{MR?=
Sf9 cells M4W4bIZtfW:{ZYPj[Y51KHCxbHHybZpifGmxbjDhd5NigQ>? NFHBO2lKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= NIT4cnQzOTF{MU[zNS=>
human HCT116 cells NFz0SG9Rem:uaX\ldoF1cW:wIHHzd4F6 MYO3NkBp MkXURY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NUGuPFIh|ryPLh?= NYO3fmpxOjV4OUO3PFc>
human HCT116 cells MWfDfZRwfG:6aXRCpIF{e2G7 NU\ZfnZUPzJiaB?= MlHkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVYvODFizszNMi=> MWOyNVk1PTJ3MB?=
human PC3 cells MmT6R5l1d3SxeHnjxsBie3OjeR?= MX63NkBp NXu2[HlWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OlEvOzVizszNMi=> MYWyNlQ5ODh3MR?=
human HuH7 cells MnHoVJJwdGmoZYLheIlwdiCjc4PhfS=> M3XPZVczKGh? MlLGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZ5LkG4JO69VS5? NUSy[ZhMOjV4OUO3PFc>
human A549 cells NXHzW|NjWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1;3NlczKGh? M4rFTWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD16Mj6zNkDPxE1w NHTCcZYzPTZ7M{e4Oy=>
human A549 cells M2\LdGN6fG:2b4jpZ:Kh[XO|YYm= MWO3NkBp MlLOR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 NVSwPXJJOjJ2OEC4OVE>
human PC3 cells NGjXR5BRem:uaX\ldoF1cW:wIHHzd4F6 M3\OTFI2KM7:TR?= NW\pdXlUOTJyIHi= NWe0XJpFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZZQhOjVidV2gZYZ1\XJiMUKwJIhzeyCkeTDNWHQh[XO|YYmgdoVt[XSrdnWgeI8hTE2VTx?= M4Dae|E3PjhyMUW5
human H460 cells Mn7jSpVv[3Srb36gZZN{[Xl? MXyzNEDPxE1? MYDJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmeiB2N{OgeZAhfG9iM{CgeW0> MVmxPFUxOTZyMR?=
human IGROV1 cells MmfOSpVv[3Srb36gZZN{[Xl? NUjKSHBHOjRiaB?= M2P0TGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgNUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 NU[2ZWRJOjF{MU[xOVE>
human IGROV1 cells MYPGeY5kfGmxbjDhd5NigQ>? NI[y[nUzPCCq M4HzO2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgOUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 NWPJ[Ip3OjF{MU[xOVE>
human H4 cells NF7HbGZHfW6ldHnvckBie3OjeR?= NV\xSJVGOiCq NFPMcFBF\WO{ZXHz[UBqdiCIWW\FMXJHWCtidnXzbYNt\SCrboTlcpNqfHlicHXyJINmdGxiaX6gbJVu[W5iSESgZ4VtdHNiYX\0[ZIhOiCqcoOgdoVt[XSrdnWgeI8h[2:wdILvcC=> MWCxPFAzPDV6NB?=
human MGC803 cells MYLGeY5kfGmxbjDhd5NigQ>? MYCyOUDPxE1? NEi5Npc1QCCq M{\EXGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJG1ISzhyMzDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{KvUUBxcGG|ZTDheEAzPSC3TTDh[pRmeiB2ODDodpMhfXOrbnegdJJweGmmaYXtJIlw\GmmZTDzeIFqdmmwZzDh[pRmeiB2ODDodpMh[nliZnzve{BkgXSxbXX0[ZIhemWuYYTpeoUhfG9iY3;ueJJwdA>? M4T5VlI1OTF7OE[5

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
E-cadherin / p-Akt / Akt; 

PubMed: 29731993     


Immunoblot analysis of E-cadherin, P-AKT, and AKT in SNU-C5/5-FU cells treated with LY294002 (20 μM).

beta-catenin / p-GSK3β / Cyclin D1; 

PubMed: 29731993     


Immunoblot analysis of P-AKT, AKT, β-catenin, P-GSK-3β, GSK-3β, and cyclin D1 in SNU-C5/5-FU cells treated with LY294002 (20 μM).

Bcl-xl / Bax / caspase3 / cleaved caspase-3; 

PubMed: 25344912     


Four esophageal cancer cell lines were treated with different concentrations of LY294002 for 48 h, and cell lysates were collected for Western blot analysis of p-AKT, AKT, p-GSK3β, GSK3β, Bcl-xL, Bax, caspase-3, and cleaved caspase-3.

p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin; 

PubMed: 23251002     


HT29, Colo205, and RKO cells were treated for 2 h with PLX4720, LY294002 or their combination at indicated concentrations. Cell lysates were subjected to western blot analysis with antibodies against phosphorylated or total forms of AKT or ERK1/2, and antibodies against p-P70S6K, pGSK3β or vinculin.

pPKB-S473; 

PubMed: 20649566     


Typical Western blot showing that basal pPKB-S473 was reduced by increasing concentrations of LY294002 (upper panel). Pre-incubating 10 µM of the MEK-1/2 inhibitor U0126 induced pPKB–S473 levels which were reduced when rising concentrations of LY294002 were added. A full suppression of pPKB–S473 below the detection limit was seen at 30 µM PI3K inhibitor (10 µM U0126 + 30 µM LY294002). β-Actin immunoreaction served as loading control.

29731993 25344912 23251002 20649566
Growth inhibition assay
Cell viability; 

PubMed: 25344912     


MTT assay was used to determine the effects of different concentrations of LY294002 on viability of esophageal cancer cells lines KYSE150, HKESC-1, KYSE270, and T.Tn. Bars, SD; * P < 0.05; **, P < 0.01; ***, P < 0.001 compared with DMSO-treated cells.

25344912
Immunofluorescence
α-SMA / CD31; 

PubMed: 27671604     


Immunofluorescence analysis for the expression levels of CD31 and α-SMA in Control, LY294002, As2O3 and As2O3 + LY294002 groups. Scale bar = 30 μm. (in HAECs).

E-cadherin / beta-catenin; 

PubMed: 29731993     


The localization of E-cadherin and β-catenin were confirmed by confocal microscopy. Scale bars, 20 μm.

COX-2 / p-NFκB; 

PubMed: 29731993     


The localization of Cox-2 and P-NF-κB was confirmed by confocal microscopy. Scale bars, 20 μm.

FOXO3a; 

PubMed: 18388194     


C2C12 cells were plated into two-well chamber sliders for 24 h and then treated with 20 μm LY294002 or the same amount of vehicle (ethanol) for 16 h. Cells were fixed and FOXO3a was stained. LY294002 treatment activates FOXO3a and leads its translocation into the nucleus.

27671604 29731993 18388194
ELISA
IL-10 / IL-1β / TNFα / IL-6; 

PubMed: 22208359     


Microglial cells were pre-treated with LY294002 for 1 h and then stimulated with LPS (100 ng/ml) or PIC (10 μg/ml) for 16 h. ELISA were performed. All values were normalized to those obtained in cultures stimulated with LPS or PIC without LY294002 (= 1). At least 3 cases were analyzed for each experiment, and statistics were performed using t-test comparing values with vs. without LY294002.

22208359
In vivo LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]

Protocol

Kinase Assay:

[4]
- Collapse

kinase assays:

PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.
Cell Research:

[2]
- Collapse
  • Cell lines: Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
  • Concentrations: 0–50 μM
  • Incubation Time: 0–48 hours
  • Method:

    1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.


    (Only for Reference)
Animal Research:

[3]
- Collapse
  • Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
  • Dosages: 0–100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (117.13 mM)
Ethanol 21 mg/mL (68.32 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing. 		5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 307.34
Formula

C19H17NO3
CAS No. 154447-36-6
Storage powder
in solvent
Synonyms SF 1101, NSC 697286
Smiles O=C1C=C(OC2=C(C=CC=C12)C3=CC=CC=C3)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Frequently Asked Questions

  • Question 1:

    I want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of LY294002 (catalog no. s1105) says it will inactivates Akt/PKB. Is LY294002 available for Akt/PI3K inhibition?

  • Answer:

    LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. It can inhibit PI3K/AKT. PKB is the alternative name of AKT.

  • Question 2:

    What is the suggested formulation of this compound for mouse injection(i.p.)?

  • Answer:

    It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

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    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147) New

    Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.

  • GNE-317 New

    GNE-317 is a potent, brain-penetrant PI3K inhibitor.

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.

  • Idelalisib (CAL-101, GS-1101)

    Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.

  • Wortmannin

    Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.

  • Dactolisib (BEZ235)

    Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.

  • Buparlisib (BKM120)

    Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

  • Alpelisib (BYL719)

    Alpelisib (BYL719) is a potent and selective PI3Kα inhibitor with IC50 of 5 nM in a cell-free assay, and minimal effect on PI3Kβ/γ/δ. Phase 2.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID