LY294002

For research use only.

Catalog No.S1105 Synonyms: SF 1101, NSC 697286

1155 publications

LY294002 Chemical Structure

CAS No. 154447-36-6

LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.

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Selleck's LY294002 has been cited by 1155 publications

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Choose Selective PI3K Inhibitors

Biological Activity

Description LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Targets
p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)		 DNA-PK [6]
(Cell-free)
0.5 μM 0.57 μM 0.97 μM 1.4 μM
In vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells MXfD[YxtKGmwdnHzbY9vKGG|c3H5 NUW2WVE2OjRiaB?= MXrJcohq[mm2aX;uJI9nKGWyaYTo[Yxq[WxiZ4Lve5RpKG[jY4Tvdk1qdmS3Y3XkJINmdGxibXnndoF1cW:wIH;mJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiMkSgbJJ{KGK7IHPlcIwhcW64YYPpc44h[XO|YYmsJGlEPTB;MD6zPEDPxE1w NVrZfnZbOjJ6MESxNFg>
Sf21 cells NVzpWY9UTnWwY4Tpc44h[XO|YYm= MmnYTY5pcWKrdHnvckBw\iCvb4Xz[UB4cWymIIT5dIUhWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lIyKGOnbHzzJINwNWW6cILld5NqdmdiTj30[ZJucW6jbDDIbZMufGGpZ3XkJIh2dWGwIIC4OYEhfXOrbnegUE1idHCqYT3wbI9{eGijdHnkfYxqdm:|aYTvcEB{fWK|dILheIUh[nliVFzDJIJie2WmIIDoc5NxcG:{IHntZYdqdmduIFnDOVA:OC53IN88US=> M4HxUVIzPTJyNkOw
Sf21 cells M2ruV2Z2dmO2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKG2xdYPlJJJm[2:vYnnuZY51KFCLM1vhcJBp[SCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMucW6oZXP0[YQhW2Z{MTDj[YxteyxiSVO1NF0xNjVizszNMi=> NEfjXGQyQTd2OEK2PS=>
Sf9 cells NFXacYFHdHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? NWDCOFN3UW6qaXLpeIlwdiCxZjDoeY1idiCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTB;MD61OUDPxE1w M4ryR|IyOTJzNkOx
THP1 cells NGXSfW5HfW6ldHnvckBie3OjeR?= NFLBUnJKdmirYnn0bY9vKG:oIGPDSlEucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBVUFBzIHPlcIx{NCCLQ{WwQVEvODFizszNMi=> M{e1dVE3Pzh7N{Sy
human PC3 cells M2q2SGZ2dmO2aX;uJIF{e2G7 NXXuPYpWOzBibXnu NITZRolKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGFMXCCyaH;zdIhwenmuYYTpc44h[XRic3XybY5mKDR5MzDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVEvO87:TT6= M1ntWlI{PDFyMEC1
HeLa (human carcinoma) cells. MVnGeY5kfGmxbjDhd5NigQ>? MUnJckB3cXS{bzDpcohq[mm2aX;uJI9nKESQQT3k[ZBmdmSnboSgdJJwfGWrbjDrbY5ie2VqRF7BMXBMMSCocn;tJGhmVGFiKHj1cYFvKGOjcnPpco9u[SliY3XscJMtKEmFNUC9NU41KM7:TT6= M3vNOlE2PjV6OEew
THP1 cells MnvkSpVv[3Srb36gZZN{[Xl? NUDNTGdEUW6qaXLpeIlwdiCxZjDNR3AyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0yNjZ3IN88UU4> NHvpN48yPjd6OUe0Ni=>
HeLa cells NIfVbFdHfW6ldHnvckBie3OjeR?= MnnzTY5pcWKrdHnvckBw\iCvVF;SJJBzd3SnaX6gbZNwdGG2ZXSg[pJwdSCKZVzhJINmdGy|LDDJR|UxRTJwNTFOwG0v MXSxOVY2QDh5MB?=
human MCF7 cells MWDDfZRwfG:6aXRCpIF{e2G7 NUTWOlhRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAzOCEQvF2gZ4htd3KxcYXpcoUh[nliU2LCJIF{e2G7LDDHTVUxRTJwNkOg{txONg>? NVS4Z4lVOTh4OUG4PVQ>
HeLa cells NG\KSYNHfW6ldHnvckBie3OjeR?= M4XtfGlvcGmkaYTpc44hd2ZiQWitO|UxOyCkaX7kbY5oKHSxIILlZ49u[mmwYX70JHBtczNiZYjwdoV{e2WmIHnuJGhmVGFiY3XscJMh[nliV3XzeIVzdiCkbH;0MEBKSzV;MzFOwG0v NVjGW|M4OTdzM{WyOFg>
human MCF7 cells NELIW4ZEgXSxdH;4bYPDqGG|c3H5 NIjpboREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExKHWPIHPocI9zd3G3aX7lJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjB6IN88UU4> MkLFNVg3QTF6OUS=
human MCF7 cells NFTjepdEgXSxdH;4bYPDqGG|c3H5 NGriUFJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k:Oy5zNjFOwG0v NXzCOWQxOTh4OUG4PVQ>
human MDA-MB-231 cells MnrRR5l1d3SxeHnjxsBie3OjeR?= NXvsZY44S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSU2zMlMzKM7:TT6= M4PRcFE5PjlzOEm0
human MDA-MB-231 cells M1SyTmN6fG:2b4jpZ:Kh[XO|YYm= MoHER5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDpckBxemW|ZX7j[UBw\iBzMDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKPTB;ND6zOUDPxE1w MYGxPFY6OTh7NB?=
human MDA-MB-468 cells NEnRTGpEgXSxdH;4bYPDqGG|c3H5 MUjDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3Ojef-8kEBKSzVyPUSuO|Yh|ryPLh?= NV;QVFc1OTh4OUG4PVQ>
human HCT116 cells M17Cfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rrZVQ5KGh? NVrJemVHT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT6zJO69VQ>? MV2yNlIyOjd{MR?=
human HCT116 cells M2T3eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\SOFghcA>? NHXpcpdIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF02NjhizszNMi=> MnX4NlIzOTJ5MkG=
HeLa cells NEnNS5BDcW6maX7nJIFn\mmwaYT5JIF{e2G7 MVHCbY5lcW6pIHHm[olvcXS7IH\vdkBRUTNva3nuZZNmKGm|b3zheIVlKG[{b32gTIVN[SClZXzsd{whU2l;NjFOwG0> MnjNNVU3PTh6N{C=
human HCT116 cells MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjLfGY1QCCq NVXocoxrT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVYvPyEQvF2u M2jKR|IzOjF{N{Kx
MDA-MB-231 cells MlmyR5l1d3SxeHnjxsBie3OjeR?= NX;rWoJGS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi55MTFOwG0v NGLHc48yQDZ7MUi5OC=>
Sf9 cells MXTGeY5kfGmxbjDhd5NigQ>? MVPJcohq[mm2aX;uJI9nKEONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVYvQSEQvF2u NY\NXGdDOTh|MkG3NVY>
human U87MG cells M1y5NGZ2dmO2aX;uJIF{e2G7 MV;Jcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCXOEfNS{Bk\WyuczDifUBGVEmVQTygTWM2OD16LkGg{txONg>? MXixPFM1PTZyOR?=
human MDA-MB-468 cells NIXYbYdEgXSxdH;4bYPDqGG|c3H5 MXLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD16LkKg{txONg>? NVzrUXRjOTh4OUG4PVQ>
human A375 cells NVflWlRuWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUK0OkBp M1zkOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB2NjDodpMtKEmFNUC9PE41KM7:TT6= Mlu5NVcxPDl{NEi=
human A375 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 MofQTY5pcWKrdHnvckBw\iC|ZYL1cU1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gbJVu[W5iQUO3OUBk\WyuczygTWM2OD16LkSg{txONg>? MljpNVc3ODF5M{m=
human HL60 cells NHrH[3pEgXSxdH;4bYPDqGG|c3H5 NXnvRWMxPzJiaB?= MV;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIUFYxKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;OT65OEDPxE1w MYeyNlQ5ODh3MR?=
mouse Raw264 macrophage MX;GeY5kfGmxbjDhd5NigQ>? NVXPdodOUW6qaXLpeIlwdiCxZjDDOYEudWWmaXH0[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hdW:3c3WgVoF4OjZ2IH3hZ5JweGijZ3WsJGlEPTB;MUCg{txONg>? MVOxOlc5QTd2Mh?=
Sf9 cells NUDTfGxETnWwY4Tpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKEircz30ZYdo\WRiYn;2bY5mKFCLM1ug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyxiSVO1NF0yOCEQvF2u MWCxNFk6QDN3MR?=
human MDA-MB-468 cells M1vYWmN6fG:2b4jpZ:Kh[XO|YYm= M3;zNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZpkhW1KEIHHzd4F6NCCLQ{WwQVExNjRizszNMi=> Mn\5NVg3QTF6OUS=
human PC3 cell Mn\KVJJwdGmoZYLheIlwdiCjc4PhfS=> NXm0XZBEPzJiaB?= NWPZWJVHUW6qaXLpeIlwdiCxZjDoeY1idiCSQ{OgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MUKuNUDPxE1w MYqyN|QyODByNR?=
human HL60 cells MVnQdo9tcW[ncnH0bY9vKGG|c3H5 M3vkWVczKGh? M{m5e2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1zOD60N{DPxE1w MWWyOVY6Ozd6Nx?=
human BT474 cell Mm\0VJJwdGmoZYLheIlwdiCjc4PhfS=> M4jRTFczKGh? M2\KbmlvcGmkaYTpc44hd2ZiaIXtZY4hSlR2N{SgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYRvwKwhUUN3ME2yNE44KM7:TT6= M1r3NlI{PDFyMEC1
THP1 cells NHXQPWRHfW6ldHnvckBie3OjeR?= MWDJcohq[mm2aX;uJI9nKE2FUEGtbY5lfWOnZDDjbIVud3SjeHnzJI9nKFSKUEGgZ4VtdHNuIFnDOVA:OzdizszNMi=> M2rmd|E3Pzh7N{Sy
human 184B5 cells NF[xUFNEgXSxdH;4bYPDqGG|c3H5 M2fCdWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJFE5PEJ3IHPlcIx{KGK7IGPSRkBie3OjeTygS2k2OD1|OT6zO{DPxE1w MnriNVg3QTF6OUS=
human KB cells MoXYR5l1d3SxeHnjxsBie3OjeR?= M2q2ZVczKGh? NILo[JFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUS0Mlc3KM7:TT6= M2\CdFIyQTR3MkWw
mouse RAW264.7 cells NEfacmZHfW6ldHnvckBie3OjeR?= NGLreYgzPSEQvF2= NYSyeWlrOjBiaB?= M{PzVmlvcGmkaYTpc44hd2ZiUFmzT{9CU1RiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCrTl;TJJBzd3SnaX6g[ZhxemW|c3nvckBifCB{NTFOwG0h[W[2ZYKgNlAhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MlHmNlQzQTl4MU[=
human A2780 cells MWjBdI9xfG:|aYOgZZN{[Xl? NGm4N5MzKM7:TR?= NXH2S2JJOTJiaB?= MljiTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDjbZNxdGG2aX6tdoV{cXO2YX70JIh2dWGwIFGyO|gxKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIIDoc5NxcG:{eXzheIVlKEGtdDDs[ZZmdCCjdDCyJJVOKGGodHXyJFEzKGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{Ng>? M1;vO|E4Pjh2MEG4
human SW480 cells M37lWmZ2dmO2aX;uJIF{e2G7 M1jCdlIxKM7:TR?= NWnTTHZsOjRiaB?= M4jreWRm[3KnYYPlJIlvKHO3co\peolvKGW6cILld5Nqd25iaX6gbJVu[W5iU2e0PFAh[2WubIOgZZQhOjBidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4SgZY5idHm|aYO= MUCxO|Q4Ojl4Mh?=
mouse mast cells MmPWSpVv[3Srb36gZZN{[Xl? NHvNUJAzOCEQvF2= NHzTO2FKdmirYnn0bY9vKG:oIGPDSk1qdmS3Y3XkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIH3hd5Qh[2WubIOgZZQhOjBizszN Ml\LNVY4QDl5NEK=
human BJ cells NULVNGVYTnWwY4Tpc44h[XO|YYm= MUKyOUDPxE1? NYK4V2xLOiCq NYnhPVhMUW6qaXLpeIlwdiCxZjDQTVNMKHOrZ37hcIlv\yCrbjDQSGdHNXO2aX31cIF1\WRic3XyeY0he3Sjco\l[EBpfW2jbjDCTkBk\WyuczD0doFve2[nY4Tl[EB4cXSqIIDsZZNucWRiRVfGVE9RUCCmb33hbY4hd2ZiQXv0JIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJHBJNUWJRmCgdoVlcXO2cnnieZRqd25idH:gdIxie22jIH3lcYJz[W6nIHH0JFI2KHWPIITy[YF1\WRiMjDodpMh[mWob4LlJHBFT0ZiY3jhcIxmdmenIHL5JINwdm[xY3HsJI1q[3Kxc3PvdJk> NEP2NI0yPjd4N{C4OS=>
human IGROV1 cells MYHGeY5kfGmxbjDhd5NigQ>? M3Xqe|I1NzR6IHi= NGO2W21KdmirYnn0bY9vKG:oIGDJN2swSWu2IHnuJIh2dWGwIFnHVm9XOSClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDS2SgcIV3\WxiYYSgNUB1dyB3IITpcYV{KEmFNUCgZYZ1\XJiMkSgeI8hPDhiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NF;5emEzOTJzNkG1NS=>
human IGROV1 cells NF3RWIZHfW6ldHnvckBie3OjeR?= MlziNlQwPDhiaB?= NVvVdpZ2UW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ5lkdGmwIFSxJIxmfmWuIHH0JFEhfG9iNTD0bY1meyCLQ{WwJIFnfGW{IEK0JJRwKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MlvvNlEzOTZzNUG=
rat RBL2H3 cells NVTPRXJzTnWwY4Tpc44h[XO|YYm= M2jYSGlvcGmkaYTpc44hd2ZiQUKzNVg4NWmwZIXj[YQh\GWpcnHueYxifGmxbjDpckBz[XRiUlLMNmg{KGOnbHzz NWC0SmZjOTh|Mki3NVY>
human BJ cells MYrGeY5kfGmxbjDhd5NigQ>? M3yzUlI2KM7:TR?= NYOy[ZBROiCq M{OzbGFkfGm4YYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDheEBVcHJ|MEigbY4hWESJRj3zeIlufWyjdHXkJJNmenWvIIP0ZZJ3\WRiaIXtZY4hSkpiY3XscJMh[XRiMkWgeW0hfHKnYYTl[EAzKGi{czDi[YZwemViUFTHSkBkcGGubHXu[4Uh[nliaX3teY5w[myxdITpcoc> NXHsWG9[OTZ5NkewPFU>
human HCT116 cells MlvYSpVv[3Srb36gZZN{[Xl? NIXIcmYyOCEQvF2= NYX3ZmlyOTBibXnu MXfJcohq[mm2aX;uJI9nKFCLM1vhcJBp[SCrbjDoeY1idiCKQ2SxNVYh[2WubIOgeZNqdmdiW{OyVH1CXFBiYYSgNVAhfU1iYX\0[ZIhOTBibXnudy=> M{fNN|IzOjF{N{Kx
human HCT116 cells M3\CNGZ2dmO2aX;uJIF{e2G7 MUWxNEDPxE1? NXPqboFHOTBibXnu Mom3TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNidYPpcochYzN{UG3BWHAh[XRiMUCgeW0h[W[2ZYKgNVAhdWmwcx?= MkGyNlIzOTJ5MkG=
human HCT116 cells MUHGeY5kfGmxbjDhd5NigQ>? NIfZXXMyOCEQvF2= M1HNNmlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGFsfCCVZYK0O|MheGixc4Doc5J6dGG2aX;uJIF1KDFyIIXNJIJ6KGmvbYXuc4Jtd3RiYX7hcJl{cXN? NV;3THM2OjJ{MUK3NlE>
human HCT116 cells NYn2OFhwTnWwY4Tpc44h[XO|YYm= NH;pNm4yOCEQvF2= MlLETY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MkHrNlIzOTJ5MkG=
human PC3 cells MnvLSpVv[3Srb36gZZN{[Xl? M4fFU|UxKM7:TR?= NF\IdVk5KGh? NXTv[nRoUW6mdXP0bY9vKG:oIICyNUBxem:2ZXnuJIV5eHKnc4Ppc44hcW5iaIXtZY4hWEN|IHPlcIx{KGG2IEWwJJVOKGmwY4XiZZRm\CCob4KgPEBpenNiYomgW4V{fGW{bjDicI91fGmwZzDy[YxifGm4ZTD0c{B2dnS{ZXH0[YQh[2:wdILvcC=> MWKyNlk6QDR5Mh?=
human LNCAP cells MXPGeY5kfGmxbjDhd5NigQ>? M1y2XVAvOS1|MDFOwG0> M1\E[VMxKG2rbh?= M3fxNWlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiM{CgcYlveyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NFmzUXczOjh|MkOxOi=>
human LNCAP cells NHH2N3lHfW6ldHnvckBie3OjeR?= MmLaNE4yNTNyIN88US=> MUGyOEBp NYPYbJJJTG:5boLl[5Vt[XSrb36gc4Yhe3W{dnn2bY4h\XiycnXzd4lwdiCrbjDoeY1idiCOTlPBVEBk\WyuczDheEAxNjFidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NEDnUVgzOjh|MkOxOi=>
HUVEC MXfGeY5kfGmxbjDhd5NigQ>? M3;nWlExNTJ3IN88US=> MlXBNVYhcA>? NEmzVZZKdmirYnn0bY9vKG:oIGTOSoFteGijLYP0bY12dGG2ZXSgTWNCVS1zIH3SUmEh\XiycnXzd4lwdiCrbjDIWXZGSyCjdDCxNEB1dyB{NTD1UUBxemW2cnXheIVlKG[xcjCxOkBpenNiYnXmc5JmKFSQRnHsdIhiKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkA3KGi{czDifUBTXC2SQ2KgZY5idHm|aYO= NXTENnB[OjJyMk[0NVA>
HUVEC MnLoSpVv[3Srb36gZZN{[Xl? NXjl[I1COTBvMkWg{txO M1rvZ|MxKG2rbh?= M{nHWmlvcGmkaYTpc44hd2ZiVF7GZYxxcGFvc4TpcZVt[XSnZDDoeY1idiCLQ1HNMVEheHKxbX;0[ZIh[WO2aY\peJkh\XiycnXzd4VlKGmwIFjVWmVEKGG|c3Xzd4VlKGG|IHLleIEu\2GuYXP0c5Nq\GG|ZTDhZ5Rqfmm2eTDheEAyOCC2bzCyOUB2VSCycnX0doVifGWmIH\vdkA{OCCvaX7zJIJm\m:{ZTDUUmZidHCqYTDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiNTDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 MWWyNlAzPjRzMB?=
human H1299 cells NFPMS2pHfW6ldHnvckBie3OjeR?= MlnZNE4yNTNyIN88US=> NYrGSmdHOjRiaB?= MYfEc5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M1\FXFIzPjJ{ME[5
human H1299 cells MX;GeY5kfGmxbjDhd5NigQ>? M3jPclAvOS1|MDFOwG0> NFfyN2wzPCCq MofiSI94diC{ZXf1cIF1cW:wIH;mJINKSVB{IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gNVAxKHWpL33sJHRTSUmOIHHu[EBRUTONIHnubIljcXSxcjDMXVI6PDByMh?= M3HSVVIzPjJ{ME[5
human H1299 cells NULiV3d5TnWwY4Tpc44h[XO|YYm= NXe5TY5QOC5zLUOwJO69VQ>? MlvONlQhcA>? NFL5SpNKdmS3Y4Tpc44hd2ZiRGK1JIV5eHKnc4Ppc44hcW5iaIXtZY4hUDF{OUmgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NGr0XokzOjZ{MkC2PS=>
human H1299 cells Mm\GSpVv[3Srb36gZZN{[Xl? MWKwMlEuOzBizszN NYLocpJZOjRiaB?= NYnlOY9{UW6mdXP0bY9vKG:oIFrOT{1u\WSrYYTl[EBEUE:SIHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MV[yNlYzOjB4OR?=
HEK293 cells NXru[ZpmTnWwY4Tpc44h[XO|YYm= MUmxMlUhcA>? MoXsSIl{eGyjY3Xt[Y51KG:oIGuzTH1NW0RiZoLvcUBpfW2jbjC1THQ3KHKnY3XweI9zKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[W[2ZYKgNU42KGi{czDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\w>? NYnuSoIxOjJ3M{exOVM>
human U251HRE cells NEnjXolHfW6ldHnvckBie3OjeR?= M{LaRWlvcGmkaYTpc44hd2ZiaInwc5hq[S2rbnT1Z4VlKEiLRkGgZYN1cX[jdHnvckBqdiCqdX3hckBWOjVzSGLFJINmdGy|IHL5JINmdGxiYnHz[YQhemWyb4L0[ZIh\2WwZTDhd5NigQ>? M2O5OFE5PTBzNkCx
human HCT116 cells MkLISpVv[3Srb36gZZN{[Xl? NITDT5MyOCEQvF2= M2\iXmlvcGmkaYTpc44hd2ZiQXv0JIV5eHKnc4Ppc44hcW5iaIXtZY4hUEOWMUG2JINmdGy|IHH0JFExKHWPIHL5JIludXWwb3Lsc5Qh[W6jbInzbZM> NXTMc5pxOjJ{MUK3NlE>
Sf9 cells NVrKfHhT\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 NFfmZ25KdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= NFWw[GQzOTF{MU[zNS=>
human HCT116 cells M13CNnBzd2yrZnXyZZRqd25iYYPzZZk> MkP4O|IhcA>? NVrDSW1USW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBi[nOxcnLhcoNmKGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVEvQDJizszNMi=> M2[zUVI2Pjl|N{i3
human HCT116 cells M2\OOWN6fG:2b4jpZ:Kh[XO|YYm= M3XKe|czKGh? Ml3SR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9OVYvODFizszNMi=> MlzVNlE6PDV{NUC=
human PC3 cells M{D0bmN6fG:2b4jpZ:Kh[XO|YYm= MXW3NkBp MnntR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NkGuN|Uh|ryPLh?= MmjENlI1QDB6NUG=
human HuH7 cells NV:2cZRQWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHraSWY4OiCq MVPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PjdwMUig{txONg>? MXeyOVY6Ozd6Nx?=
human A549 cells NVTnb4NrWHKxbHnm[ZJifGmxbjDhd5NigQ>? NIrs[|U4OiCq MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QDJwM{Kg{txONg>? NYq3S5B6OjV4OUO3PFc>
human A549 cells M{DtVGN6fG:2b4jpZ:Kh[XO|YYm= M3K3[lczKGh? NWDMfWlRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 M1W5TVIzPDhyOEWx
human PC3 cells MlK5VJJwdGmoZYLheIlwdiCjc4PhfS=> NIr5dGozPSEQvF2= MljNNVIxKGh? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjdDCyOUB2VSCjZoTldkAyOjBiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDEUXNQ NWLWdHN1OTZ4OECxOVk>
human H460 cells NHfqNGdHfW6ldHnvckBie3OjeR?= MVOzNEDPxE1? MVHJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gTFQ3OCClZXzsd{Bie3Onc4Pl[EBieyCDa4SgdIhwe3Cqb4L5cIF1cW:wIHH0JHNmeiB2N{OgeZAhfG9iM{CgeW0> NUeyVVNjOTh3MEG2NFE>
human IGROV1 cells M4S1Z2Z2dmO2aX;uJIF{e2G7 MXuyOEBp NELRO5ZE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBKT1KRVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexJJBp[XOnIHH0JFEh\m:uZDDJR|UxKGGodHXyJFI1KGi{czDifUBndG:5IHP5eI9u\XS{eR?= NWrWO2RlOjF{MU[xOVE>
human IGROV1 cells NVjDTFdLTnWwY4Tpc44h[XO|YYm= M2nxS|I1KGh? NFnS[VhE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBKT1KRVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexJJBp[XOnIHH0JFUh\m:uZDDJR|UxKGGodHXyJFI1KGi{czDifUBndG:5IHP5eI9u\XS{eR?= M3XmVVIyOjF4MUWx
human H4 cells MW\GeY5kfGmxbjDhd5NigQ>? NU\jclJUOiCq MXvE[YNz\WG|ZTDpckBHYV[HLWLGVEshfmW|aXPs[UBqdnSnboPpeJkheGW{IHPlcIwhcW5iaIXtZY4hUDRiY3XscJMh[W[2ZYKgNkBpenNicnXsZZRqfmVidH:gZ49vfHKxbB?= M4izOVE5ODJ2NUi0
human MGC803 cells MXPGeY5kfGmxbjDhd5NigQ>? NFLKd2MzPSEQvF2= NWHNTVRwPDhiaB?= NFPPfpNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOT0N6MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZZQhOjVidV2gZYZ1\XJiNEigbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZYZ1\XJiNEigbJJ{KGK7IH\sc5ch[3m2b33leIVzKHKnbHH0bZZmKHSxIHPvcpRzd2x? MkC4NlQyOTl6Nkm=

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

PubMed: 29731993     


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

beta-catenin / p-GSK3β / Cyclin D1; 

PubMed: 29731993     


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

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

PubMed: 25344912     


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

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

PubMed: 23251002     


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

pPKB-S473; 

PubMed: 20649566     


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

29731993 25344912 23251002 20649566
Growth inhibition assay
Cell viability; 

PubMed: 25344912     


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

25344912
Immunofluorescence
α-SMA / CD31; 

PubMed: 27671604     


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

E-cadherin / beta-catenin; 

PubMed: 29731993     


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

COX-2 / p-NFκB; 

PubMed: 29731993     


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

FOXO3a; 

PubMed: 18388194     


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

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

PubMed: 22208359     


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

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

Protocol

Kinase Assay:

[4]
- Collapse

kinase assays:

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

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

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


    (Only for Reference)
Animal Research:

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 307.34
Formula

C19H17NO3
CAS No. 154447-36-6
Storage powder
in solvent
Synonyms SF 1101, NSC 697286
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4

In vivo Formulation Calculator (Clear solution)

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

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

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

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

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

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

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Tech Support

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

Handling Instructions

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

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

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Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

  • Question 2:

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

  • Answer:

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

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    Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

    Features:A beta isoform-sparing PI3K inhibitor.

  • Pilaralisib (XL147) New

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

  • GNE-317 New

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

  • 3-Methyladenine (3-MA)

    3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.

  • Idelalisib (CAL-101, GS-1101)

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

  • Wortmannin

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

  • Dactolisib (BEZ235)

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

  • Buparlisib (BKM120)

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

  • Pictilisib (GDC-0941)

    Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

  • Alpelisib (BYL719)

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID