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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USD 270 In stock
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Cited by 1011 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 M1PufWNmdGxiaX72ZZNqd25iYYPzZZk> MWSyOEBp NW\DdI46UW6qaXLpeIlwdiCxZjDldIl1cGWuaXHsJIdzd3e2aDDmZYN1d3JvaX7keYNm\CClZXzsJI1q\3KjdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBk\WyuIHnueoF{cW:wIHHzd4F6NCCLQ{WwQVAvOzhizszNMi=> NVTRb2lFOjJ6MESxNFg>
Sf21 cells MYDGeY5kfGmxbjDhd5NigQ>? NFzmPZNKdmirYnn0bY9vKG:oIH3veZNmKHerbHSgeJlx\SCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnOjFiY3XscJMh[29vZYjwdoV{e2mwZzDOMZRmem2rbnHsJGhqey22YXfn[YQhcHWvYX6gdFg2[SC3c3nu[{BNNWGucHjhMZBpd3OyaHH0bYR6dGmwb4PpeI9tKHO3YoP0doF1\SCkeTDUUGMh[mG|ZXSgdIhwe3Cqb4KgbY1i\2mwZzygTWM2OD1yLkWg{txO MlLnNlI2OjB4M{C=
Sf21 cells MYrGeY5kfGmxbjDhd5NigQ>? Ml;ETY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{NWmwZnXjeIVlKFOoMkGgZ4VtdHNuIFnDOVA:OC53IN88UU4> NHm4VngyQTd2OEK2PS=>
Sf9 cells M3fmV2ZtfW:{ZYPj[Y51KHCxbHHybZpifGmxbjDhd5NigQ>? NFnHUodKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vhcJBp[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeTygTWM2OD1yLkW1JO69VS5? MXSyNVEzOTZ|MR?=
THP1 cells NFrtVmFHfW6ldHnvckBie3OjeR?= NVXvRnZ4UW6qaXLpeIlwdiCxZjDTR2YyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0yNjBzIN88UU4> MXSxOlc5QTd2Mh?=
human PC3 cells MV;GeY5kfGmxbjDhd5NigQ>? NWDXdXRKOzBibXnu NIrW[I1KdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGFMXCCyaH;zdIhwenmuYYTpc44h[XRic3XybY5mKDR5MzDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVEvO87:TT6= NGLYRZUzOzRzMECwOS=>
HeLa (human carcinoma) cells. NHjocYRHfW6ldHnvckBie3OjeR?= M3rkNmlvKH[rdILvJIlvcGmkaYTpc44hd2ZiRF7BMYRmeGWwZHXueEBxem:2ZXnuJItqdmG|ZTjEUmEuWEtrIH\yc40hUGWOYTCobJVu[W5iY3HyZ4lvd22jKTDj[YxteyxiSVO1NF0yNjRizszNMi=> MonnNVU3PTh6N{C=
THP1 cells NHT0RnVHfW6ldHnvckBie3OjeR?= NEnie|hKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBVUFBzIHPlcIx{NCCLQ{WwQVEvPjVizszNMi=> NFXVdHQyPjd6OUe0Ni=>
HeLa cells M2rnVWZ2dmO2aX;uJIF{e2G7 MonBTY5pcWKrdHnvckBw\iCvVF;SJJBzd3SnaX6gbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|LDDJR|UxRTJwNTFOwG0v M1rnUVE2PjV6OEew
human MCF7 cells NWnMSXloS3m2b4TvfIlkyqCjc4PhfS=> NGHMUJdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFIxKM7:TTDjbIxwem:zdXnu[UBjgSCVUlKgZZN{[XluIFfJOVA:Oi54MzFOwG0v M1;y[VE5PjlzOEm0
HeLa cells NXPaXWFOTnWwY4Tpc44h[XO|YYm= Mn\qTY5pcWKrdHnvckBw\iCDWD23OVA{KGKrbnTpcochfG9icnXjc41jcW6jboSgVIxsOyCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{BjgSCZZYP0[ZJvKGKub4SsJGlEPT1|IN88UU4> NGrMSY8yPzF|NUK0PC=>
human MCF7 cells NUnZdo96S3m2b4TvfIlkyqCjc4PhfS=> MVvDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME2zMlA5KM7:TT6= MY[xPFY6OTh7NB?=
human MCF7 cells M16zfmN6fG:2b4jpZ:Kh[XO|YYm= MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m9N{4yPiEQvF2u NF3NUWwyQDZ7MUi5OC=>
human MDA-MB-231 cells NXOwfmRVS3m2b4TvfIlkyqCjc4PhfS=> NXzMSGVoS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSU2zMlMzKM7:TT6= MonrNVg3QTF6OUS=
human MDA-MB-231 cells NX3ibXpKS3m2b4TvfIlkyqCjc4PhfS=> MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD12LkO1JO69VS5? MWKxPFY6OTh7NB?=
human MDA-MB-468 cells M{TYOmN6fG:2b4jpZ:Kh[XO|YYm= M33pZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMkCgeW0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H589yNKEmFNUC9OE44PiEQvF2u NF\FXGoyQDZ7MUi5OC=>
human HCT116 cells M2XPUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;IdINqPDhiaB?= NGXsVWtIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKEhzMES3VkBufXSjboSgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13LkOg{txO MU[yNlIyOjd{MR?=
human HCT116 cells NUXHWmg{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYS2S|ZiPDhiaB?= NUPOW2ZCT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IN88UU4> MoHpNlIzOTJ5MkG=
HeLa cells NFHpVmVDcW6maX7nJIFn\mmwaYT5JIF{e2G7 MYnCbY5lcW6pIHHm[olvcXS7IH\vdkBRUTNva3nuZZNmKGm|b3zheIVlKG[{b32gTIVN[SClZXzsd{whU2l;NjFOwG0> NXe1N3J2OTV4NUi4O|A>
human HCT116 cells NWj3ZodFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUHlO4FOPDhiaB?= MkTmS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJHBKO0ujbIDoZUBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[uO{DPxE1w NWP1OGl1OjJ{MUK3NlE>
MDA-MB-231 cells NVfCT2V7S3m2b4TvfIlkyqCjc4PhfS=> NWfNW5hNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi55MTFOwG0v NVHERYdZOTh4OUG4PVQ>
Sf9 cells MnrnSpVv[3Srb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKEONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVYvQSEQvF2u NVm1N216OTh|MkG3NVY>
human U87MG cells M4rqc2Z2dmO2aX;uJIF{e2G7 MkHoTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iVUi3UWch[2WubIOgZpkhTUyLU1GsJGlEPTB;OD6xJO69VS5? MVKxPFM1PTZyOR?=
human MDA-MB-468 cells MYnDfZRwfG:6aXRCpIF{e2G7 Mki3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUS2PEBk\WyuczDpckBxemW|ZX7j[UBw\iBzMDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKPTB;OD6yJO69VS5? NGLubJIyQDZ7MUi5OC=>
human A375 cells NEjoNmlRem:uaX\ldoF1cW:wIHHzd4F6 MVm0OkBp MoizRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDR4IHjyd{whUUN3ME24MlQh|ryPLh?= Mn7kNVcxPDl{NEi=
human A375 cells NUfUVZJFWHKxbHnm[ZJifGmxbjDhd5NigQ>? NFuzdnNKdmirYnn0bY9vKG:oIIPldpVuNWmwZIXj[YQheHKxbHnm[ZJifGmxbjDv[kBpfW2jbjDBN|c2KGOnbHzzMEBKSzVyPUiuOEDPxE1w NFTMSIIyPzZyMUezPS=>
human HL60 cells NWqxS3hQS3m2b4TvfIlkyqCjc4PhfS=> M2XldVczKGh? NVPS[Jd4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvQTRizszNMi=> MYeyNlQ5ODh3MR?=
mouse Raw264 macrophage NGH4WIpHfW6ldHnvckBie3OjeR?= MnrTTY5pcWKrdHnvckBw\iCFNXGtcYVlcWG2ZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gcY92e2ViUnH3NlY1KG2jY4LvdIhi\2VuIFnDOVA:OTBizszNMi=> M2nidlE3Pzh7N{Sy
Sf9 cells MXTGeY5kfGmxbjDhd5NigQ>? NFfQU5lKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgZo93cW6nIGDJN2sh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1zMDFOwG0v MnnWNVA6QTh|NUG=
human MDA-MB-468 cells MUfDfZRwfG:6aXRCpIF{e2G7 M{jvVWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZpkhW1KEIHHzd4F6NCCLQ{WwQVExNjRizszNMi=> NGToVWYyQDZ7MUi5OC=>
human PC3 cell NVT2[HlOWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mne2O|IhcA>? NVvxfYNtUW6qaXLpeIlwdiCxZjDoeY1idiCSQ{OgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MUKuNUDPxE1w NEHLflAzOzRzMECwOS=>
human HL60 cells M3fhfnBzd2yrZnXyZZRqd25iYYPzZZk> NHLHW284OiCq NGDGRldCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUiuOFMh|ryPLh?= NXnjUmxxOjV4OUO3PFc>
human BT474 cell MonCVJJwdGmoZYLheIlwdiCjc4PhfS=> NWfxT2hYPzJiaB?= NUK0NGtOUW6qaXLpeIlwdiCxZjDoeY1idiCEVES3OEBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JJNx\WO2cn;wbI91d22ndILpZ{BidmGueYPpd-+9lCCLQ{WwQVIxNjdizszNMi=> NVHlTHI2OjN2MUCwNFU>
THP1 cells NEWxOY9HfW6ldHnvckBie3OjeR?= M2HxVmlvcGmkaYTpc44hd2ZiTVPQNU1qdmS3Y3XkJINp\W2xdHH4bZMhd2ZiVFjQNUBk\WyuczygTWM2OD1|NzFOwG0v MnXlNVY4QDl5NEK=
human 184B5 cells MX3DfZRwfG:6aXRCpIF{e2G7 MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxPFRDPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OzlwM{eg{txONg>? MYKxPFY6OTh7NB?=
human KB cells NH3aXWVEgXSxdH;4bYPDqGG|c3H5 NE\wcWc4OiCq NXrDUHBkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hU0JiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME20OE44PiEQvF2u NF\SUo0zOTl2NUK1NC=>
mouse RAW264.7 cells MoTUSpVv[3Srb36gZZN{[Xl? M3rReFI2KM7:TR?= NWjrOWVSOjBiaB?= MknFTY5pcWKrdHnvckBw\iCSSUPLM2FMXCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2OgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDJ3IN88UUBi\nSncjCyNEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MkfZNlQzQTl4MU[=
human A2780 cells MWrBdI9xfG:|aYOgZZN{[Xl? NWK3[XJkOiEQvF2= NHLvUFMyOiCq NWHhXYx[UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBkcXOybHH0bY4uemW|aYP0ZY51KGi3bXHuJGEzPzhyIHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJJBpd3OyaH;yfYxifGWmIFHreEBt\X[nbDDheEAzKHWPIHHmeIVzKDF{IHjyd{BjgSCrbX31co9jdG:2IHHuZYx6e2m|Lh?= M4m2OVE4Pjh2MEG4
human SW480 cells M1iyTmZ2dmO2aX;uJIF{e2G7 NXHZTHk1OjBizszN MUCyOEBp MnLRSIVkemWjc3WgbY4he3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCVV{S4NEBk\WyuczDheEAzOCC3TTDh[pRmeiB{NDDodpMh[nliaX3teY5w[myxdDDhcoFtgXOrcx?= M4W0dFE4PDd{OU[y
mouse mast cells M3\vZ2Z2dmO2aX;uJIF{e2G7 NW\TSWRROjBizszN Mm\ETY5pcWKrdHnvckBw\iCVQ1[tbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCvYYP0JINmdGy|IHH0JFIxKM7:TR?= NHHhNJAyPjd6OUe0Ni=>
human BJ cells M2fQdmZ2dmO2aX;uJIF{e2G7 NWP0SWFiOjVizszN NUfucnJDOiCq M2LKW2lvcGmkaYTpc44hd2ZiUFmzT{B{cWewYXzpcochcW5iUFTHSk1{fGmvdXzheIVlKHOncoXtJJN1[XK4ZXSgbJVu[W5iQlqgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCybHHzcYllKEWJRmCvVGgh\G:vYXnuJI9nKEGtdDDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDQTE1GT0[SIILl[Il{fHKrYoX0bY9vKHSxIIDsZZNu[SCvZX3idoFv\SCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDjc45nd2OjbDDtbYNzd3Olb4D5 MnT1NVY4PjdyOEW=
human IGROV1 cells NIrJcVlHfW6ldHnvckBie3OjeR?= NUTLUW5sOjRxNEigbC=> MXvJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MmfKNlEzOTZzNUG=
human IGROV1 cells M2PmTGZ2dmO2aX;uJIF{e2G7 MXeyOE81QCCq NXrMT4tRUW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ5lkdGmwIFSxJIxmfmWuIHH0JFEhfG9iNTD0bY1meyCLQ{WwJIFnfGW{IEK0JJRwKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M3\INlIyOjF4MUWx
rat RBL2H3 cells NGjMSHlHfW6ldHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKEF{M{G4O{1qdmS3Y3XkJIRm\3KjboXsZZRqd25iaX6gdoF1KFKETELIN{Bk\Wyucx?= Mn3iNVg{Ojh5MU[=
human BJ cells NFvjeFNHfW6ldHnvckBie3OjeR?= NGfBc3ozPSEQvF2= MU[yJIg> MmPtRYN1cX[jdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHRpejNyODDpckBRTEeILYP0bY12dGG2ZXSgd4VzfW1ic4ThdpZm\CCqdX3hckBDUiClZXzsd{BifCB{NTD1UUB1emWjdHXkJFIhcHK|IHLl[o9z\SCSRFfGJINp[WyuZX7n[UBjgSCrbX31co9jdG:2dHnu[y=> NXHtXW5WOTZ5NkewPFU>
human HCT116 cells NHn4cXpHfW6ldHnvckBie3OjeR?= MU[xNEDPxE1? MnrCNVAhdWmw MoHhTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJJV{cW6pIGuzNnBeSVSSIHH0JFExKHWPIHHmeIVzKDFyIH3pcpM> NXWwcVNXOjJ{MUK3NlE>
human HCT116 cells MYDGeY5kfGmxbjDhd5NigQ>? M2L0O|ExKM7:TR?= NWXkXFV1OTBibXnu M2PXOmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFixNFQ4WiCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IIXzbY5oKFt|MmDdRXRRKGG2IEGwJJVOKGGodHXyJFExKG2rboO= M1jPNFIzOjF{N{Kx
human HCT116 cells NITSTFJHfW6ldHnvckBie3OjeR?= NVz0c2s2OTBizszN MofSTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRYt1KFOnckS3N{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? NVjHSo1DOjJ{MUK3NlE>
human HCT116 cells NWLy[YlPTnWwY4Tpc44h[XO|YYm= NHjN[nIyOCEQvF2= M2fHVmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIFixNFQ4WiCvdYThcpQhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JHNmejR5MzDwbI9{eGixconsZZRqd25iYYSgNVAhfU1iYomgbY1ufW6xYnzveEBidmGueYPpdy=> Moi5NlIzOTJ5MkG=
human PC3 cells NIHwXW1HfW6ldHnvckBie3OjeR?= M{DPTFUxKM7:TR?= NULG[XhNQCCq MYLJcoR2[3Srb36gc4YheDJzIIDyc5RmcW5iZYjwdoV{e2mxbjDpckBpfW2jbjDQR|Mh[2WubIOgZZQhPTBidV2gbY5kfWKjdHXkJIZweiB6IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5oKHKnbHH0bZZmKHSxIIXueJJm[XSnZDDjc451em:u MkjuNlI6QTh2N{K=
human LNCAP cells MXHGeY5kfGmxbjDhd5NigQ>? MV6wMlEuOzBizszN M2riclMxKG2rbh?= MlW4TY5pcWKrdHnvckBw\iCDa4SgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFzOR2FRKGOnbHzzJIF1KDBwMTD0c{A{OCC3TTDh[pRmeiB|MDDtbY5{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MWWyNlg{OjNzNh?=
human LNCAP cells MX\GeY5kfGmxbjDhd5NigQ>? MY[wMlEuOzBizszN NFzjeFgzPCCq M1z3PGRwf26{ZXf1cIF1cW:wIH;mJJN2en[rdnnuJIV5eHKnc4Ppc44hcW5iaIXtZY4hVE6FQWCgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NEj5TlkzOjh|MkOxOi=>
HUVEC MWfGeY5kfGmxbjDhd5NigQ>? MWixNE0zPSEQvF2= MmK1NVYhcA>? NW\XUlBKUW6qaXLpeIlwdiCxZjDUUmZidHCqYT3zeIlufWyjdHXkJGlESU1vMTDtVm5CKGW6cILld5Nqd25iaX6gTHVXTUNiYYSgNVAhfG9iMkWgeW0heHKndILlZZRm\CCob4KgNVYhcHK|IHLl[o9z\SCWTl\hcJBp[SClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPiCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz MXmyNlAzPjRzMB?=
HUVEC M1WyPWZ2dmO2aX;uJIF{e2G7 MWKxNE0zPSEQvF2= MYOzNEBucW5? MV\Jcohq[mm2aX;uJI9nKFSQRnHsdIhiNXO2aX31cIF1\WRiaIXtZY4hUUODTT2xJJBzd22xdHXyJIFkfGm4aYT5JIV5eHKnc4Pl[EBqdiCKVW\FR{Bie3Onc4Pl[EBieyCkZYThMYdidGGldH;zbYRie2ViYXP0bZZqfHliYYSgNVAhfG9iMkWgeW0heHKndILlZZRm\CCob4KgN|AhdWmwczDi[YZwemViVF7GZYxxcGFiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGy3Y3nm[ZJie2VicnXwc5J1\XJiZ3Xu[UBie3OjeR?= MnvUNlIxOjZ2MUC=
human H1299 cells MULGeY5kfGmxbjDhd5NigQ>? M4KzWVAvOS1|MDFOwG0> MmHTNlQhcA>? NHnqWpRFd3ewIILl[5Vt[XSrb36gc4Yh[0mDUEKg[ZhxemW|c3nvckBqdiCqdX3hckBJOTJ7OTDj[YxteyCjdDCwMlEhfG9iM{CgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MoPUNlI3OjJyNkm=
human H1299 cells M{T6V2Z2dmO2aX;uJIF{e2G7 NVfpblBMOC5zLUOwJO69VQ>? NUnjPYtVOjRiaB?= MVvEc5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjCxNFAhfWdxbXygWHJCUUxiYX7kJHBKO0tiaX7obYJqfG:{IFzZNlk1ODB{ MVSyNlYzOjB4OR?=
human H1299 cells MlXkSpVv[3Srb36gZZN{[Xl? MXKwMlEuOzBizszN M1rtTlI1KGh? MmnXTY5lfWO2aX;uJI9nKESUNTDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NWj0[mx7OjJ4MkKwOlk>
human H1299 cells NInyXFRHfW6ldHnvckBie3OjeR?= MVKwMlEuOzBizszN MnHVNlQhcA>? NVvnXnpNUW6mdXP0bY9vKG:oIFrOT{1u\WSrYYTl[EBEUE:SIHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M2Tvc|IzPjJ{ME[5
HEK293 cells NFXWXlVHfW6ldHnvckBie3OjeR?= NGntRZYyNjViaB?= NInISm1FcXOybHHj[Y1mdnRib3[gX|NJZUyVRDDmdo9uKGi3bXHuJFVJXDZicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkAyNjViaILzJIJ6KGyrcYXp[EB{[2mwdHnscIF1cW:wIHPveY51cW6p M1HlUlIzPTN5MUWz
human U251HRE cells M4n6fmZ2dmO2aX;uJIF{e2G7 Mn\kTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhUEmIMTDhZ5RqfmG2aX;uJIlvKGi3bXHuJHUzPTGKUlWgZ4VtdHNiYomgZ4VtdCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 NVzId4dlOTh3MEG2NFE>
human HCT116 cells NGXwNHlHfW6ldHnvckBie3OjeR?= MnzMNVAh|ryP MXjJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz NXPIUYloOjJ{MUK3NlE>
Sf9 cells NYjLdXRl\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 NFzrRXNKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= MlLMNlEyOjF4M{G=
human HCT116 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 MXi3NkBp NFzONIRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJIFje2:{YnHuZ4Uh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME21NU45OiEQvF2u NXq4TZpuOjV4OUO3PFc>
human HCT116 cells MlLWR5l1d3SxeHnjxsBie3OjeR?= M3i5e|czKGh? MmrrR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVYvODFizszNMi=> MlP2NlE6PDV{NUC=
human PC3 cells M4jKV2N6fG:2b4jpZ:Kh[XO|YYm= M3HnSVczKGh? MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14MT6zOUDPxE1w MVSyNlQ5ODh3MR?=
human HuH7 cells MXrQdo9tcW[ncnH0bY9vKGG|c3H5 MlvZO|IhcA>? NXP6d2hQSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIeWg4KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[3MlE5KM7:TT6= NG\QcJczPTZ7M{e4Oy=>
human A549 cells MlSxVJJwdGmoZYLheIlwdiCjc4PhfS=> NGPFWWc4OiCq MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QDJwM{Kg{txONg>? NFjlPWgzPTZ7M{e4Oy=>
human A549 cells NU\0T2hPS3m2b4TvfIlkyqCjc4PhfS=> NVjyPYhQPzJiaB?= MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= M3nNclIzPDhyOEWx
human PC3 cells MknaVJJwdGmoZYLheIlwdiCjc4PhfS=> MmLqNlUh|ryP MkjqNVIxKGh? MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjdDCyOUB2VSCjZoTldkAyOjBiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDEUXNQ M3P4V|E3PjhyMUW5
human H460 cells NEDEcWVHfW6ldHnvckBie3OjeR?= NYjsboEzOzBizszN MYXJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmeiB2N{OgeZAhfG9iM{CgeW0> MUmxPFUxOTZyMR?=
human IGROV1 cells NImwT2tHfW6ldHnvckBie3OjeR?= M{n5[lI1KGh? NYWwPXJRS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUUeUT2[xJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNUBxcGG|ZTDheEAyKG[xbHSgTWM2OCCjZoTldkAzPCCqcoOgZpkh\myxdzDjfZRwdWW2com= NUe4doJvOjF{MU[xOVE>
human IGROV1 cells MmTBSpVv[3Srb36gZZN{[Xl? NHv6Wo4zPCCq M4HqcmNmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGlIWk:YMTDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiR{GgdIhie2ViYYSgOUBnd2ymIFnDOVAh[W[2ZYKgNlQhcHK|IHL5JIZtd3diY4n0c41mfHK7 NF3Xb48zOTJzNkG1NS=>
human H4 cells NGjqTlhHfW6ldHnvckBie3OjeR?= NYTLc|A1OiCq M3naRWRm[3KnYYPlJIlvKE[\VlWtVmZRMyC4ZYPpZ4xmKGmwdHXud4l1gSCyZYKgZ4VtdCCrbjDoeY1idiCKNDDj[YxteyCjZoTldkAzKGi{czDy[YxifGm4ZTD0c{Bkd262cn;s MliwNVgxOjR3OES=
human MGC803 cells NVnYSVBoTnWwY4Tpc44h[XO|YYm= M{P1SFI2KM7:TR?= NWrIUWxQPDhiaB?= NYnkNJVjS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hVUeFOECzJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNk9OKHCqYYPlJIF1KDJ3IIXNJIFnfGW{IES4JIhzeyC3c3nu[{Bxem:yaXTpeY0hcW:maXTlJJN1[WmwaX7nJIFnfGW{IES4JIhzeyCkeTDmcI94KGO7dH;t[ZRmeiC{ZXzheIl3\SC2bzDjc451em:u NHnQcXozPDFzOUi2PS=>

... 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
  • 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.

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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