LY294002

For research use only.

Catalog No.S1105 Synonyms: SF 1101, NSC 697286

1164 publications

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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Selleck's LY294002 has been cited by 1164 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 NGDKVVJE\WyuIHnueoF{cW:wIHHzd4F6 MmrrNlQhcA>? NUfBOXN3UW6qaXLpeIlwdiCxZjDldIl1cGWuaXHsJIdzd3e2aDDmZYN1d3JvaX7keYNm\CClZXzsJI1q\3KjdHnvckBw\iCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJJBz\S2rbnP1ZoF1\WRiZn;yJFI1KGi{czDifUBk\WyuIHnueoF{cW:wIHHzd4F6NCCLQ{WwQVAvOzhizszNMi=> NEfwSoYzOjhyNEGwPC=>
Sf21 cells NVj0dFZbTnWwY4Tpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKG2xdYPlJJdqdGRidInw[UBRUTONYXzwbIEh\XiycnXzd4VlKGmwIGPmNlEh[2WubIOgZ48u\XiycnXzd4lv\yCQLYTldo1qdmGuIFjpd{11[WepZXSgbJVu[W5icEi1ZUB2e2mwZzDMMYFteGijLYDoc5NxcGG2aXT5cIlvd3OrdH;sJJN2[nO2cnH0[UBjgSCWTFOgZoF{\WRicHjvd5Bpd3JiaX3h[4lv\yxiSVO1NF0xNjVizszN MnTRNlI2OjB4M{C=
Sf21 cells NIf5OJBHfW6ldHnvckBie3OjeR?= NIPrWY1KdmirYnn0bY9vKG:oIH3veZNmKHKnY3;tZolv[W62IGDJN2tidHCqYTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNvaX7m[YN1\WRiU3[yNUBk\WyuczygTWM2OD1yLkWg{txONg>? NWjZfmIzOTl5NEiyOlk>
Sf9 cells MVXGcJVwemW|Y3XueEBxd2yjcnn6ZZRqd25iYYPzZZk> M2rzO2lvcGmkaYTpc44hd2ZiaIXtZY4hWEl|S3HsdIhiKGW6cILld5Nm\CCrbjDT[lkh[2WubIOgZpkh\my3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7LDDJR|UxRTBwNUWg{txONg>? M3\4OlIyOTJzNkOx
THP1 cells NFrGO4RHfW6ldHnvckBie3OjeR?= NI\veYdKdmirYnn0bY9vKG:oIGPDSlEucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBVUFBzIHPlcIx{NCCLQ{WwQVEvODFizszNMi=> MUixOlc5QTd2Mh?=
human PC3 cells MlrSSpVv[3Srb36gZZN{[Xl? MnnxN|AhdWmw MX3Jcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhe2W{aX7lJFQ4OyCjZoTldkA{OCCvaX7zJIJ6KEWOSWPBMEBKSzVyPUGuN:69VS5? MojENlM1OTByMEW=
HeLa (human carcinoma) cells. MX3GeY5kfGmxbjDhd5NigQ>? MXTJckB3cXS{bzDpcohq[mm2aX;uJI9nKESQQT3k[ZBmdmSnboSgdJJwfGWrbjDrbY5ie2VqRF7BMXBMMSCocn;tJGhmVGFiKHj1cYFvKGOjcnPpco9u[SliY3XscJMtKEmFNUC9NU41KM7:TT6= MXqxOVY2QDh5MB?=
THP1 cells MXHGeY5kfGmxbjDhd5NigQ>? MnL0TY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gWGhROSClZXzsd{whUUN3ME2xMlY2KM7:TT6= MUWxOlc5QTd2Mh?=
HeLa cells M2rYeWZ2dmO2aX;uJIF{e2G7 MWnJcohq[mm2aX;uJI9nKG2WT2KgdJJwfGWrbjDpd49t[XSnZDDmdo9uKEinTHGgZ4VtdHNuIFnDOVA:Oi53IN88UU4> MUKxOVY2QDh5MB?=
human MCF7 cells MXHDfZRwfG:6aXRCpIF{e2G7 NXXidlJxS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAzOCEQvF2gZ4htd3KxcYXpcoUh[nliU2LCJIF{e2G7LDDHTVUxRTJwNkOg{txONg>? NF31[3UyQDZ7MUi5OC=>
HeLa cells M{P5OGZ2dmO2aX;uJIF{e2G7 M1HhPWlvcGmkaYTpc44hd2ZiQWitO|UxOyCkaX7kbY5oKHSxIILlZ49u[mmwYX70JHBtczNiZYjwdoV{e2WmIHnuJGhmVGFiY3XscJMh[nliV3XzeIVzdiCkbH;0MEBKSzV;MzFOwG0v M3nWb|E4OTN3MkS4
human MCF7 cells MX7DfZRwfG:6aXRCpIF{e2G7 NUfVXopES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAyOCC3TTDjbIxwem:zdXnu[UBjgSCVUlKgZZN{[XluIFfJOVA:Oy5yODFOwG0v NXjGW2JZOTh4OUG4PVQ>
human MCF7 cells M2PBdWN6fG:2b4jpZ:Kh[XO|YYm= Mlq0R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BjgSCVUlKgZZN{[XluIFfJQVMvOTZizszNMi=> MYCxPFY6OTh7NB?=
human MDA-MB-231 cells NEK5d2NEgXSxdH;4bYPDqGG|c3H5 NI\ROGFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJO69VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLPUOuN|Ih|ryPLh?= M1\aRlE5PjlzOEm0
human MDA-MB-231 cells M2n3TWN6fG:2b4jpZ:Kh[XO|YYm= NYf3NnRXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCxNEB2VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLNUC9OE4{PSEQvF2u M3Owd|E5PjlzOEm0
human MDA-MB-468 cells NV;LR3BJS3m2b4TvfIlkyqCjc4PhfS=> MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3Ojef-8kEBKSzVyPUSuO|Yh|ryPLh?= NV\GTWM1OTh4OUG4PVQ>
human HCT116 cells MoDyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUm0PEBp NEnIWmNIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKEhzMES3VkBufXSjboSgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13LkOg{txO M{jGfVIzOjF{N{Kx
human HCT116 cells MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVXyRXNzPDhiaB?= M2nuPGdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2u NWDVfFdtOjJ{MUK3NlE>
HeLa cells M13BR2JqdmSrbnegZYZncW6rdImgZZN{[Xl? MYrCbY5lcW6pIHHm[olvcXS7IH\vdkBRUTNva3nuZZNmKGm|b3zheIVlKG[{b32gTIVN[SClZXzsd{whU2l;NjFOwG0> MlHTNVU3PTh6N{C=
human HCT116 cells MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfDOFghcA>? NXPjfoV7T3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVYvPyEQvF2u MUGyNlIyOjd{MR?=
MDA-MB-231 cells MWrDfZRwfG:6aXRCpIF{e2G7 M3vnfGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvPzFizszNMi=> M2TCflE5PjlzOEm0
Sf9 cells MofhSpVv[3Srb36gZZN{[Xl? NFqyZ|dKdmirYnn0bY9vKG:oIFPLNkBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTZwOTFOwG0v NX75To9mOTh|MkG3NVY>
human U87MG cells M17Be2Z2dmO2aX;uJIF{e2G7 NYPFPIU2UW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgbY4hcHWvYX6gWVg4VUdiY3XscJMh[nliRVzJV2EtKEmFNUC9PE4yKM7:TT6= NH3C[ZYyQDN2NU[wPS=>
human MDA-MB-468 cells NHG2cGxEgXSxdH;4bYPDqGG|c3H5 M1zWTGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMUCgeW0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H5MEBIUTVyPUiuNkDPxE1w NFXkNFMyQDZ7MUi5OC=>
human A375 cells NIr3bGJRem:uaX\ldoF1cW:wIHHzd4F6 MX20OkBp MkD2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDR4IHjyd{whUUN3ME24MlQh|ryPLh?= NXLheYJJOTdyNEmyOFg>
human A375 cells MoP0VJJwdGmoZYLheIlwdiCjc4PhfS=> M3zkZWlvcGmkaYTpc44hd2Zic3XyeY0ucW6mdXPl[EBxem:uaX\ldoF1cW:wIH;mJIh2dWGwIFGzO|Uh[2WubIOsJGlEPTB;OD60JO69VS5? NG\sZnIyPzZyMUezPS=>
human HL60 cells NWTIdYNES3m2b4TvfIlkyqCjc4PhfS=> MnXmO|IhcA>? NHLvVItEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJVDZyIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9PU46PCEQvF2u NILHc5czOjR6MEi1NS=>
mouse Raw264 macrophage NHzkcoNHfW6ldHnvckBie3OjeR?= M2XE[WlvcGmkaYTpc44hd2ZiQ{XhMY1m\GmjdHXkJHBMSi:Da4SgdIhwe3Cqb4L5cIF1cW:wIHnuJI1wfXOnIGLhe|I3PCCvYXPyc5Bp[WenLDDJR|UxRTFyIN88UU4> Mke2NVY4QDl5NEK=
Sf9 cells NUTTNmNUTnWwY4Tpc44h[XO|YYm= MXfJcohq[mm2aX;uJI9nKEircz30ZYdo\WRiYn;2bY5mKFCLM1ug[ZhxemW|c3XkJIlvKFOoOTDj[YxteyxiSVO1NF0yOCEQvF2u NGP5SJkyODl7OEO1NS=>
human MDA-MB-468 cells NXW0[Yk{S3m2b4TvfIlkyqCjc4PhfS=> M2PWTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZpkhW1KEIHHzd4F6NCCLQ{WwQVExNjRizszNMi=> MVSxPFY6OTh7NB?=
human PC3 cell NUjJR5BuWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{PTTVczKGh? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHBEOyClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHOyZXP0do9xcG:2b33leJJq[yCjbnHsfZNqeyxiSVO1NF0yOi5zIN88UU4> M2[2T|I{PDFyMEC1
human HL60 cells NIXhdlVRem:uaX\ldoF1cW:wIHHzd4F6 NVziUlN1PzJiaB?= NIOzfJNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUiuOFMh|ryPLh?= NIezTHczPTZ7M{e4Oy=>
human BT474 cell NIPCUmNRem:uaX\ldoF1cW:wIHHzd4F6 MVG3NkBp NYfWN295UW6qaXLpeIlwdiCxZjDoeY1idiCEVES3OEBk\WyuIIDyc4xq\mW{YYTpc44h[W[2ZYKgO|IhcHK|IHL5JJNx\WO2cn;wbI91d22ndILpZ{BidmGueYPpd-+9lCCLQ{WwQVIxNjdizszNMi=> NWDYT451OjN2MUCwNFU>
THP1 cells MVPGeY5kfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKE2FUEGtbY5lfWOnZDDjbIVud3SjeHnzJI9nKFSKUEGgZ4VtdHNuIFnDOVA:OzdizszNMi=> M2jSWFE3Pzh7N{Sy
human 184B5 cells M33tc2N6fG:2b4jpZ:Kh[XO|YYm= MYDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjCxPFRDPSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:OzlwM{eg{txONg>? MWexPFY6OTh7NB?=
human KB cells Mn7DR5l1d3SxeHnjxsBie3OjeR?= NYX1fXJHPzJiaB?= M2DMZ2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NESuO|Yh|ryPLh?= NYS5Umc5OjF7NEWyOVA>
mouse RAW264.7 cells MWDGeY5kfGmxbjDhd5NigQ>? NG\2UlIzPSEQvF2= MVWyNEBp NVLz[YVWUW6qaXLpeIlwdiCxZjDQTVNMN0GNVDDpckBud3W|ZTDSRXczPjRwNzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKEySUz3pcoR2[2WmIHnOU3MheHKxdHXpckBmgHC{ZYPzbY9vKGG2IEK1JO69VSCjZoTldkAzOCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NHvtW5kzPDJ7OU[xOi=>
human A2780 cells NVjBZmVtSXCxcITvd4l{KGG|c3H5 NGfmdXozKM7:TR?= M13Tb|EzKGh? M3rmdGlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gZ4l{eGyjdHnuMZJme2m|dHHueEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDwbI9{eGixconsZZRm\CCDa4SgcIV3\WxiYYSgNkB2VSCjZoTldkAyOiCqcoOgZpkhcW2vdX7vZoxwfCCjbnHsfZNqey5? NGfuS|cyPzZ6NECxPC=>
human SW480 cells M1Ozb2Z2dmO2aX;uJIF{e2G7 NFXXcVEzOCEQvF2= M1rKV|I1KGh? M{P6SGRm[3KnYYPlJIlvKHO3co\peolvKGW6cILld5Nqd25iaX6gbJVu[W5iU2e0PFAh[2WubIOgZZQhOjBidV2gZYZ1\XJiMkSgbJJ{KGK7IHntcZVvd2Kub4SgZY5idHm|aYO= Mnf2NVc1PzJ7NkK=
mouse mast cells NHnwO2hHfW6ldHnvckBie3OjeR?= MYiyNEDPxE1? Mnf4TY5pcWKrdHnvckBw\iCVQ1[tbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCvYYP0JINmdGy|IHH0JFIxKM7:TR?= NV\OPXlEOTZ5OEm3OFI>
human BJ cells MYLGeY5kfGmxbjDhd5NigQ>? NHPTRYgzPSEQvF2= M3vKeVIhcA>? M13YZWlvcGmkaYTpc44hd2ZiUFmzT{B{cWewYXzpcochcW5iUFTHSk1{fGmvdXzheIVlKHOncoXtJJN1[XK4ZXSgbJVu[W5iQlqgZ4VtdHNidILhcpNn\WO2ZXSge4l1cCCybHHzcYllKEWJRmCvVGgh\G:vYXnuJI9nKEGtdDDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDQTE1GT0[SIILl[Il{fHKrYoX0bY9vKHSxIIDsZZNu[SCvZX3idoFv\SCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDjc45nd2OjbDDtbYNzd3Olb4D5 M1nt[lE3PzZ5MEi1
human IGROV1 cells MWnGeY5kfGmxbjDhd5NigQ>? NUDuS2ZYOjRxNEigbC=> MXnJcohq[mm2aX;uJI9nKFCLM1uvRYt1KGmwIHj1cYFvKEmJUl;WNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwenmuYYTl[EBCU1RibHX2[Ywh[XRiMTD0c{A2KHSrbXXzJGlEPTBiYX\0[ZIhOjRidH:gOFghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MVGyNVIyPjF3MR?=
human IGROV1 cells NH\5XoVHfW6ldHnvckBie3OjeR?= NVq1eox7OjRxNEigbC=> NXWwSYVWUW6qaXLpeIlwdiCxZjDQTVNMN0GtdDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ5lkdGmwIFSxJIxmfmWuIHH0JFEhfG9iNTD0bY1meyCLQ{WwJIFnfGW{IEK0JJRwKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= M2jW[VIyOjF4MUWx
rat RBL2H3 cells M2niW2Z2dmO2aX;uJIF{e2G7 MX3Jcohq[mm2aX;uJI9nKEF{M{G4O{1qdmS3Y3XkJIRm\3KjboXsZZRqd25iaX6gdoF1KFKETELIN{Bk\Wyucx?= MYqxPFMzQDdzNh?=
human BJ cells M4nr[WZ2dmO2aX;uJIF{e2G7 MV6yOUDPxE1? NXvTZpNHOiCq NXuwWFBCSWO2aY\heIlwdiCxZjDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFSqckOwPEBqdiCSRFfGMZN1cW23bHH0[YQhe2W{dX2gd5Rien[nZDDoeY1idiCESjDj[YxteyCjdDCyOUB2VSC2cnXheIVlKDJiaILzJIJm\m:{ZTDQSGdHKGOqYXzs[Y5o\SCkeTDpcY12dm:kbH;0eIlv\w>? MUKxOlc3PzB6NR?=
human HCT116 cells NWe0elRiTnWwY4Tpc44h[XO|YYm= M2K3cVExKM7:TR?= NUTpUY55OTBibXnu NWfmdlByUW6qaXLpeIlwdiCxZjDQTVNM[WyyaHGgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KHW|aX7nJHs{OlCfQWTQJIF1KDFyIIXNJIFnfGW{IEGwJI1qdnN? M{\6clIzOjF{N{Kx
human HCT116 cells MUTGeY5kfGmxbjDhd5NigQ>? NXG1ZVhtOTBizszN M4DEe|ExKG2rbh?= MnTGTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNidYPpcochYzN{UG3BWHAh[XRiMUCgeW0h[W[2ZYKgNVAhdWmwcx?= NWmyNXVNOjJ{MUK3NlE>
human HCT116 cells NIDL[ZZHfW6ldHnvckBie3OjeR?= M3npbVExKM7:TR?= MkfqTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRYt1KFOnckS3N{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? M4TSUlIzOjF{N{Kx
human HCT116 cells NGPVZpVHfW6ldHnvckBie3OjeR?= Mln5NVAh|ryP Mom3TY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MlHENlIzOTJ5MkG=
human PC3 cells NYPYPJhQTnWwY4Tpc44h[XO|YYm= NUHvfJBzPTBizszN MkDMPEBp NHXR[FdKdmS3Y4Tpc44hd2ZicEKxJJBzd3SnaX6g[ZhxemW|c3nvckBqdiCqdX3hckBRSzNiY3XscJMh[XRiNUCgeW0hcW6ldXLheIVlKG[xcjC4JIhzeyCkeTDX[ZN1\XKwIHLsc5R1cW6pIILlcIF1cX[nIITvJJVvfHKnYYTl[EBkd262cn;s MUOyNlk6QDR5Mh?=
human LNCAP cells NIr5ZYpHfW6ldHnvckBie3OjeR?= NW[3W4FrOC5zLUOwJO69VQ>? MmDjN|AhdWmw M1HuXGlvcGmkaYTpc44hd2ZiQXv0JJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiM{CgcYlveyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NIjHR48zOjh|MkOxOi=>
human LNCAP cells NFPT[nRHfW6ldHnvckBie3OjeR?= MlfUNE4yNTNyIN88US=> NIC1bFEzPCCq NH:0d2tFd3ewcnXneYxifGmxbjDv[kB{fXK4aY\pckBmgHC{ZYPzbY9vKGmwIHj1cYFvKEyQQ1HQJINmdGy|IHH0JFAvOSC2bzCzNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NFT3c3IzOjh|MkOxOi=>
HUVEC MlPUSpVv[3Srb36gZZN{[Xl? NGXMR4MyOC1{NTFOwG0> NF;GVYsyPiCq NV7XUJJwUW6qaXLpeIlwdiCxZjDUUmZidHCqYT3zeIlufWyjdHXkJGlESU1vMTDtVm5CKGW6cILld5Nqd25iaX6gTHVXTUNiYYSgNVAhfG9iMkWgeW0heHKndILlZZRm\CCob4KgNVYhcHK|IHLl[o9z\SCWTl\hcJBp[SClaHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPiCqcoOgZpkhWlRvUFPSJIFv[Wy7c3nz NGDEZmszOjB{NkSxNC=>
HUVEC NHfxW3VHfW6ldHnvckBie3OjeR?= MUWxNE0zPSEQvF2= M4rRelMxKG2rbh?= NH7XTYdKdmirYnn0bY9vKG:oIGTOSoFteGijLYP0bY12dGG2ZXSgbJVu[W5iSVPBUU0yKHC{b33veIVzKGGldHn2bZR6KGW6cILld5Nm\CCrbjDIWXZGSyCjc4Pld5Nm\CCjczDi[ZRiNWejbHHjeI9{cWSjc3WgZYN1cX[rdImgZZQhOTBidH:gNlUhfU1icILleJJm[XSnZDDmc5IhOzBibXnud{Bj\W[xcnWgWG5H[WyyaHGgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IEWgbJJ{KGK7IHz1Z4ln\XKjc3WgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> NVX2[WNCOjJyMk[0NVA>
human H1299 cells NYi1RVRyTnWwY4Tpc44h[XO|YYm= NWjyUplHOC5zLUOwJO69VQ>? NVvXZXpnOjRiaB?= NWLzZ2U{TG:5bjDy[Yd2dGG2aX;uJI9nKGOLQWCyJIV5eHKnc4Ppc44hcW5iaIXtZY4hUDF{OUmgZ4VtdHNiYYSgNE4yKHSxIEOwJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MX[yNlYzOjB4OR?=
human H1299 cells MXTGeY5kfGmxbjDhd5NigQ>? MlnSNE4yNTNyIN88US=> MkmxNlQhcA>? NEjhZYtFd3ewIILl[5Vt[XSrb36gc4Yh[0mDUEKg[ZhxemW|c3nvckBqdiCqdX3hckBJOTJ7OTDj[YxteyCjdDCwMlEhfG9iM{CgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kAyODBidXevcYwhXFKDSVygZY5lKFCLM1ugbY5pcWKrdH;yJGx[Ojl2MECy NWPl[m9COjJ4MkKwOlk>
human H1299 cells Mo\4SpVv[3Srb36gZZN{[Xl? MlrxNE4yNTNyIN88US=> NUDTTmtrOjRiaB?= MlLOTY5lfWO2aX;uJI9nKESUNTDlfJBz\XO|aX;uJIlvKGi3bXHuJGgyOjl7IHPlcIx{KGG2IECuNUB1dyB|MDD1UUBi\nSncjCyOEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NGTMbmgzOjZ{MkC2PS=>
human H1299 cells MnnRSpVv[3Srb36gZZN{[Xl? M3znUVAvOS1|MDFOwG0> M{[we|I1KGh? NUXze213UW6mdXP0bY9vKG:oIFrOT{1u\WSrYYTl[EBEUE:SIHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MnvGNlI3OjJyNkm=
HEK293 cells NGWzfmJHfW6ldHnvckBie3OjeR?= MV:xMlUhcA>? M3v3ZmRqe3CuYXPlcYVvfCCxZjDbN2heVFOGIH\yc40hcHWvYX6gOWhVPiC{ZXPldJRweiCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFEvPSCqcoOgZpkhdGmzdXnkJJNkcW62aXzsZZRqd25iY3;1cpRqdmd? NIHKZ4kzOjV|N{G1Ny=>
human U251HRE cells M{nMUGZ2dmO2aX;uJIF{e2G7 NVzGU2p{UW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKFV{NUHIVmUh[2WubIOgZpkh[2WubDDiZZNm\CC{ZYDvdpRmeiCpZX7lJIF{e2G7 MkT1NVg2ODF4MEG=
human HCT116 cells NWnqclV5TnWwY4Tpc44h[XO|YYm= MYmxNEDPxE1? MYnJcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz NF3wNo0zOjJzMkeyNS=>
Sf9 cells MmLa[ox2d3Knc3PlcpQheG:uYYLpfoF1cW:wIHHzd4F6 NHT2PJdKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= MVqyNVEzOTZ|MR?=
human HCT116 cells NFOxfZVRem:uaX\ldoF1cW:wIHHzd4F6 M1:1WlczKGh? MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13MT64NkDPxE1w MkjFNlU3QTN5OEe=
human HCT116 cells MknKR5l1d3SxeHnjxsBie3OjeR?= MXS3NkBp M2j2T2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVU3NjBzIN88UU4> NIjyWnozOTl2NUK1NC=>
human PC3 cells MknLR5l1d3SxeHnjxsBie3OjeR?= NEHwdG04OiCq M4TqUGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[xMlM2KM7:TT6= MXWyNlQ5ODh3MR?=
human HuH7 cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 MoPvO|IhcA>? MkfDRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZ5LkG4JO69VS5? NHe3S2szPTZ7M{e4Oy=>
human A549 cells MXnQdo9tcW[ncnH0bY9vKGG|c3H5 NV3Rfmk3PzJiaB?= NXrXd|k2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUiyMlMzKM7:TT6= NXnNZVF1OjV4OUO3PFc>
human A549 cells NED5N2ZEgXSxdH;4bYPDqGG|c3H5 Mne2O|IhcA>? M3;oOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfS=> MYiyNlQ5ODh3MR?=
human PC3 cells NInWTWhRem:uaX\ldoF1cW:wIHHzd4F6 NHrGVXQzPSEQvF2= NGDoc3kyOjBiaB?= MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjdDCyOUB2VSCjZoTldkAyOjBiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDEUXNQ NYfvVlI{OTZ4OECxOVk>
human H460 cells MUXGeY5kfGmxbjDhd5NigQ>? NV7aVmZtOzBizszN NEn1fnlKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hUDR4MDDj[YxteyCjc4Pld5Nm\CCjczDBb5QheGixc4Doc5J6dGG2aX;uJIF1KFOncjC0O|MhfXBidH:gN|AhfU1? NXrXW49rOTh3MEG2NFE>
human IGROV1 cells M2PFbGZ2dmO2aX;uJIF{e2G7 MmXYNlQhcA>? MY\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDJS3JQXjFiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEdzIIDoZZNmKGG2IEGg[o9t\CCLQ{WwJIFnfGW{IEK0JIhzeyCkeTDmcI94KGO7dH;t[ZRzgQ>? NETuVmIzOTJzNkG1NS=>
human IGROV1 cells M{j0fmZ2dmO2aX;uJIF{e2G7 NYm2fJlqOjRiaB?= NHz4OmdE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBKT1KRVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexJJBp[XOnIHH0JFUh\m:uZDDJR|UxKGGodHXyJFI1KGi{czDifUBndG:5IHP5eI9u\XS{eR?= NEnjT|AzOTJzNkG1NS=>
human H4 cells Mmq3SpVv[3Srb36gZZN{[Xl? M1S3SFIhcA>? NIn3[4lF\WO{ZXHz[UBqdiCIWW\FMXJHWCtidnXzbYNt\SCrboTlcpNqfHlicHXyJINmdGxiaX6gbJVu[W5iSESgZ4VtdHNiYX\0[ZIhOiCqcoOgdoVt[XSrdnWgeI8h[2:wdILvcC=> Mnu3NVgxOjR3OES=
human MGC803 cells M3zvSGZ2dmO2aX;uJIF{e2G7 NYC1PYtsOjVizszN NWnBfmxiPDhiaB?= NIixdlNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOT0N6MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZZQhOjVidV2gZYZ1\XJiNEigbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZYZ1\XJiNEigbJJ{KGK7IH\sc5ch[3m2b33leIVzKHKnbHH0bZZmKHSxIHPvcpRzd2x? M3vrdlI1OTF7OE[5

... 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
  • 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
Smiles O=C1C=C(OC2=C(C=CC=C12)C3=CC=CC=C3)N4CCOCC4

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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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*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:

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID