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 in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

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Cited by 72 Publications

14 Customer Reviews

  • Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).

    Hepatology 2014 59(4), 1262-72. LY294002 purchased from Selleck.

    different signal-inhibitory profile by applying 120 nmol/L BGT226, 20 μmol/L LY294002, or 100 nmol/L rapamycin in FaDu cells.

    Clin Cancer Res 2011 17, 7116-7126. LY294002 purchased from Selleck.

  • Stimulation response of p37d-expressing cells. (c) Western blot of 5 min serum stimulated HEK-293 cells stably expressing p37d, p110d or control, with the presence of inhibitors as indicated at the top.

    Oncogene 2012 31, 3277–3286. LY294002 purchased from Selleck.

    PTEN transfection or inhibition of the PI3K-AKT and IGF-1R signaling pathways increases the trastuzumab sensitivity of NCI-N87/TR cells. After treating the cells with a PI3K inhibitor (LY294002), the expression of AKT and P-AKT proteins was assessed by Western blotting. Tubulin expression indicated equal loading. All gels run under the same experimental conditions and the experiments were repeated 3 times. The representative images were cropped and shown. Control: cells without any treatment.

    Sci Rep 2015 5, 11634. LY294002 purchased from Selleck.

  • SCC61 or Detroit 562 xenografted tumors respond to treatment by PI3K inhibitor, LY294002 alone, or in combination with gefitinib. % tumor growth is shown. By two-way ANOVA, the effect of treatment and time is considered significant;

    Mol Oncol 2013 7, 359-68. LY294002 purchased from Selleck.

    Inhibition of EGFR and PI3K/AKT pathway has additive effects in SCCHN cell lines with constitutively active PIK3CA mutations, while removing negative regulation of PI3K/AKT pathway increases resistance in sensitive SCCHN cell line. A, results from MTT assays on cells treated with PI3K inhibitor, LY294002, and gefitinib.

    Mol Oncol 2013 7, 359-68. LY294002 purchased from Selleck.

  • Lyn-PI3K-BTK signaling is required for the inhibitory effect of anti-CD180 on the activation of IFN-α signaling. (a and b) Isolated murine splenic B220+ B cells were pretreated with dasatinib (5 μM), a Lyn inhibitor; LY294002 (5 μM), a PI3K inhibitor; ibturinib (1 μM), a BTK inhibitor; enzastaurin (1 μM), a PKC β inhibitor; U0126 (3 μM), an ERK inhibitor; SP600126 (2 μM), a JNK inhibitor or SB20358 (1 μM), a p38 inhibitor for 1 h, followed by stimulation with anti-CD180 antibody (0.2 μg/mL) or mouse IFN-α (1000 U/mL) for 4 h. qPCR analysis of the expression of IFIT1 (a) and MX1 (b). (c) Isolated murine splenic B220+ B cells were pretreated with dasatinib (5 μM), LY294002 (5 μM), and ibturinib (1 μM) for 1 h, followed by stimulation with anti-CD180 antibody (0.2 μg mL−1) or mouse IFN-α (1000 U mL−1) for 40 min. Western blot analysis of the phosphorylation level of STAT-2. The data shown represent the mean values of three independent experiments, and the error bars represent the SEM. *p < 0.05, **p < 0.01, ***p < 0.001, as determined by ANOVA; ns denotes p > 0.05.

    Cell Mol Immunol, 2017, 14(2):192-202. LY294002 purchased from Selleck.

    Immunofluorescence and flow cytometric analyses of the translocation of ABCG2 in MCF-7 FLV1000 cells before and after treatment with the PI3K inhibitor LY294002. Confocal microscopy of MCF-7 FLV1000 cells after a 16-h treatment with 2 uM or 4 uM of LY294002 was performed as described in Figure.

    Br J Pharmacol 2013 70(5), 1137-51. LY294002 purchased from Selleck.

  • IGF1 increases apical fibronectin in late stage blastocysts. Representative confocal images of blastocysts stained for fibronectin (Green) and DAPI (Blue). Day 5 blastocysts were cultured in SS medium for 24 (A and B), 48 (C and D) or 72 h (E-H) in the absence (A, C and E) or presence (B, D and F) of 10 ng/ml IGF1 or in the presence of a PI3 Kinase inhibitor (5 uM LY294002 + 10 ng/ml IGF1) (G) or in the presence of 10 ng/ml IGF1, attached to a coverslip (H). Scale bars represent 20 mm. Red line indicates location of coverslip. Arrow indicates location of the inner cell mass (ICM). The following total number of blastocysts were analysed, from at least 3 experimental repeats in each treatment; 24 in the SS group (24 h), 21 in SS plus IGF1 (24 h), 26 in SS (48 h), 30 in SS plus IGF1 (48 h), 40 in SS (72 h), 59 in SS plus IGF1 (72 h), 13 in SS plus IGF1 + LY294002 (48 h) and 15 blastocysts were analysed that were attached to a coverslip (72 h).

    Hum Reprod 2015 30(2), 284-98. LY294002 purchased from Selleck.

    Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.

    Int J Biochem Cell Biol 2015 60, 34-42. LY294002 purchased from Selleck.

  • Comparative effects of inhibitors by immunofluorescence microscopy study. Confluent HC11 cells were grown on poly-L-lysine-coated glass coverslips (immunofluorescence) and on plastic plates (biochemical control) and then treated with inhibitors according to the standard procedure. Upper part: the biochemical action of the inhibitors was tested to validate the immunofluorescence results. Cellular proteins were analyzed by SDS-PAGE and the immunoblots were successively probed with anti-ADRP, anti-β-casein, and anti- β-actin antibodies and their respective HRP-conjugated secondary antibodies. Each experimental condition was performed in duplicate. Lower part: cells were fixed, permeabilized and subjected to immunofluorescence microscopy using antiserum against ADRP and TRITC-conjugated secondary antibody (red).

    Biochim Biophys Acta 2012 1823(5), 987-96. LY294002 purchased from Selleck.

    Comparative effects of wortmannin and LY294002 on ADRP and β -casein synthesis. Con fluent HC11 cells were treated according to the standard procedure in the absence or presence of 4 ng/ml EGF either with or without 100 nM wortmannin or 50μM LY294002. Cellular proteins were analyzed by SDS-PAGE and immunoblot successively probed with anti-ADRP, anti-β-casein, anti-β -actin antibodies and their respective HRP-conjugated secondary antibodies. ECL signals were quantified by densitometry and normalized to β-actin. Each experimental condition was performed in triplicate. Percentages of inhibition for both inhibitor and hormonal treatments are indicated in the text.

    Biochim Biophys Acta 2012 1823(5), 987-96. LY294002 purchased from Selleck.

  • We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.

     

     

    2010 Saraswati Sukumar of Johns Hopkins University School of Medicine. LY294002 purchased from Selleck.

    T47Dcells were pretreated with 100 ng/ml EGF for 20 min and then treated with the indicated concentrations of LY294002 for 24 hours.

     

     

    2010 Dr. Zhang of Tianjin Medical University. LY294002 purchased from Selleck.

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 in cell-free assays, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
Targets
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
0.5 μM 0.57 μM 0.97 μM
In vitro

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 M{Th[2NmdGxiaX72ZZNqd25iYYPzZZk> NIfBeJMzPCCq NGnLXJVKdmirYnn0bY9vKG:oIHXwbZRp\WyrYXyg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGOnbHygcYloemG2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgdJJmNWmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JINmdGxiaX72ZZNqd25iYYPzZZktKEmFNUC9NE4{QCEQvF2u NF;IZ5MzOjhyNEGwPC=>
Sf21 cells NYjweYlJTnWwY4Tpc44h[XO|YYm= NEDVbJBKdmirYnn0bY9vKG:oIH3veZNmKHerbHSgeJlx\SCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnOjFiY3XscJMh[29vZYjwdoV{e2mwZzDOMZRmem2rbnHsJGhqey22YXfn[YQhcHWvYX6gdFg2[SC3c3nu[{BNNWGucHjhMZBpd3OyaHH0bYR6dGmwb4PpeI9tKHO3YoP0doF1\SCkeTDUUGMh[mG|ZXSgdIhwe3Cqb4KgbY1i\2mwZzygTWM2OD1yLkWg{txO MWqyNlUzODZ|MB?=
Sf21 cells MnnwSpVv[3Srb36gZZN{[Xl? M1T5OGlvcGmkaYTpc44hd2ZibX;1d4UhemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkKxJINmdGy|LDDJR|UxRTBwNTFOwG0v MojGNVk4PDh{Nkm=
Sf9 cells NXjwUoRYTmy3b4Lld4NmdnRicH;sZZJqgmG2aX;uJIF{e2G7 NV7zW5RiUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTB;MD61OUDPxE1w NGXndFYzOTF{MU[zNS=>
THP1 cells NF;PdY9HfW6ldHnvckBie3OjeR?= NWrGOpY5UW6qaXLpeIlwdiCxZjDTR2YyNWmwZIXj[YQhWEuEL1HreEBxcG:|cHjvdplt[XSrb36gbY4hXEiSMTDj[YxteyxiSVO1NF0yNjBzIN88UU4> NHfzPHUyPjd6OUe0Ni=>
human PC3 cells NVnjenZQTnWwY4Tpc44h[XO|YYm= MoTyN|AhdWmw MYnJcohq[mm2aX;uJI9nKFCLM1ugbY4hcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhe2W{aX7lJFQ4OyCjZoTldkA{OCCvaX7zJIJ6KEWOSWPBMEBKSzVyPUGuN:69VS5? MVOyN|QyODByNR?=
HeLa (human carcinoma) cells. NXzncHZXTnWwY4Tpc44h[XO|YYm= Ml;XTY4hfmm2cn:gbY5pcWKrdHnvckBw\iCGTlGt[IVx\W6mZX70JJBzd3SnaX6gb4lv[XOnKFTORU1RUyliZoLvcUBJ\UyjIDjoeY1idiClYYLjbY5wdWFrIHPlcIx{NCCLQ{WwQVEvPCEQvF2u NFH5cIYyPTZ3OEi3NC=>
THP1 cells MXXGeY5kfGmxbjDhd5NigQ>? MXrJcohq[mm2aX;uJI9nKE2FUEGtbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDUTHAyKGOnbHzzMEBKSzVyPUGuOlUh|ryPLh?= M1KxPFE3Pzh7N{Sy
HeLa cells NVLVNWhqTnWwY4Tpc44h[XO|YYm= NHriVXdKdmirYnn0bY9vKG:oIH3UU3IheHKxdHXpckBqe2:uYYTl[EBnem:vIFjlUIEh[2WubIOsJGlEPTB;Mj61JO69VS5? MoPCNVU3PTh6N{C=
human MCF7 cells M4LTXWN6fG:2b4jpZ:Kh[XO|YYm= MlrXR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVIvPjNizszNMi=> MWixPFY6OTh7NB?=
HeLa cells MnzPSpVv[3Srb36gZZN{[Xl? NVHiRpl6UW6qaXLpeIlwdiCxZjDBXE04PTB|IHLpcoRqdmdidH:gdoVkd22kaX7hcpQhWGytMzDlfJBz\XO|ZXSgbY4hUGWOYTDj[YxteyCkeTDX[ZN1\XKwIHLsc5QtKEmFNU2zJO69VS5? MnHLNVcyOzV{NEi=
human MCF7 cells MVfDfZRwfG:6aXRCpIF{e2G7 NGm3VmJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExKHWPIHPocI9zd3G3aX7lJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjB6IN88UU4> MmDxNVg3QTF6OUS=
human MCF7 cells NIrOUVlEgXSxdH;4bYPDqGG|c3H5 NFHQR3lEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGK7IGPSRkBie3OjeTygS2k:Oy5zNjFOwG0v NUH4XG9tOTh4OUG4PVQ>
human MDA-MB-231 cells M3fHbGN6fG:2b4jpZ:Kh[XO|YYm= NIHGO5NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEKwJO69VSClaHzvdo9yfWmwZTDifUBUWkJiYYPzZZktKEeLPUOuN|Ih|ryPLh?= NVKy[lJJOTh4OUG4PVQ>
human MDA-MB-231 cells Ml;ER5l1d3SxeHnjxsBie3OjeR?= M1fXPGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMUCgeW0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H5MEBIUTVyPUSuN|Uh|ryPLh?= NUnR[4VtOTh4OUG4PVQ>
human MDA-MB-468 cells MnnHR5l1d3SxeHnjxsBie3OjeR?= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3Ojef-8kEBKSzVyPUSuO|Yh|ryPLh?= MoDTNVg3QTF6OUS=
human HCT116 cells NFjSTphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV60PEBp NV7wSpFOT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKFCLM1vhcJBp[SCKMUC0O3IhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NT6zJO69VQ>? MXGyNlIyOjd{MR?=
human HCT116 cells NEK1W4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml7KOFghcA>? NUL4R41CT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IN88UU4> NYHNNmVUOjJ{MUK3NlE>
HeLa cells M3;ZV2JqdmSrbnegZYZncW6rdImgZZN{[Xl? MUnCbY5lcW6pIHHm[olvcXS7IH\vdkBRUTNva3nuZZNmKGm|b3zheIVlKG[{b32gTIVN[SClZXzsd{whU2l;NjFOwG0> NH;1d|kyPTZ3OEi3NC=>
human HCT116 cells NYL4[41lT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXCeYQyPDhiaB?= MXTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMhd3[ncnX4dJJme3OrbnegVGk{U2GucHjhJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63JO69VS5? NFvDVnQzOjJzMkeyNS=>
MDA-MB-231 cells NYfLNo1HS3m2b4TvfIlkyqCjc4PhfS=> NV;5RW0zS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi55MTFOwG0v M3u0blE5PjlzOEm0
Sf9 cells MoXMSpVv[3Srb36gZZN{[Xl? NUDUW4dPUW6qaXLpeIlwdiCxZjDDT|Ih\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD14Lkmg{txONg>? M4fW[|E5OzJzN{G2
human U87MG cells NIf5dZhHfW6ldHnvckBie3OjeR?= MUjJcohq[mm2aX;uJI9nKEeVS{OtZoV1[SCrbjDoeY1idiCXOEfNS{Bk\WyuczDifUBGVEmVQTygTWM2OD16LkGg{txONg>? MYOxPFM1PTZyOR?=
human MDA-MB-468 cells MoH2R5l1d3SxeHnjxsBie3OjeR?= MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDFyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3OjeTygS2k2OD16LkKg{txONg>? NIT0NWYyQDZ7MUi5OC=>
human A375 cells M4LsUXBzd2yrZnXyZZRqd25iYYPzZZk> MWW0OkBp NYHnTHJsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IES2JIhzeyxiSVO1NF05NjRizszNMi=> MkHaNVcxPDl{NEi=
human A375 cells MnryVJJwdGmoZYLheIlwdiCjc4PhfS=> NFf4VHRKdmirYnn0bY9vKG:oIIPldpVuNWmwZIXj[YQheHKxbHnm[ZJifGmxbjDv[kBpfW2jbjDBN|c2KGOnbHzzMEBKSzVyPUiuOEDPxE1w NHGwZ3YyPzZyMUezPS=>
human HL60 cells M4W5OWN6fG:2b4jpZ:Kh[XO|YYm= NXrCbpVYPzJiaB?= MoraR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGw3OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUmuPVQh|ryPLh?= MXWyNlQ5ODh3MR?=
mouse Raw264 macrophage MlTOSpVv[3Srb36gZZN{[Xl? NIHvXZhKdmirYnn0bY9vKG:oIFO1ZU1u\WSrYYTl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDSZZczPjRibXHjdo9xcGGpZTygTWM2OD1zMDFOwG0v Mof2NVY4QDl5NEK=
Sf9 cells Mof3SpVv[3Srb36gZZN{[Xl? Mk\lTY5pcWKrdHnvckBw\iCKaYOteIFo\2WmIHLveolv\SCSSUPLJIV5eHKnc4Pl[EBqdiCVZkmgZ4VtdHNuIFnDOVA:OTBizszNMi=> M{C3dlExQTl6M{Wx
human MDA-MB-468 cells MV\DfZRwfG:6aXRCpIF{e2G7 NXrkN49MS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVQ3QCClZXzsd{BjgSCVUlKgZZN{[XluIFnDOVA:OTBwNDFOwG0v NXHBWVRNOTh4OUG4PVQ>
human PC3 cell MnKzVJJwdGmoZYLheIlwdiCjc4PhfS=> MkLFO|IhcA>? M13XSmlvcGmkaYTpc44hd2ZiaIXtZY4hWEN|IHPlcIwheHKxbHnm[ZJifGmxbjDh[pRmeiB5MjDodpMh[nlic4DlZ5Rzd3Cqb4TvcYV1emmlIHHuZYx6e2m|LDDJR|UxRTF{LkGg{txONg>? MmjtNlM1OTByMEW=
human HL60 cells MYTQdo9tcW[ncnH0bY9vKGG|c3H5 MX[3NkBp MmDuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTF6LkSzJO69VS5? M2K2fVI2Pjl|N{i3
human BT474 cell NXnJWm1PWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUjMN|NJPzJiaB?= M1LDUWlvcGmkaYTpc44hd2ZiaIXtZY4hSlR2N{SgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYRvwKwhUUN3ME2yNE44KM7:TT6= M4qx[lI{PDFyMEC1
THP1 cells MYfGeY5kfGmxbjDhd5NigQ>? MljBTY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgZ4hmdW:2YYjpd{Bw\iCWSGCxJINmdGy|LDDJR|UxRTN5IN88UU4> NVzJNmlGOTZ5OEm3OFI>
human 184B5 cells MnzmR5l1d3SxeHnjxsBie3OjeR?= NH3NeI1EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyQDSENTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{muN|ch|ryPLh?= MoXZNVg3QTF6OUS=
human KB cells NEm1OGFEgXSxdH;4bYPDqGG|c3H5 MlPkO|IhcA>? M1r0WmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NESuO|Yh|ryPLh?= NWDke2hVOjF7NEWyOVA>
mouse RAW264.7 cells NHXsZ4NHfW6ldHnvckBie3OjeR?= M1P5RlI2KM7:TR?= NEjyWGEzOCCq M4CzdGlvcGmkaYTpc44hd2ZiUFmzT{9CU1RiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBNWFNvaX7keYNm\CCrTl;TJJBzd3SnaX6g[ZhxemW|c3nvckBifCB{NTFOwG0h[W[2ZYKgNlAhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MV[yOFI6QTZzNh?=
human A2780 cells NXv4VWtHSXCxcITvd4l{KGG|c3H5 MV6yJO69VQ>? NG[5XJUyOiCq MUjJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHPpd5Bt[XSrbj3y[ZNqe3SjboSgbJVu[W5iQUK3PFAh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icHjvd5Bpd3K7bHH0[YQhSWu2IHzleoVtKGG2IEKgeW0h[W[2ZYKgNVIhcHK|IHL5JIludXWwb3Lsc5Qh[W6jbInzbZMv M2\vUFE4Pjh2MEG4
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human H1299 cells NXSzeWNKTnWwY4Tpc44h[XO|YYm= MnHZNE4yNTNyIN88US=> MlfPNlQhcA>? MX;Ec5dvKHKnZ4XsZZRqd25ib3[gZ2lCWDJiZYjwdoV{e2mxbjDpckBpfW2jbjDINVI6QSClZXzsd{BifCByLkGgeI8hOzBidV2gZYZ1\XJiMkSgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpd{BqdiCycnXz[Y5k\SCxZjCxNFAhfWdxbXygWHJCUUxiYX7kJHBKO0tiaX7obYJqfG:{IFzZNlk1ODB{ NUDRVlFKOjJ4MkKwOlk>
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human H1299 cells NXzHNmtjTnWwY4Tpc44h[XO|YYm= MXSwMlEuOzBizszN M3H6dFI1KGh? MX\JcoR2[3Srb36gc4YhUk6NLX3l[IlifGWmIFPIU3Ah\XiycnXzd4lwdiCrbjDoeY1idiCKMUK5PUBk\WyuczDheEAxNjFidH:gN|AhfU1iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= M3G5eVIzPjJ{ME[5
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human HCT116 cells NHS4dVNHfW6ldHnvckBie3OjeR?= MkjxNVAh|ryP NULze5BsUW6qaXLpeIlwdiCxZjDBb5Qh\XiycnXzd4lwdiCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? Mn3aNlIzOTJ5MkG=
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human HCT116 cells NV[0bIU1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MYq3NkBp M2\MNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gZYJ{d3KkYX7j[UBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUWxMlgzKM7:TT6= MUKyOVY6Ozd6Nx?=
human HCT116 cells M{job2N6fG:2b4jpZ:Kh[XO|YYm= MnvwO|IhcA>? NVPiSppKS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PTZwMEGg{txONg>? NEXadWgzOTl2NUK1NC=>
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human HuH7 cells NFPsXXVRem:uaX\ldoF1cW:wIHHzd4F6 NIrxOGs4OiCq NHnxR41CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFj1TFch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NkeuNVgh|ryPLh?= MXGyOVY6Ozd6Nx?=
human A549 cells M1G3dHBzd2yrZnXyZZRqd25iYYPzZZk> NIX6e2g4OiCq MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:QDJwM{Kg{txONg>? MW[yOVY6Ozd6Nx?=
human A549 cells MWHDfZRwfG:6aXRCpIF{e2G7 Mn33O|IhcA>? MnT2R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 MnO1NlI1QDB6NUG=
human PC3 cells NUTjcIFkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NY\Td2dCOjVizszN Mmn6NVIxKGh? M3TSWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHH0JFI2KHWPIHHmeIVzKDF{MDDodpMh[nliTWTUJIF{e2G7IILlcIF1cX[nIITvJGROW09? M3;3XlE3PjhyMUW5
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human IGROV1 cells MYfGeY5kfGmxbjDhd5NigQ>? MVGyOEBp NVvmb25lS2WubDDjfYNt\SCjcoLld5QhcW5iaIXtZY4hUUeUT2[xJINmdGy|IHHzd4V{e2WmIHHzJIFk[3WvdXzheIlwdiCjdDDHNUBxcGG|ZTDheEA2KG[xbHSgTWM2OCCjZoTldkAzPCCqcoOgZpkh\myxdzDjfZRwdWW2com= MkXRNlEzOTZzNUG=
human H4 cells MYTGeY5kfGmxbjDhd5NigQ>? NXLVUZFCOiCq M2q4R2Rm[3KnYYPlJIlvKE[\VlWtVmZRMyC4ZYPpZ4xmKGmwdHXud4l1gSCyZYKgZ4VtdCCrbjDoeY1idiCKNDDj[YxteyCjZoTldkAzKGi{czDy[YxifGm4ZTD0c{Bkd262cn;s MXSxPFAzPDV6NB?=
human MGC803 cells MULGeY5kfGmxbjDhd5NigQ>? MnjNNlUh|ryP Mli2OFghcA>? MY\D[YxtKGO7Y3zlJIFzemW|dDDpckBpfW2jbjDNS2M5ODNiY3XscJMh[XO|ZYPz[YQh[XNiYXPjeY12dGG2aX;uJIF1KEd{L12gdIhie2ViYYSgNlUhfU1iYX\0[ZIhPDhiaILzJJV{cW6pIIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdiYX\0[ZIhPDhiaILzJIJ6KG[ub4egZ5l1d22ndHXyJJJmdGG2aY\lJJRwKGOxboTyc4w> M{LkUFI1OTF7OE[5

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:[4]
+ Expand

kinase assays:

PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.
Cell Research:[2]
+ Expand
  • Cell lines: Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
  • Concentrations: 0–50 μM
  • Incubation Time: 0–48 hours
  • Method: 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
  • Formulation: Dissolved in DMSO plus 0.25 ml of PBS
  • Dosages: 0–100 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (117.13 mM)
Ethanol 21 mg/mL (68.32 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
Synonyms SF 1101, NSC 697286

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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

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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