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 1026 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 M1XkdGNmdGxiaX72ZZNqd25iYYPzZZk> MoPxNlQhcA>? MUDJcohq[mm2aX;uJI9nKGWyaYTo[Yxq[WxiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJINmdGxibXnndoF1cW:wIH;mJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IHPlcIwhcW64YYPpc44h[XO|YYmsJGlEPTB;MD6zPEDPxE1w MXyyNlgxPDFyOB?=
Sf21 cells NIGx[VZHfW6ldHnvckBie3OjeR?= MWrJcohq[mm2aX;uJI9nKG2xdYPlJJdqdGRidInw[UBRUTONYXzwbIEh\XiycnXzd4VlKGmwIGPmNlEh[2WubIOgZ48u\XiycnXzd4lv\yCQLYTldo1qdmGuIFjpd{11[WepZXSgbJVu[W5icEi1ZUB2e2mwZzDMMYFteGijLYDoc5NxcGG2aXT5cIlvd3OrdH;sJJN2[nO2cnH0[UBjgSCWTFOgZoF{\WRicHjvd5Bpd3JiaX3h[4lv\yxiSVO1NF0xNjVizszN NFi3Z5AzOjV{ME[zNC=>
Sf21 cells M1LWN2Z2dmO2aX;uJIF{e2G7 NH7ETlhKdmirYnn0bY9vKG:oIH3veZNmKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiU3[yNUBk\WyuczygTWM2OD1yLkWg{txONg>? MUSxPVc1QDJ4OR?=
Sf9 cells NEG0WpZHdHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? M2jDZ2lvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxRTBwNUWg{txONg>? MWiyNVEzOTZ|MR?=
THP1 cells NV3pVYJlTnWwY4Tpc44h[XO|YYm= NEP6fIpKdmirYnn0bY9vKG:oIGPDSlEucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBVUFBzIHPlcIx{NCCLQ{WwQVEvODFizszNMi=> M37zc|E3Pzh7N{Sy
human PC3 cells NH:5NXZHfW6ldHnvckBie3OjeR?= NF;ocmc{OCCvaX6= M{DoOWlvcGmkaYTpc44hd2ZiUFmzT{BqdiCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCC|ZYLpcoUhPDd|IHHmeIVzKDNyIH3pcpMh[nliRVzJV2EtKEmFNUC9NU4{|ryPLh?= M13ReVI{PDFyMEC1
HeLa (human carcinoma) cells. M3zaNWZ2dmO2aX;uJIF{e2G7 NX3HNWI3UW5idnn0do8hcW6qaXLpeIlwdiCxZjDEUmEu\GWyZX7k[Y51KHC{b4TlbY4hc2mwYYPlLGRPSS2SSzmg[pJwdSCKZVzhJEhpfW2jbjDjZZJkcW6xbXGpJINmdGy|LDDJR|UxRTFwNDFOwG0v M2LGPFE2PjV6OEew
THP1 cells M4G4bGZ2dmO2aX;uJIF{e2G7 NUjVdY5PUW6qaXLpeIlwdiCxZjDNR3AyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0yNjZ3IN88UU4> MUmxOlc5QTd2Mh?=
HeLa cells NFXZZ|FHfW6ldHnvckBie3OjeR?= MoL0TY5pcWKrdHnvckBw\iCvVF;SJJBzd3SnaX6gbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|LDDJR|UxRTJwNTFOwG0v NWH1fGpXOTV4NUi4O|A>
human MCF7 cells MlS2R5l1d3SxeHnjxsBie3OjeR?= Mkj3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVIvPjNizszNMi=> NVLJc2F{OTh4OUG4PVQ>
HeLa cells MWTGeY5kfGmxbjDhd5NigQ>? M2fiemlvcGmkaYTpc44hd2ZiQWitO|UxOyCkaX7kbY5oKHSxIILlZ49u[mmwYX70JHBtczNiZYjwdoV{e2WmIHnuJGhmVGFiY3XscJMh[nliV3XzeIVzdiCkbH;0MEBKSzV;MzFOwG0v MVSxO|E{PTJ2OB?=
human MCF7 cells NEXsZ2pEgXSxdH;4bYPDqGG|c3H5 NG[yZmREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExKHWPIHPocI9zd3G3aX7lJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjB6IN88UU4> MmTRNVg3QTF6OUS=
human MCF7 cells M3npcWN6fG:2b4jpZ:Kh[XO|YYm= NW\qV2diS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCkeTDTVmIh[XO|YYmsJGdKRTNwMU[g{txONg>? Mn;JNVg3QTF6OUS=
human MDA-MB-231 cells MWTDfZRwfG:6aXRCpIF{e2G7 MnvzR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDpckBxemW|ZX7j[UBw\iB{MDFOwG0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H5MEBIUT1|LkOyJO69VS5? M{LEe|E5PjlzOEm0
human MDA-MB-231 cells MXnDfZRwfG:6aXRCpIF{e2G7 NXTmUVZ1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCxNEB2VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLNUC9OE4{PSEQvF2u MmjENVg3QTF6OUS=
human MDA-MB-468 cells Ml3nR5l1d3SxeHnjxsBie3OjeR?= NGrRcZhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4Phfg+9lCCLQ{WwQVQvPzZizszNMi=> M1GwfVE5PjlzOEm0
human HCT116 cells NY\T[4lwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3TlfFQ5KGh? NInGbWJIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKEhzMES3VkBufXSjboSgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13LkOg{txO M372SlIzOjF{N{Kx
human HCT116 cells NG[2eZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFzZeVk1QCCq NIfwVXhIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02NjhizszNMi=> NUXBXZRWOjJ{MUK3NlE>
HeLa cells NEO0NHlDcW6maX7nJIFn\mmwaYT5JIF{e2G7 MoWwRolv\GmwZzDh[oZqdmm2eTDmc5IhWEl|LXvpcoF{\SCrc3;sZZRm\CCocn;tJGhmVGFiY3XscJMtKEurPU[g{txO Ml6wNVU3PTh6N{C=
human HCT116 cells MkfJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M160d|Q5KGh? MX3Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMhd3[ncnX4dJJme3OrbnegVGk{U2GucHjhJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63JO69VS5? MW[yNlIyOjd{MR?=
MDA-MB-231 cells Ml\oR5l1d3SxeHnjxsBie3OjeR?= NWHiW3J2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi55MTFOwG0v NUHxZ3lROTh4OUG4PVQ>
Sf9 cells MUPGeY5kfGmxbjDhd5NigQ>? M2jsNGlvcGmkaYTpc44hd2ZiQ1uyJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:Pi57IN88UU4> M1i0WlE5OzJzN{G2
human U87MG cells MUHGeY5kfGmxbjDhd5NigQ>? NHmyW5FKdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTDpckBpfW2jbjDVPFdOTyClZXzsd{BjgSCHTFnTRUwhUUN3ME24MlEh|ryPLh?= NUXqVIFYOTh|NEW2NFk>
human MDA-MB-468 cells NV\HRo5kS3m2b4TvfIlkyqCjc4PhfS=> MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD16LkKg{txONg>? MlX3NVg3QTF6OUS=
human A375 cells NH7hdYlRem:uaX\ldoF1cW:wIHHzd4F6 M4DQOlQ3KGh? NG\hdmlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOgZYZ1\XJiNE[gbJJ{NCCLQ{WwQVgvPCEQvF2u NGrSWWEyPzB2OUK0PC=>
human A375 cells NIPxbIlRem:uaX\ldoF1cW:wIHHzd4F6 M4e4UmlvcGmkaYTpc44hd2Zic3XyeY0ucW6mdXPl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIFGzO|Uh[2WubIOsJGlEPTB;OD60JO69VS5? M2GweFE4PjBzN{O5
human HL60 cells MXPDfZRwfG:6aXRCpIF{e2G7 MnLrO|IhcA>? MlzTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUmuPVQh|ryPLh?= MnPyNlI1QDB6NUG=
mouse Raw264 macrophage MVvGeY5kfGmxbjDhd5NigQ>? M1SyVGlvcGmkaYTpc44hd2ZiQ{XhMY1m\GmjdHXkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIGLhe|I3PCCvYXPyc5Bp[WenLDDJR|UxRTFyIN88UU4> M4CwbVE3Pzh7N{Sy
Sf9 cells NWrPbG06TnWwY4Tpc44h[XO|YYm= NHzOWmlKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgZo93cW6nIGDJN2sh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1zMDFOwG0v M3zwVlExQTl6M{Wx
human MDA-MB-468 cells MVzDfZRwfG:6aXRCpIF{e2G7 NX7Fc5hZS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{BjgSCVUlKgZZN{[XluIFnDOVA:OTBwNDFOwG0v MX6xPFY6OTh7NB?=
human PC3 cell MXLQdo9tcW[ncnH0bY9vKGG|c3H5 MmG5O|IhcA>? NFOyXJhKdmirYnn0bY9vKG:oIHj1cYFvKFCFMzDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrczygTWM2OD1zMj6xJO69VS5? M{LnTFI{PDFyMEC1
human HL60 cells NULpPGl1WHKxbHnm[ZJifGmxbjDhd5NigQ>? M{HNWVczKGh? MULBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThwNEOg{txONg>? MmPINlU3QTN5OEe=
human BT474 cell MkC1VJJwdGmoZYLheIlwdiCjc4PhfS=> MmfYO|IhcA>? MmKxTY5pcWKrdHnvckBw\iCqdX3hckBDXDR5NDDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrc,-8kEBKSzVyPUKwMlch|ryPLh?= MVqyN|QyODByNR?=
THP1 cells NXy4XZlsTnWwY4Tpc44h[XO|YYm= NGr6cYlKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KG:oIGTIVFEh[2WubIOsJGlEPTB;M{eg{txONg>? M4TjUFE3Pzh7N{Sy
human 184B5 cells MVHDfZRwfG:6aXRCpIF{e2G7 NYq4fZh7S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOTh2QkWgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUO5MlM4KM7:TT6= MoTsNVg3QTF6OUS=
human KB cells M3vmRmN6fG:2b4jpZ:Kh[XO|YYm= MmnDO|IhcA>? NYjCfnB2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20OE44PiEQvF2u MXKyNVk1PTJ3MB?=
mouse RAW264.7 cells MoXjSpVv[3Srb36gZZN{[Xl? NFzpZWszPSEQvF2= NXvyUW9uOjBiaB?= MnPFTY5pcWKrdHnvckBw\iCSSUPLM2FMXCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2OgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDJ3IN88UUBi\nSncjCyNEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NFPhenEzPDJ7OU[xOi=>
human A2780 cells NHna[o5CeG:ydH;zbZMh[XO|YYm= M2nJU|Ih|ryP NXuzO5VpOTJiaB?= MXLJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHPpd5Bt[XSrbj3y[ZNqe3SjboSgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSWu2IHzleoVtKGG2IEKgeW0h[W[2ZYKgNVIhcHK|IHL5JIludXWwb3Lsc5Qh[W6jbInzbZMv NXzOZoxYOTd4OESwNVg>
human SW480 cells NWnC[2Z2TnWwY4Tpc44h[XO|YYm= NHPYNYozOCEQvF2= MVyyOEBp MlnqSIVkemWjc3WgbY4he3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCVV{S4NEBk\WyuczDheEAzOCC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= MWGxO|Q4Ojl4Mh?=
mouse mast cells Mn;qSpVv[3Srb36gZZN{[Xl? NVnSUZg{OjBizszN NWTKUFFlUW6qaXLpeIlwdiCxZjDTR2YucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDtZZN1KGOnbHzzJIF1KDJyIN88US=> MkPwNVY4QDl5NEK=
human BJ cells NXvNN4lFTnWwY4Tpc44h[XO|YYm= NWO5dlZvOjVizszN NWXyZZRjOiCq NIKyb2pKdmirYnn0bY9vKG:oIGDJN2she2mpbnHsbY5oKGmwIGDES2Yue3SrbYXsZZRm\CC|ZYL1cUB{fGG{dnXkJIh2dWGwIFLKJINmdGy|IITyZY5{\mWldHXkJJdqfGhicHzhd41q\CCHR1\QM3BJKGSxbXHpckBw\iCDa4SgZZN{\XO|ZXSgZZMhe3WycILld5Nqd25ib3[gVGguTUeIUDDy[YRqe3S{aXL1eIlwdiC2bzDwcIF{dWFibXXtZpJidmViYYSgNlUhfU1idILlZZRm\CB{IHjyd{Bj\W[xcnWgVGRITiClaHHscIVv\2ViYomgZ49v\m:lYXygcYlkem:|Y3;wfS=> M3G3XFE3PzZ5MEi1
human IGROV1 cells NV;ZVm5qTnWwY4Tpc44h[XO|YYm= MlPaNlQwPDhiaB?= MVzJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MUeyNVIyPjF3MR?=
human IGROV1 cells NGjzO4JHfW6ldHnvckBie3OjeR?= M{PuSVI1NzR6IHi= MV;Jcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCleXPsbY4hTDFibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NIe4UJAzOTJzNkG1NS=>
rat RBL2H3 cells MoXVSpVv[3Srb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKEF{M{G4O{1qdmS3Y3XkJIRm\3KjboXsZZRqd25iaX6gdoF1KFKETELIN{Bk\Wyucx?= MYSxPFMzQDdzNh?=
human BJ cells M33iR2Z2dmO2aX;uJIF{e2G7 Mn\vNlUh|ryP MoHZNkBp MlTkRYN1cX[jdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHRpejNyODDpckBRTEeILYP0bY12dGG2ZXSgd4VzfW1ic4ThdpZm\CCqdX3hckBDUiClZXzsd{BifCB{NTD1UUB1emWjdHXkJFIhcHK|IHLl[o9z\SCSRFfGJINp[WyuZX7n[UBjgSCrbX31co9jdG:2dHnu[y=> M3;3[VE3PzZ5MEi1
human HCT116 cells M4rzemZ2dmO2aX;uJIF{e2G7 MlzqNVAh|ryP MlLYNVAhdWmw NWnQWYtvUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KHW|aX7nJHs{OlCfQWTQJIF1KDFyIIXNJIFnfGW{IEGwJI1qdnN? NYjnfJZmOjJ{MUK3NlE>
human HCT116 cells MojCSpVv[3Srb36gZZN{[Xl? NUG1UWhwOTBizszN NXL3NYg6OTBibXnu M17TT2lvcGmkaYTpc44hd2ZiUFmzT4FteGijIFixNFQ4WiCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IIXzbY5oKFt|MmDdRXRRKGG2IEGwJJVOKGGodHXyJFExKG2rboO= MkXSNlIzOTJ5MkG=
human HCT116 cells NX\1R2U5TnWwY4Tpc44h[XO|YYm= NGTNb2syOCEQvF2= MmDaTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRYt1KFOnckS3N{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? NYTqZ3dXOjJ{MUK3NlE>
human HCT116 cells MnmxSpVv[3Srb36gZZN{[Xl? M{HURlExKM7:TR?= NH7FTHNKdmirYnn0bY9vKG:oIGDJN2tidHCqYTDINVA1P1JibYX0ZY51KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBU\XJ2N{OgdIhwe3Cqb4L5cIF1cW:wIHH0JFExKHWPIHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> NX;5W4E{OjJ{MUK3NlE>
human PC3 cells MoD4SpVv[3Srb36gZZN{[Xl? NUPHXW9CPTBizszN MUS4JIg> M1rncmlv\HWldHnvckBw\iCyMkGgdJJwfGWrbjDlfJBz\XO|aX;uJIlvKGi3bXHuJHBEOyClZXzsd{BifCB3MDD1UUBqdmO3YnH0[YQh\m:{IEigbJJ{KGK7IGfld5Rmem5iYnzveJRqdmdicnXsZZRqfmVidH:geY51emWjdHXkJINwdnS{b3y= M4DQRlIzQTl6NEey
human LNCAP cells M1m3TWZ2dmO2aX;uJIF{e2G7 NFzKOGMxNjFvM{Cg{txO MYWzNEBucW5? NFTOO3NKdmirYnn0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEOwJI1qdnNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NWLhUGcxOjJ6M{KzNVY>
human LNCAP cells MoTlSpVv[3Srb36gZZN{[Xl? NG\4VG4xNjFvM{Cg{txO M3KwclI1KGh? NFKwU2lFd3ewcnXneYxifGmxbjDv[kB{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHj1cYFvKEyQQ1HQJINmdGy|IHH0JFAvOSC2bzCzNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MYqyNlg{OjNzNh?=
HUVEC NFPITndHfW6ldHnvckBie3OjeR?= Mn3iNVAuOjVizszN NFS0[2QyPiCq M{DIW2lvcGmkaYTpc44hd2ZiVF7GZYxxcGFvc4TpcZVt[XSnZDDJR2FONTFibWLORUBmgHC{ZYPzbY9vKGmwIFjVWmVEKGG2IEGwJJRwKDJ3IIXNJJBz\XS{ZXH0[YQh\m:{IEG2JIhzeyCkZX\vdoUhXE6IYXzwbIEh[2ijbHzlcodmKG2nYYP1doVlKGGodHXyJFYhcHK|IHL5JHJVNVCFUjDhcoFtgXOrcx?= M3:zflIzODJ4NEGw
HUVEC MoiwSpVv[3Srb36gZZN{[Xl? MWKxNE0zPSEQvF2= Mnu0N|AhdWmw M1LPZmlvcGmkaYTpc44hd2ZiVF7GZYxxcGFvc4TpcZVt[XSnZDDoeY1idiCLQ1HNMVEheHKxbX;0[ZIh[WO2aY\peJkh\XiycnXzd4VlKGmwIFjVWmVEKGG|c3Xzd4VlKGG|IHLleIEu\2GuYXP0c5Nq\GG|ZTDhZ5Rqfmm2eTDheEAyOCC2bzCyOUB2VSCycnX0doVifGWmIH\vdkA{OCCvaX7zJIJm\m:{ZTDUUmZidHCqYTDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiNTDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NXvVS4pROjJyMk[0NVA>
human H1299 cells NIS1ZZVHfW6ldHnvckBie3OjeR?= Mmf2NE4yNTNyIN88US=> M1LxTFI1KGh? MmDYSI94diC{ZXf1cIF1cW:wIH;mJINKSVB{IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MVKyNlYzOjB4OR?=
human H1299 cells MWTGeY5kfGmxbjDhd5NigQ>? M3fWfFAvOS1|MDFOwG0> M2jiOFI1KGh? MYPEc5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjCxNFAhfWdxbXygWHJCUUxiYX7kJHBKO0tiaX7obYJqfG:{IFzZNlk1ODB{ MnnDNlI3OjJyNkm=
human H1299 cells NUXPfFc4TnWwY4Tpc44h[XO|YYm= M4\3OVAvOS1|MDFOwG0> NVP5SI11OjRiaB?= NUPpdYlGUW6mdXP0bY9vKG:oIFTSOUBmgHC{ZYPzbY9vKGmwIHj1cYFvKEhzMkm5JINmdGy|IHH0JFAvOSC2bzCzNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MYeyNlYzOjB4OR?=
human H1299 cells MXLGeY5kfGmxbjDhd5NigQ>? MUmwMlEuOzBizszN NXLXe|J1OjRiaB?= MYnJcoR2[3Srb36gc4YhUk6NLX3l[IlifGWmIFPIU3Ah\XiycnXzd4lwdiCrbjDoeY1idiCKMUK5PUBk\WyuczDheEAxNjFidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MlXhNlI3OjJyNkm=
HEK293 cells MkfnSpVv[3Srb36gZZN{[Xl? MVexMlUhcA>? MWjEbZNxdGGlZX3lcpQhd2ZiW{PIYWxUTCCocn;tJIh2dWGwIEXIWFYhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bi\nSncjCxMlUhcHK|IHL5JIxqeXWrZDDzZ4lvfGmubHH0bY9vKGOxdX70bY5o M{jkdVIzPTN5MUWz
human U251HRE cells M4jzTGZ2dmO2aX;uJIF{e2G7 NIe1emVKdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hXTJ3MVjSSUBk\WyuczDifUBk\WyuIHLhd4VlKHKncH;yeIVzKGenbnWgZZN{[Xl? NVG0e21MOTh3MEG2NFE>
human HCT116 cells Mlm4SpVv[3Srb36gZZN{[Xl? M3OxVVExKM7:TR?= MVjJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MY[yNlIyOjd{MR?=
Sf9 cells NFS1VFdndHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? NWHjRpZHUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPL[4FudWFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYm= M1LXVFIyOTJzNkOx
human HCT116 cells MWHQdo9tcW[ncnH0bY9vKGG|c3H5 M3v5XlczKGh? NYC0NmlHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBi[nOxcnLhcoNmKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVEvQDJizszNMi=> NYryPGx2OjV4OUO3PFc>
human HCT116 cells NVXtRXJVS3m2b4TvfIlkyqCjc4PhfS=> MYC3NkBp MnTmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVYvODFizszNMi=> NUHWbW1jOjF7NEWyOVA>
human PC3 cells M2PNXWN6fG:2b4jpZ:Kh[XO|YYm= MXK3NkBp NE\neHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME22NU4{PSEQvF2u NWTHRYREOjJ2OEC4OVE>
human HuH7 cells MnfxVJJwdGmoZYLheIlwdiCjc4PhfS=> Mo[xO|IhcA>? MVzBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PjdwMUig{txONg>? NISwe5QzPTZ7M{e4Oy=>
human A549 cells NILUTYZRem:uaX\ldoF1cW:wIHHzd4F6 MoK0O|IhcA>? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QDJwM{Kg{txONg>? MkHsNlU3QTN5OEe=
human A549 cells M3f2b2N6fG:2b4jpZ:Kh[XO|YYm= MXK3NkBp MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= NFjRWYgzOjR6MEi1NS=>
human PC3 cells NV3SfGhFWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVyyOUDPxE1? M3W3S|EzOCCq MWHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjdDCyOUB2VSCjZoTldkAyOjBiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDEUXNQ MlXuNVY3QDBzNUm=
human H460 cells NInOblJHfW6ldHnvckBie3OjeR?= MkXYN|Ah|ryP MnjyTY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJGg1PjBiY3XscJMh[XO|ZYPz[YQh[XNiQXv0JJBpd3OyaH;yfYxifGmxbjDheEBU\XJiNEezJJVxKHSxIEOwJJVO NX\LfZhqOTh3MEG2NFE>
human IGROV1 cells NITTXYlHfW6ldHnvckBie3OjeR?= NVPhbHo1OjRiaB?= NUjuZ3R1S2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUUeUT2[xJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNUBxcGG|ZTDheEAyKG[xbHSgTWM2OCCjZoTldkAzPCCqcoOgZpkh\myxdzDjfZRwdWW2com= NWfZTXJkOjF{MU[xOVE>
human IGROV1 cells NYLSVoZtTnWwY4Tpc44h[XO|YYm= M1nJcVI1KGh? M4\kN2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgOUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 M4TrOFIyOjF4MUWx
human H4 cells NH;TU4pHfW6ldHnvckBie3OjeR?= NHn2c5MzKGh? Mo\wSIVkemWjc3WgbY4hTlmYRT3SSnAsKH[nc3njcIUhcW62ZX7zbZR6KHCncjDj[YxtKGmwIHj1cYFvKEh2IHPlcIx{KGGodHXyJFIhcHK|IILlcIF1cX[nIITvJINwdnS{b3y= NHHRcYkyQDB{NEW4OC=>
human MGC803 cells NWG1VoxDTnWwY4Tpc44h[XO|YYm= MX[yOUDPxE1? MY[0PEBp MWnD[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDNS2M5ODNiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEd{L12gdIhie2ViYYSgNlUhfU1iYX\0[ZIhPDhiaILzJJV{cW6pIIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYX\0[ZIhPDhiaILzJIJ6KG[ub4egZ5l1d22ndHXyJJJmdGG2aY\lJJRwKGOxboTyc4w> MYCyOFEyQTh4OR?=

... 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]

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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]

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  • 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]

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  • 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID