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 245 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 NYHWZYhVS2WubDDpcpZie2mxbjDhd5NigQ>? MlnNNlQhcA>? NV3XVIRKUW6qaXLpeIlwdiCxZjDldIl1cGWuaXHsJIdzd3e2aDDmZYN1d3JvaX7keYNm\CClZXzsJI1q\3KjdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBk\WyuIHnueoF{cW:wIHHzd4F6NCCLQ{WwQVAvOzhizszNMi=> NYDNdG5kOjJ6MESxNFg>
Sf21 cells Mm[ySpVv[3Srb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKG2xdYPlJJdqdGRidInw[UBRUTONYXzwbIEh\XiycnXzd4VlKGmwIGPmNlEh[2WubIOgZ48u\XiycnXzd4lv\yCQLYTldo1qdmGuIFjpd{11[WepZXSgbJVu[W5icEi1ZUB2e2mwZzDMMYFteGijLYDoc5NxcGG2aXT5cIlvd3OrdH;sJJN2[nO2cnH0[UBjgSCWTFOgZoF{\WRicHjvd5Bpd3JiaX3h[4lv\yxiSVO1NF0xNjVizszN NY\YfVB{OjJ3MkC2N|A>
Sf21 cells NULDcHdSTnWwY4Tpc44h[XO|YYm= NXXrb3BIUW6qaXLpeIlwdiCxZjDtc5V{\SC{ZXPvcYJqdmGwdDDQTVNM[WyyaHGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|LXnu[oVkfGWmIGPmNlEh[2WubIOsJGlEPTB;MD61JO69VS5? NXnZR|VCOTl5NEiyOlk>
Sf9 cells Mn3FSox2d3Knc3PlcpQheG:uYYLpfoF1cW:wIHHzd4F6 M{TtOWlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxRTBwNUWg{txONg>? Mn\lNlEyOjF4M{G=
THP1 cells NGm0b2hHfW6ldHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKFOFRkGtbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDUTHAyKGOnbHzzMEBKSzVyPUGuNFEh|ryPLh?= MnT6NVY4QDl5NEK=
human PC3 cells M3;jPWZ2dmO2aX;uJIF{e2G7 M{fz[FMxKG2rbh?= NYPiVmZ5UW6qaXLpeIlwdiCxZjDQTVNMKGmwIHj1cYFvKFCFMzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IIPldolv\SB2N{OgZYZ1\XJiM{CgcYlveyCkeTDFUGlUSSxiSVO1NF0yNjQQvF2u NUfTS3h3OjN2MUCwNFU>
HeLa (human carcinoma) cells. M4[yNmZ2dmO2aX;uJIF{e2G7 NV;ZOIFNUW5idnn0do8hcW6qaXLpeIlwdiCxZjDEUmEu\GWyZX7k[Y51KHC{b4TlbY4hc2mwYYPlLGRPSS2SSzmg[pJwdSCKZVzhJEhpfW2jbjDjZZJkcW6xbXGpJINmdGy|LDDJR|UxRTFwNDFOwG0v MnOyNVU3PTh6N{C=
THP1 cells NIjUeXBHfW6ldHnvckBie3OjeR?= NYnDc|BoUW6qaXLpeIlwdiCxZjDNR3AyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0yNjZ3IN88UU4> NGrnR5gyPjd6OUe0Ni=>
HeLa cells MYjGeY5kfGmxbjDhd5NigQ>? Mn34TY5pcWKrdHnvckBw\iCvVF;SJJBzd3SnaX6gbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|LDDJR|UxRTJwNTFOwG0v NXLDZXMxOTV4NUi4O|A>
human MCF7 cells MVzDfZRwfG:6aXRCpIF{e2G7 MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJO69VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLNUC9Nk43OyEQvF2u NGnYSFYyQDZ7MUi5OC=>
HeLa cells NXLrRopFTnWwY4Tpc44h[XO|YYm= M37BfmlvcGmkaYTpc44hd2ZiQWitO|UxOyCkaX7kbY5oKHSxIILlZ49u[mmwYX70JHBtczNiZYjwdoV{e2WmIHnuJGhmVGFiY3XscJMh[nliV3XzeIVzdiCkbH;0MEBKSzV;MzFOwG0v MUexO|E{PTJ2OB?=
human MCF7 cells Ml7HR5l1d3SxeHnjxsBie3OjeR?= MYHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME2zMlA5KM7:TT6= NWXyb2tUOTh4OUG4PVQ>
human MCF7 cells NGOyRY5EgXSxdH;4bYPDqGG|c3H5 MkXpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BjgSCVUlKgZZN{[XluIFfJQVMvOTZizszNMi=> NX\seYVXOTh4OUG4PVQ>
human MDA-MB-231 cells MYHDfZRwfG:6aXRCpIF{e2G7 MoDMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDpckBxemW|ZX7j[UBw\iB{MDFOwG0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H5MEBIUT1|LkOyJO69VS5? MmC4NVg3QTF6OUS=
human MDA-MB-231 cells M4f5UWN6fG:2b4jpZ:Kh[XO|YYm= MnzqR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDpckBxemW|ZX7j[UBw\iBzMDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKPTB;ND6zOUDPxE1w MkHtNVg3QTF6OUS=
human MDA-MB-468 cells NXu0W3FjS3m2b4TvfIlkyqCjc4PhfS=> Mmq5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDpckBxemW|ZX7j[UBw\iB{MDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYpvwKwhUUN3ME20Mlc3KM7:TT6= M1q5ZlE5PjlzOEm0
human HCT116 cells M3KxWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXXPflZ7PDhiaB?= NUTwdno5T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT6zJO69VQ>? M{PQOFIzOjF{N{Kx
human HCT116 cells NG\MdVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIfQPGY1QCCq M4LKeWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2u M37lOVIzOjF{N{Kx
HeLa cells NUS0SXJKSmmwZHnu[{Bi\m[rbnn0fUBie3OjeR?= MXXCbY5lcW6pIHHm[olvcXS7IH\vdkBRUTNva3nuZZNmKGm|b3zheIVlKG[{b32gTIVN[SClZXzsd{whU2l;NjFOwG0> MYCxOVY2QDh5MB?=
human HCT116 cells Mnj6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\5cFQ5KGh? MUjHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMhd3[ncnX4dJJme3OrbnegVGk{U2GucHjhJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63JO69VS5? MVyyNlIyOjd{MR?=
MDA-MB-231 cells NWfjWVZQS3m2b4TvfIlkyqCjc4PhfS=> MmHKR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDifUBUWkJiYYPzZZktKEeLNUC9Ok44OSEQvF2u Ml;6NVg3QTF6OUS=
Sf9 cells NHPGZ5VHfW6ldHnvckBie3OjeR?= NHvlb3ZKdmirYnn0bY9vKG:oIFPLNkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTZwOTFOwG0v M1jDflE5OzJzN{G2
human U87MG cells NX7keFBnTnWwY4Tpc44h[XO|YYm= NGfZWXVKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDVPFdOTyClZXzsd{BjgSCHTFnTRUwhUUN3ME24MlEh|ryPLh?= MmOwNVg{PDV4MEm=
human MDA-MB-468 cells MVjDfZRwfG:6aXRCpIF{e2G7 NFrhfopEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME24MlIh|ryPLh?= NX;QNG03OTh4OUG4PVQ>
human A375 cells MYjQdo9tcW[ncnH0bY9vKGG|c3H5 MYS0OkBp NWfn[IZlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IES2JIhzeyxiSVO1NF05NjRizszNMi=> NHXQOXAyPzB2OUK0PC=>
human A375 cells NUO1S2VvWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{DrcGlvcGmkaYTpc44hd2Zic3XyeY0ucW6mdXPl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIFGzO|Uh[2WubIOsJGlEPTB;OD60JO69VS5? MUOxO|YxOTd|OR?=
human HL60 cells M3vGRWN6fG:2b4jpZ:Kh[XO|YYm= NYq1TJBLPzJiaB?= M1T4bmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhNPjBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME25Mlk1KM7:TT6= MmPpNlI1QDB6NUG=
mouse Raw264 macrophage MlrUSpVv[3Srb36gZZN{[Xl? MV\Jcohq[mm2aX;uJI9nKEN3YT3t[YRq[XSnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCUYYeyOlQhdWGlcn;wbIFo\SxiSVO1NF0yOCEQvF2u M3OxR|E3Pzh7N{Sy
Sf9 cells MU\GeY5kfGmxbjDhd5NigQ>? MorHTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIHLveolv\SCSSUPLJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:OTBizszNMi=> NHHGVlEyODl7OEO1NS=>
human MDA-MB-468 cells M2\KS2N6fG:2b4jpZ:Kh[XO|YYm= MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHL5JHNTSiCjc4PhfUwhUUN3ME2xNE41KM7:TT6= MWSxPFY6OTh7NB?=
human PC3 cell NHvqR2RRem:uaX\ldoF1cW:wIHHzd4F6 NXjDOWZ[PzJiaB?= M2LjWmlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nlic4DlZ5Rzd3Cqb4TvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTF{LkGg{txONg>? Mn\1NlM1OTByMEW=
human HL60 cells MmrqVJJwdGmoZYLheIlwdiCjc4PhfS=> MXO3NkBp MoqxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF6LkSzJO69VS5? NEWyXlIzPTZ7M{e4Oy=>
human BT474 cell M3zEZnBzd2yrZnXyZZRqd25iYYPzZZk> MWC3NkBp NWTVW2xvUW6qaXLpeIlwdiCxZjDoeY1idiCEVES3OEBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JJNx\WO2cn;wbI91d22ndILpZ{BidmGueYPpd-+9lCCLQ{WwQVIxNjdizszNMi=> Mmj2NlM1OTByMEW=
THP1 cells Ml7CSpVv[3Srb36gZZN{[Xl? NHq0e4ZKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KG:oIGTIVFEh[2WubIOsJGlEPTB;M{eg{txONg>? Ml\pNVY4QDl5NEK=
human 184B5 cells NHzNNppEgXSxdH;4bYPDqGG|c3H5 MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxPFRDPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OzlwM{eg{txONg>? M3PDVFE5PjlzOEm0
human KB cells NYX4Uo1rS3m2b4TvfIlkyqCjc4PhfS=> MYS3NkBp MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDLRkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTR2Lke2JO69VS5? MXWyNVk1PTJ3MB?=
mouse RAW264.7 cells M3HxV2Z2dmO2aX;uJIF{e2G7 MVGyOUDPxE1? NFL1[2YzOCCq NVi4c2lWUW6qaXLpeIlwdiCxZjDQTVNMN0GNVDDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIHnOU3MheHKxdHXpckBmgHC{ZYPzbY9vKGG2IEK1JO69VSCjZoTldkAzOCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NHnJd20zPDJ7OU[xOi=>
human A2780 cells Mn23RZBweHSxc3nzJIF{e2G7 NF\kSJAzKM7:TR?= M1TNZlEzKGh? MXHJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHPpd5Bt[XSrbj3y[ZNqe3SjboSgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSWu2IHzleoVtKGG2IEKgeW0h[W[2ZYKgNVIhcHK|IHL5JIludXWwb3Lsc5Qh[W6jbInzbZMv MmXUNVc3QDRyMUi=
human SW480 cells MoL4SpVv[3Srb36gZZN{[Xl? MXOyNEDPxE1? NGPJdHczPCCq NEjuXoZF\WO{ZXHz[UBqdiC|dYL2bZZqdiCneIDy[ZN{cW:wIHnuJIh2dWGwIGPXOFgxKGOnbHzzJIF1KDJyIIXNJIFnfGW{IEK0JIhzeyCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MnrDNVc1PzJ7NkK=
mouse mast cells M37CR2Z2dmO2aX;uJIF{e2G7 M3LmZlIxKM7:TR?= MYrJcohq[mm2aX;uJI9nKFOFRj3pcoR2[2WmIGDLRk9Cc3RicHjvd5Bpd3K7bHH0bY9vKGmwIH3veZNmKG2jc4SgZ4VtdHNiYYSgNlAh|ryP NF;xbVMyPjd6OUe0Ni=>
human BJ cells NYTu[JlMTnWwY4Tpc44h[XO|YYm= NICyW3czPSEQvF2= M2X5WVIhcA>? MUPJcohq[mm2aX;uJI9nKFCLM1ugd4lodmGuaX7nJIlvKFCGR1[td5RqdXWuYYTl[EB{\XK3bTDzeIFzfmWmIHj1cYFvKEKMIHPlcIx{KHS{YX7z[oVkfGWmIIfpeIgheGyjc33p[EBGT0[SL2DIJIRwdWGrbjDv[kBCc3RiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiUFitSWdHWCC{ZXTpd5RzcWK3dHnvckB1dyCybHHzcYEhdWWvYoLhcoUh[XRiMkWgeW0hfHKnYYTl[EAzKGi{czDi[YZwemViUFTHSkBkcGGubHXu[4Uh[nliY3;u[o9k[WxibXnjdo9{[2:yeR?= MXixOlc3PzB6NR?=
human IGROV1 cells NH3rWXdHfW6ldHnvckBie3OjeR?= MYmyOE81QCCq Mme3TY5pcWKrdHnvckBw\iCSSUPLM2FsfCCrbjDoeY1idiCLR2LPWlEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSUuWIHzleoVtKGG2IEGgeI8hPSC2aX3ld{BKSzVyIHHmeIVzKDJ2IITvJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NXfifY1nOjF{MU[xOVE>
human IGROV1 cells MoLxSpVv[3Srb36gZZN{[Xl? NXL3cJB7OjRxNEigbC=> MUfJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCleXPsbY4hTDFibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NGn1eW8zOTJzNkG1NS=>
rat RBL2H3 cells Mn\hSpVv[3Srb36gZZN{[Xl? NYXaXGtCUW6qaXLpeIlwdiCxZjDBNlMyQDdvaX7keYNm\CCmZXfyZY52dGG2aX;uJIlvKHKjdDDSRmwzUDNiY3XscJM> MnjyNVg{Ojh5MU[=
human BJ cells MX;GeY5kfGmxbjDhd5NigQ>? NX34NYNwOjVizszN NEjG[HIzKGh? NFTTeYdC[3SrdnH0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gZZQhXGi{M{C4JIlvKFCGR1[td5RqdXWuYYTl[EB{\XK3bTDzeIFzfmWmIHj1cYFvKEKMIHPlcIx{KGG2IEK1JJVOKHS{ZXH0[YQhOiCqcoOgZoVnd3KnIGDES2Yh[2ijbHzlcodmKGK7IHntcZVvd2Kub4T0bY5o MUmxOlc3PzB6NR?=
human HCT116 cells NXrJWng1TnWwY4Tpc44h[XO|YYm= MXKxNEDPxE1? NUDwWVJ{OTBibXnu NIjmS|dKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDpckBpfW2jbjDIR3QyOTZiY3XscJMhfXOrbnegX|MzWF2DVGCgZZQhOTBidV2gZYZ1\XJiMUCgcYlvew>? NGHoXIIzOjJzMkeyNS=>
human HCT116 cells MmPGSpVv[3Srb36gZZN{[Xl? NUDWT3JLOTBizszN MYSxNEBucW5? M3;lPGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFixNFQ4WiCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IIXzbY5oKFt|MmDdRXRRKGG2IEGwJJVOKGGodHXyJFExKG2rboO= NGjIXm0zOjJzMkeyNS=>
human HCT116 cells M1jEcWZ2dmO2aX;uJIF{e2G7 NIHLWYQyOCEQvF2= Mn;ITY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRYt1KFOnckS3N{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? MkjzNlIzOTJ5MkG=
human HCT116 cells NFL3UIJHfW6ldHnvckBie3OjeR?= NVHaNnNGOTBizszN MY\Jcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEGtdDDT[ZI1PzNicHjvd5Bpd3K7bHH0bY9vKGG2IEGwJJVOKGK7IHntcZVvd2Kub4SgZY5idHm|aYO= M3m2RlIzOjF{N{Kx
human PC3 cells NEXkbIdHfW6ldHnvckBie3OjeR?= MnP6OVAh|ryP M33hbFghcA>? NHnUNlJKdmS3Y4Tpc44hd2ZicEKxJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCqdX3hckBRSzNiY3XscJMh[XRiNUCgeW0hcW6ldXLheIVlKG[xcjC4JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIILlcIF1cX[nIITvJJVvfHKnYYTl[EBkd262cn;s M4O5dFIzQTl6NEey
human LNCAP cells MoH3SpVv[3Srb36gZZN{[Xl? M4DBd|AvOS1|MDFOwG0> NIK5Vms{OCCvaX6= Mmm2TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFzOR2FRKGOnbHzzJIF1KDBwMTD0c{A{OCC3TTDh[pRmeiB|MDDtbY5{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NVfRelROOjJ6M{KzNVY>
human LNCAP cells M3zxS2Z2dmO2aX;uJIF{e2G7 NGf1ZZExNjFvM{Cg{txO MWKyOEBp NFnZXGxFd3ewcnXneYxifGmxbjDv[kB{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHj1cYFvKEyQQ1HQJINmdGy|IHH0JFAvOSC2bzCzNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NXeyTpB2OjJ6M{KzNVY>
HUVEC NYmzZotXTnWwY4Tpc44h[XO|YYm= NHj0Z2IyOC1{NTFOwG0> NVO2WG1NOTZiaB?= MYPJcohq[mm2aX;uJI9nKFSQRnHsdIhiNXO2aX31cIF1\WRiSVPBUU0yKG2UTlGg[ZhxemW|c3nvckBqdiCKVW\FR{BifCBzMDD0c{AzPSC3TTDwdoV1emWjdHXkJIZweiBzNjDodpMh[mWob4LlJHRPTmGucHjhJINp[WyuZX7n[UBu\WG|dYLl[EBi\nSncjC2JIhzeyCkeTDSWE1RS1JiYX7hcJl{cXN? MUmyNlAzPjRzMB?=
HUVEC MoH1SpVv[3Srb36gZZN{[Xl? M2XtUFExNTJ3IN88US=> MnfMN|AhdWmw Mnj4TY5pcWKrdHnvckBw\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= MXiyNlAzPjRzMB?=
human H1299 cells M{jHTWZ2dmO2aX;uJIF{e2G7 NVLCe2JTOC5zLUOwJO69VQ>? NEPLOVczPCCq M2rseGRwf25icnXneYxifGmxbjDv[kBkUUGSMjDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NGr4V|kzOjZ{MkC2PS=>
human H1299 cells MmjnSpVv[3Srb36gZZN{[Xl? M3:ySFAvOS1|MDFOwG0> M3zPflI1KGh? MVfEc5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjCxNFAhfWdxbXygWHJCUUxiYX7kJHBKO0tiaX7obYJqfG:{IFzZNlk1ODB{ NUG3TZZVOjJ4MkKwOlk>
human H1299 cells MWHGeY5kfGmxbjDhd5NigQ>? NVzkU5hSOC5zLUOwJO69VQ>? MmrGNlQhcA>? MWLJcoR2[3Srb36gc4YhTFJ3IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NV\FcVgyOjJ4MkKwOlk>
human H1299 cells NHfjeGFHfW6ldHnvckBie3OjeR?= MlT2NE4yNTNyIN88US=> NWLoN281OjRiaB?= NGf4bpBKdmS3Y4Tpc44hd2ZiSl7LMY1m\GmjdHXkJGNJV1BiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NID6Z3IzOjZ{MkC2PS=>
HEK293 cells NETKZYlHfW6ldHnvckBie3OjeR?= MnTnNU42KGh? NFL3RVNFcXOybHHj[Y1mdnRib3[gX|NJZUyVRDDmdo9uKGi3bXHuJFVJXDZicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkAyNjViaILzJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6p MlH2NlI2OzdzNUO=
human U251HRE cells M4jBW2Z2dmO2aX;uJIF{e2G7 Mn\PTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhUEmIMTDhZ5RqfmG2aX;uJIlvKGi3bXHuJHUzPTGKUlWgZ4VtdHNiYomgZ4VtdCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 NXzhdGM3OTh3MEG2NFE>
human HCT116 cells MVTGeY5kfGmxbjDhd5NigQ>? NXXQN3pHOTBizszN MVnJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz NYnYV5I1OjJ{MUK3NlE>
Sf9 cells NX\T[Ytj\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 M4X6VWlvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3fhcY1iKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 MVeyNVEzOTZ|MR?=
human HCT116 cells Ml;jVJJwdGmoZYLheIlwdiCjc4PhfS=> Mn[5O|IhcA>? MnX5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NUGuPFIh|ryPLh?= M1j2eVI2Pjl|N{i3
human HCT116 cells NFXWWplEgXSxdH;4bYPDqGG|c3H5 NUfKdVdJPzJiaB?= NXHqTGFbS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PTZwMEGg{txONg>? NV7rU4FGOjF7NEWyOVA>
human PC3 cells M4nRR2N6fG:2b4jpZ:Kh[XO|YYm= MY[3NkBp NV\INm9ZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OlEvOzVizszNMi=> NYnTW2NlOjJ2OEC4OVE>
human HuH7 cells MmO3VJJwdGmoZYLheIlwdiCjc4PhfS=> NIKyZ|U4OiCq MorpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZ5LkG4JO69VS5? MXqyOVY6Ozd6Nx?=
human A549 cells MkfnVJJwdGmoZYLheIlwdiCjc4PhfS=> MV[3NkBp M1j6RWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD16Mj6zNkDPxE1w NGHWUVYzPTZ7M{e4Oy=>
human A549 cells MXHDfZRwfG:6aXRCpIF{e2G7 MmXQO|IhcA>? MlrGR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 Mn3mNlI1QDB6NUG=
human PC3 cells NUHmW3pQWHKxbHnm[ZJifGmxbjDhd5NigQ>? MnPYNlUh|ryP NILzNlUyOjBiaB?= NUft[2x{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZZQhOjVidV2gZYZ1\XJiMUKwJIhzeyCkeTDNWHQh[XO|YYmgdoVt[XSrdnWgeI8hTE2VTx?= M4L2OlE3PjhyMUW5
human H460 cells M3zxZWZ2dmO2aX;uJIF{e2G7 M1LnXFMxKM7:TR?= Ml3aTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJGg1PjBiY3XscJMh[XO|ZYPz[YQh[XNiQXv0JJBpd3OyaH;yfYxifGmxbjDheEBU\XJiNEezJJVxKHSxIEOwJJVO M4SwWlE5PTBzNkCx
human IGROV1 cells NFjtdmhHfW6ldHnvckBie3OjeR?= MmXSNlQhcA>? MWnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNmKGG2IEGg[o9t\CCLQ{WwJIFnfGW{IEK0JIhzeyCkeTDmcI94KGO7dH;t[ZRzgQ>? NYTu[mNNOjF{MU[xOVE>
human IGROV1 cells NWXTeJR3TnWwY4Tpc44h[XO|YYm= MUiyOEBp M1mxVGNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgOUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 MmK4NlEzOTZzNUG=
human H4 cells MYPGeY5kfGmxbjDhd5NigQ>? Mn;3NkBp NFfMZZJF\WO{ZXHz[UBqdiCIWW\FMXJHWCtidnXzbYNt\SCrboTlcpNqfHlicHXyJINmdGxiaX6gbJVu[W5iSESgZ4VtdHNiYX\0[ZIhOiCqcoOgdoVt[XSrdnWgeI8h[2:wdILvcC=> MlfiNVgxOjR3OES=
human MGC803 cells MYDGeY5kfGmxbjDhd5NigQ>? NWqzVXI5OjVizszN NUXqXIdxPDhiaB?= Mn71R4VtdCCleXPs[UBienKnc4SgbY4hcHWvYX6gUWdEQDB|IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCJMj;NJJBp[XOnIHH0JFI2KHWPIHHmeIVzKDR6IHjyd{B2e2mwZzDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pIHHmeIVzKDR6IHjyd{BjgSCobH;3JIN6fG:vZYTldkBz\WyjdHn2[UB1dyClb370do9t NFHobmgzPDFzOUi2PS=>

... 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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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

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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.

selleck catalog

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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