LY294002

Catalog No.S1105 Synonyms: SF 1101, NSC 697286

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.

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In DMSO USD 191 In stock
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Cited by 273 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.
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 M2fiVGNmdGxiaX72ZZNqd25iYYPzZZk> M36zcVI1KGh? MYHJcohq[mm2aX;uJI9nKGWyaYTo[Yxq[WxiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJINmdGxibXnndoF1cW:wIH;mJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IHPlcIwhcW64YYPpc44h[XO|YYmsJGlEPTB;MD6zPEDPxE1w NX\hO|BCOjJ6MESxNFg>
Sf21 cells NH32VWlHfW6ldHnvckBie3OjeR?= NF7qOGxKdmirYnn0bY9vKG:oIH3veZNmKHerbHSgeJlx\SCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnOjFiY3XscJMh[29vZYjwdoV{e2mwZzDOMZRmem2rbnHsJGhqey22YXfn[YQhcHWvYX6gdFg2[SC3c3nu[{BNNWGucHjhMZBpd3OyaHH0bYR6dGmwb4PpeI9tKHO3YoP0doF1\SCkeTDUUGMh[mG|ZXSgdIhwe3Cqb4KgbY1i\2mwZzygTWM2OD1yLkWg{txO MoPWNlI2OjB4M{C=
Sf21 cells Ml62SpVv[3Srb36gZZN{[Xl? NEXSeZdKdmirYnn0bY9vKG:oIH3veZNmKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiU3[yNUBk\WyuczygTWM2OD1yLkWg{txONg>? MXexPVc1QDJ4OR?=
Sf9 cells NVXNN2g3Tmy3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 M3izbGlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxRTBwNUWg{txONg>? NWLuO5hTOjFzMkG2N|E>
THP1 cells M4PGTWZ2dmO2aX;uJIF{e2G7 MmT1TY5pcWKrdHnvckBw\iCVQ1[xMYlv\HWlZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gWGhROSClZXzsd{whUUN3ME2xMlAyKM7:TT6= NIPwV2MyPjd6OUe0Ni=>
human PC3 cells NVLQR5VXTnWwY4Tpc44h[XO|YYm= NF;kbZQ{OCCvaX6= MlXWTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KHOncnnu[UA1PzNiYX\0[ZIhOzBibXnud{BjgSCHTFnTRUwhUUN3ME2xMlPPxE1w MV[yN|QyODByNR?=
HeLa (human carcinoma) cells. MU\GeY5kfGmxbjDhd5NigQ>? MVrJckB3cXS{bzDpcohq[mm2aX;uJI9nKESQQT3k[ZBmdmSnboSgdJJwfGWrbjDrbY5ie2VqRF7BMXBMMSCocn;tJGhmVGFiKHj1cYFvKGOjcnPpco9u[SliY3XscJMtKEmFNUC9NU41KM7:TT6= M33te|E2PjV6OEew
THP1 cells MVnGeY5kfGmxbjDhd5NigQ>? M4riVWlvcGmkaYTpc44hd2ZiTVPQNU1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJHRJWDFiY3XscJMtKEmFNUC9NU43PSEQvF2u MUCxOlc5QTd2Mh?=
HeLa cells Mnq3SpVv[3Srb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKG2WT2KgdJJwfGWrbjDpd49t[XSnZDDmdo9uKEinTHGgZ4VtdHNuIFnDOVA:Oi53IN88UU4> NHPxWIQyPTZ3OEi3NC=>
human MCF7 cells M4ntbmN6fG:2b4jpZ:Kh[XO|YYm= NWTHeJYzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAzOCEQvF2gZ4htd3KxcYXpcoUh[nliU2LCJIF{e2G7LDDHTVUxRTJwNkOg{txONg>? M{KyblE5PjlzOEm0
HeLa cells MoCwSpVv[3Srb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKEG[LUe1NFMh[mmwZHnu[{B1dyC{ZXPvcYJqdmGwdDDQcIs{KGW6cILld5Nm\CCrbjDI[WxiKGOnbHzzJIJ6KFenc4Tldo4h[myxdDygTWM2RTNizszNMi=> M2fxblE4OTN3MkS4
human MCF7 cells NYjnUFNLS3m2b4TvfIlkyqCjc4PhfS=> NVrrTmZ7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAyOCC3TTDjbIxwem:zdXnu[UBjgSCVUlKgZZN{[XluIFfJOVA:Oy5yODFOwG0v NGfvNWUyQDZ7MUi5OC=>
human MCF7 cells MYDDfZRwfG:6aXRCpIF{e2G7 MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m9N{4yPiEQvF2u M4CxR|E5PjlzOEm0
human MDA-MB-231 cells MVLDfZRwfG:6aXRCpIF{e2G7 MYTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIN88UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKRTNwM{Kg{txONg>? M{HFO|E5PjlzOEm0
human MDA-MB-231 cells M3PKS2N6fG:2b4jpZ:Kh[XO|YYm= NGX1U|FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME20MlM2KM7:TT6= MVKxPFY6OTh7NB?=
human MDA-MB-468 cells NYPkTHZVS3m2b4TvfIlkyqCjc4PhfS=> M2nwS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMkCgeW0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H589yNKEmFNUC9OE44PiEQvF2u MUexPFY6OTh7NB?=
human HCT116 cells Mn7QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFflW|M1QCCq NVrsS|FvT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT6zJO69VQ>? NHPJXGIzOjJzMkeyNS=>
human HCT116 cells NWHsVnI6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;HOFghcA>? NVjCemlxT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IN88UU4> NXvNfGJ4OjJ{MUK3NlE>
HeLa cells NV2wdFdiSmmwZHnu[{Bi\m[rbnn0fUBie3OjeR?= NVzI[JdISmmwZHnu[{Bi\m[rbnn0fUBnd3JiUFmzMYtqdmG|ZTDpd49t[XSnZDDmdo9uKEinTHGgZ4VtdHNuIFvpQVYh|ryP MlPYNVU3PTh6N{C=
human HCT116 cells M4XQTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkjCOFghcA>? M{\NSmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCxdnXy[ZhxemW|c3nu[{BRUTONYXzwbIEh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22Mlch|ryPLh?= NYfI[4QxOjJ{MUK3NlE>
MDA-MB-231 cells MYXDfZRwfG:6aXRCpIF{e2G7 MlTWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok44OSEQvF2u MWWxPFY6OTh7NB?=
Sf9 cells Mn\1SpVv[3Srb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKEONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVYvQSEQvF2u MmrYNVg{OjF5MU[=
human U87MG cells NWLP[Yd2TnWwY4Tpc44h[XO|YYm= NHGxOmFKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDVPFdOTyClZXzsd{BjgSCHTFnTRUwhUUN3ME24MlEh|ryPLh?= M3G1NFE5OzR3NkC5
human MDA-MB-468 cells MnPoR5l1d3SxeHnjxsBie3OjeR?= NHzDeGJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME24MlIh|ryPLh?= NHm0fIwyQDZ7MUi5OC=>
human A375 cells NFTWSFVRem:uaX\ldoF1cW:wIHHzd4F6 MnTFOFYhcA>? NF;6VmlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiNE[gbJJ{NCCLQ{WwQVgvPCEQvF2u Ml63NVcxPDl{NEi=
human A375 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NHLIRmZKdmirYnn0bY9vKG:oIIPldpVuNWmwZIXj[YQheHKxbHnm[ZJifGmxbjDv[kBpfW2jbjDBN|c2KGOnbHzzMEBKSzVyPUiuOEDPxE1w NIjYTHoyPzZyMUezPS=>
human HL60 cells NEDjZXFEgXSxdH;4bYPDqGG|c3H5 MU[3NkBp NHLkSmtEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9PU46PCEQvF2u M2m5fVIzPDhyOEWx
mouse Raw264 macrophage NID6[41HfW6ldHnvckBie3OjeR?= NX6xSo9MUW6qaXLpeIlwdiCxZjDDOYEudWWmaXH0[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgVoF4OjZ2IH3hZ5JweGijZ3WsJGlEPTB;MUCg{txONg>? NHTnS|UyPjd6OUe0Ni=>
Sf9 cells NHzFTFdHfW6ldHnvckBie3OjeR?= MkOwTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIHLveolv\SCSSUPLJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:OTBizszNMi=> MljqNVA6QTh|NUG=
human MDA-MB-468 cells MkTrR5l1d3SxeHnjxsBie3OjeR?= Ml;WR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDifUBUWkJiYYPzZZktKEmFNUC9NVAvPCEQvF2u Mlf2NVg3QTF6OUS=
human PC3 cell NHfCUYtRem:uaX\ldoF1cW:wIHHzd4F6 NXrMSmpIPzJiaB?= MkPCTY5pcWKrdHnvckBw\iCqdX3hckBRSzNiY3XscEBxem:uaX\ldoF1cW:wIHHmeIVzKDd{IHjyd{BjgSC|cHXjeJJweGixdH;t[ZRzcWNiYX7hcJl{cXNuIFnDOVA:OTJwMTFOwG0v NXjIT5dlOjN2MUCwNFU>
human HL60 cells M{\MdnBzd2yrZnXyZZRqd25iYYPzZZk> M1zaR|czKGh? M17iOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zOD60N{DPxE1w NVPwemR5OjV4OUO3PFc>
human BT474 cell M{nodHBzd2yrZnXyZZRqd25iYYPzZZk> NV7pZlh1PzJiaB?= M{PwN2lvcGmkaYTpc44hd2ZiaIXtZY4hSlR2N{SgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYRvwKwhUUN3ME2yNE44KM7:TT6= MorhNlM1OTByMEW=
THP1 cells NInzR2pHfW6ldHnvckBie3OjeR?= M4\XfWlvcGmkaYTpc44hd2ZiTVPQNU1qdmS3Y3XkJINp\W2xdHH4bZMhd2ZiVFjQNUBk\WyuczygTWM2OD1|NzFOwG0v NUG1R3FHOTZ5OEm3OFI>
human 184B5 cells NXKxUXNNS3m2b4TvfIlkyqCjc4PhfS=> MorSR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gNVg1SjViY3XscJMh[nliU2LCJIF{e2G7LDDHTVUxRTN7LkO3JO69VS5? M4XWdlE5PjlzOEm0
human KB cells NITEZZlEgXSxdH;4bYPDqGG|c3H5 NWHuVoFUPzJiaB?= MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTR2Lke2JO69VS5? NYX6VY4xOjF7NEWyOVA>
mouse RAW264.7 cells MlXjSpVv[3Srb36gZZN{[Xl? NEHQOHAzPSEQvF2= MY[yNEBp MkK4TY5pcWKrdHnvckBw\iCSSUPLM2FMXCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2OgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDJ3IN88UUBi\nSncjCyNEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M1viRlI1Ojl7NkG2
human A2780 cells M1zEWGFxd3C2b4Ppd{Bie3OjeR?= MV2yJO69VQ>? NGjqT3gyOiCq MnLWTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDjbZNxdGG2aX6tdoV{cXO2YX70JIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDoc5NxcG:{eXzheIVlKEGtdDDs[ZZmdCCjdDCyJJVOKGGodHXyJFEzKGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{Ng>? MWqxO|Y5PDBzOB?=
human SW480 cells M{nJT2Z2dmO2aX;uJIF{e2G7 NH\xNo8zOCEQvF2= NU\oXJJsOjRiaB?= NHm3XZFF\WO{ZXHz[UBqdiC|dYL2bZZqdiCneIDy[ZN{cW:wIHnuJIh2dWGwIGPXOFgxKGOnbHzzJIF1KDJyIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz M2HXXFE4PDd{OU[y
mouse mast cells NILmRVdHfW6ldHnvckBie3OjeR?= NG\GOZczOCEQvF2= MmHOTY5pcWKrdHnvckBw\iCVQ1[tbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCvYYP0JINmdGy|IHH0JFIxKM7:TR?= MmfYNVY4QDl5NEK=
human BJ cells NGLmNVJHfW6ldHnvckBie3OjeR?= NELXdGczPSEQvF2= NXXEfJVmOiCq Mkj3TY5pcWKrdHnvckBw\iCSSUPLJJNq\26jbHnu[{BqdiCSRFfGMZN1cW23bHH0[YQhe2W{dX2gd5Rien[nZDDoeY1idiCESjDj[YxteyC2cnHud4Zm[3SnZDD3bZRpKHCuYYPtbYQhTUeIUD;QTEBld22jaX6gc4YhSWu2IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIGDIMWVITlBicnXkbZN1emmkdYTpc44hfG9icHzhd41iKG2nbXLyZY5mKGG2IEK1JJVOKHS{ZXH0[YQhOiCqcoOgZoVnd3KnIGDES2Yh[2ijbHzlcodmKGK7IHPvcoZw[2GuIH3pZ5Jwe2OxcIm= MoDiNVY4PjdyOEW=
human IGROV1 cells M{\rcGZ2dmO2aX;uJIF{e2G7 M{fpV|I1NzR6IHi= NVfNeolUUW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gdIhwe3Cqb4L5cIF1\WRiQVvUJIxmfmWuIHH0JFEhfG9iNTD0bY1meyCLQ{WwJIFnfGW{IEK0JJRwKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M1;DclIyOjF4MUWx
human IGROV1 cells NID1V25HfW6ldHnvckBie3OjeR?= NFnGZoEzPC92ODDo MXfJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCleXPsbY4hTDFibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NH31TFQzOTJzNkG1NS=>
rat RBL2H3 cells NW\HbGZ2TnWwY4Tpc44h[XO|YYm= Mm[5TY5pcWKrdHnvckBw\iCDMkOxPFcucW6mdXPl[EBl\We{YX71cIF1cW:wIHnuJJJifCCUQlyyTFMh[2WubIO= NYLVSZJOOTh|Mki3NVY>
human BJ cells NUK1OIJ6TnWwY4Tpc44h[XO|YYm= MoDzNlUh|ryP MlrJNkBp Mlf3RYN1cX[jdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHRpejNyODDpckBRTEeILYP0bY12dGG2ZXSgd4VzfW1ic4ThdpZm\CCqdX3hckBDUiClZXzsd{BifCB{NTD1UUB1emWjdHXkJFIhcHK|IHLl[o9z\SCSRFfGJINp[WyuZX7n[UBjgSCrbX31co9jdG:2dHnu[y=> Mn\MNVY4PjdyOEW=
human HCT116 cells NW\QZ|hWTnWwY4Tpc44h[XO|YYm= Mli4NVAh|ryP MXixNEBucW5? MonZTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJJV{cW6pIGuzNnBeSVSSIHH0JFExKHWPIHHmeIVzKDFyIH3pcpM> MYmyNlIyOjd{MR?=
human HCT116 cells MkDVSpVv[3Srb36gZZN{[Xl? MlvCNVAh|ryP MWmxNEBucW5? NV\4dXpLUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgTFExPDeUIH31eIFvfCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgeZNqdmdiW{OyVH1CXFBiYYSgNVAhfU1iYX\0[ZIhOTBibXnudy=> MUeyNlIyOjd{MR?=
human HCT116 cells MmfVSpVv[3Srb36gZZN{[Xl? M2f4XFExKM7:TR?= MW\Jcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDifUBqdW23bn;icI91KGGwYXz5d4l{ MWCyNlIyOjd{MR?=
human HCT116 cells M1\lN2Z2dmO2aX;uJIF{e2G7 NGrFdXEyOCEQvF2= NUDQc3ZFUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgTFExPDeUIH31eIFvfCCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDBb5QhW2W{NEezJJBpd3OyaH;yfYxifGmxbjDheEAyOCC3TTDifUBqdW23bn;icI91KGGwYXz5d4l{ NYezT4luOjJ{MUK3NlE>
human PC3 cells MVjGeY5kfGmxbjDhd5NigQ>? M4GzSlUxKM7:TR?= NX;LNYljQCCq MWnJcoR2[3Srb36gc4YheDJzIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBpfW2jbjDQR|Mh[2WubIOgZZQhPTBidV2gbY5kfWKjdHXkJIZweiB6IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKHKnbHH0bZZmKHSxIIXueJJm[XSnZDDjc451em:u Ml;iNlI6QTh2N{K=
human LNCAP cells NVTzUZBYTnWwY4Tpc44h[XO|YYm= M{LPUFAvOS1|MDFOwG0> NHq5PVQ{OCCvaX6= M4LDTWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiM{CgcYlveyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MVWyNlg{OjNzNh?=
human LNCAP cells NIexO4xHfW6ldHnvckBie3OjeR?= MUewMlEuOzBizszN MViyOEBp NFLpN3pFd3ewcnXneYxifGmxbjDv[kB{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHj1cYFvKEyQQ1HQJINmdGy|IHH0JFAvOSC2bzCzNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NEW1fWYzOjh|MkOxOi=>
HUVEC NYHPdpE1TnWwY4Tpc44h[XO|YYm= MVixNE0zPSEQvF2= M2TBUVE3KGh? M2jsbWlvcGmkaYTpc44hd2ZiVF7GZYxxcGFvc4TpcZVt[XSnZDDJR2FONTFibWLORUBmgHC{ZYPzbY9vKGmwIFjVWmVEKGG2IEGwJJRwKDJ3IIXNJJBz\XS{ZXH0[YQh\m:{IEG2JIhzeyCkZX\vdoUhXE6IYXzwbIEh[2ijbHzlcodmKG2nYYP1doVlKGGodHXyJFYhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= M4HCRVIzODJ4NEGw
HUVEC M4[4SmZ2dmO2aX;uJIF{e2G7 NYPzO4ZmOTBvMkWg{txO MoL0N|AhdWmw MoW1TY5pcWKrdHnvckBw\iCWTl\hcJBp[S2|dHnteYxifGWmIHj1cYFvKEmFQV2tNUBxem:vb4TldkBi[3Srdnn0fUBmgHC{ZYPz[YQhcW5iSGXWSWMh[XO|ZYPz[YQh[XNiYnX0ZU1o[WyjY4Tvd4ll[XOnIHHjeIl3cXS7IHH0JFExKHSxIEK1JJVOKHC{ZYTy[YF1\WRiZn;yJFMxKG2rboOgZoVnd3KnIGTOSoFteGijIHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB3IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYm= MYSyNlAzPjRzMB?=
human H1299 cells MVPGeY5kfGmxbjDhd5NigQ>? MoHQNE4yNTNyIN88US=> M2TVS|I1KGh? NULOPZk2TG:5bjDy[Yd2dGG2aX;uJI9nKGOLQWCyJIV5eHKnc4Ppc44hcW5iaIXtZY4hUDF{OUmgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MV6yNlYzOjB4OR?=
human H1299 cells MWXGeY5kfGmxbjDhd5NigQ>? M3HWbVAvOS1|MDFOwG0> NWjGc5ZTOjRiaB?= M3\TbWRwf25icnXneYxifGmxbjDv[kBkUUGSMjDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJFExOCC3Zz;tcEBVWkGLTDDhcoQhWEl|SzDpcohq[mm2b4KgUHkzQTRyMEK= MVKyNlYzOjB4OR?=
human H1299 cells MVrGeY5kfGmxbjDhd5NigQ>? NFvZV4QxNjFvM{Cg{txO NInZPHAzPCCq MUnJcoR2[3Srb36gc4YhTFJ3IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> Mm\ZNlI3OjJyNkm=
human H1299 cells MnHwSpVv[3Srb36gZZN{[Xl? NIHhVnoxNjFvM{Cg{txO MXOyOEBp MYDJcoR2[3Srb36gc4YhUk6NLX3l[IlifGWmIFPIU3Ah\XiycnXzd4lwdiCrbjDoeY1idiCKMUK5PUBk\WyuczDheEAxNjFidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MnHaNlI3OjJyNkm=
HEK293 cells MUfGeY5kfGmxbjDhd5NigQ>? NEfhSlEyNjViaB?= MUXEbZNxdGGlZX3lcpQhd2ZiW{PIYWxUTCCocn;tJIh2dWGwIEXIWFYhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bi\nSncjCxMlUhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o MoPMNlI2OzdzNUO=
human U251HRE cells NGnLS3hHfW6ldHnvckBie3OjeR?= M1PGO2lvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBWOjVzSGLFJINmdGy|IHL5JINmdGxiYnHz[YQhemWyb4L0[ZIh\2WwZTDhd5NigQ>? NIjBcnYyQDVyMU[wNS=>
human HCT116 cells NET0SXVHfW6ldHnvckBie3OjeR?= MUGxNEDPxE1? MVXJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MVSyNlIyOjd{MR?=
Sf9 cells NELBVYNndHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? NIXteoZKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= NHK3NWszOTF{MU[zNS=>
human HCT116 cells NIqzeG1Rem:uaX\ldoF1cW:wIHHzd4F6 NVnrc5lDPzJiaB?= NHfiVplCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIFje2:{YnHuZ4Uh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21NU45OiEQvF2u NY\JSIt2OjV4OUO3PFc>
human HCT116 cells M1rOW2N6fG:2b4jpZ:Kh[XO|YYm= M2excVczKGh? M3ywdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVU3NjBzIN88UU4> NH7HR3UzOTl2NUK1NC=>
human PC3 cells Mn3IR5l1d3SxeHnjxsBie3OjeR?= NHLIdlc4OiCq Ml;ZR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NkGuN|Uh|ryPLh?= NFTmOI0zOjR6MEi1NS=>
human HuH7 cells NE[3UVlRem:uaX\ldoF1cW:wIHHzd4F6 MkHPO|IhcA>? MXzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PjdwMUig{txONg>? Ml;RNlU3QTN5OEe=
human A549 cells NVv5[GVHWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYLofZR[PzJiaB?= NYnzRndoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUiyMlMzKM7:TT6= NHvJfY8zPTZ7M{e4Oy=>
human A549 cells MVjDfZRwfG:6aXRCpIF{e2G7 NFnqWWY4OiCq MoPoR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 MVOyNlQ5ODh3MR?=
human PC3 cells MmnCVJJwdGmoZYLheIlwdiCjc4PhfS=> M{\4WVI2KM7:TR?= M3XBVFEzOCCq Mln5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYYSgNlUhfU1iYX\0[ZIhOTJyIHjyd{BjgSCPVGSgZZN{[XlicnXsZZRqfmVidH:gSG1UVw>? NV\jeI5LOTZ4OECxOVk>
human H460 cells Ml6xSpVv[3Srb36gZZN{[Xl? MX[zNEDPxE1? MUPJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmeiB2N{OgeZAhfG9iM{CgeW0> MlfxNVg2ODF4MEG=
human IGROV1 cells MmnUSpVv[3Srb36gZZN{[Xl? NETBXoQzPCCq M3v4NGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgNUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 NEX3OJgzOTJzNkG1NS=>
human IGROV1 cells MXnGeY5kfGmxbjDhd5NigQ>? Ml\RNlQhcA>? MXXD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNmKGG2IEWg[o9t\CCLQ{WwJIFnfGW{IEK0JIhzeyCkeTDmcI94KGO7dH;t[ZRzgQ>? MYOyNVIyPjF3MR?=
human H4 cells NHTnSWdHfW6ldHnvckBie3OjeR?= NH;JTm0zKGh? NEXBeI1F\WO{ZXHz[UBqdiCIWW\FMXJHWCtidnXzbYNt\SCrboTlcpNqfHlicHXyJINmdGxiaX6gbJVu[W5iSESgZ4VtdHNiYX\0[ZIhOiCqcoOgdoVt[XSrdnWgeI8h[2:wdILvcC=> M3GwTFE5ODJ2NUi0
human MGC803 cells MlSwSpVv[3Srb36gZZN{[Xl? M1;OXVI2KM7:TR?= NGTIR2Y1QCCq NWjEe5U4S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUeFOECzJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNk9OKHCqYYPlJIF1KDJ3IIXNJIFnfGW{IES4JIhzeyC3c3nu[{Bxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIFnfGW{IES4JIhzeyCkeTDmcI94KGO7dH;t[ZRmeiC{ZXzheIl3\SC2bzDjc451em:u MUmyOFEyQTh4OR?=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
  • Formulation: Dissolved in DMSO plus 0.25 ml of PBS
  • 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

Bio Calculators

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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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    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. 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.

  • 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. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.

  • Dactolisib (BEZ235, NVP-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.

  • Buparlisib (BKM120, NVP-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. 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). 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