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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Cited by 73 Publications

15 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.

    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.

  • 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.

    The effects of GLP-1R siRNA and LY294002 on neurological score at 24 hours after subarachnoid hemorrhage (SAH) in Ex-4 treated rats.

    Neuropharmacology, 2018, 128:142-151. 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.

  • 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.

    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.

  • 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.

    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, 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)
DNA-PK [6]
(Cell-free assay)
0.5 μM 0.57 μM 0.97 μM 1.4 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 NYr1VIt1S2WubDDpcpZie2mxbjDhd5NigQ>? NIXrXHEzPCCq Mkm1TY5pcWKrdHnvckBw\iCncHn0bIVtcWGuIHfyc5d1cCCoYXP0c5IucW6mdXPl[EBk\WyuIH3p[5JifGmxbjDv[kBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IIDy[U1qdmO3YnH0[YQh\m:{IEK0JIhzeyCkeTDj[YxtKGmwdnHzbY9vKGG|c3H5MEBKSzVyPUCuN|gh|ryPLh?= NFjMNY8zOjhyNEGwPC=>
Sf21 cells NVnRSmgyTnWwY4Tpc44h[XO|YYm= NFnWOJRKdmirYnn0bY9vKG:oIH3veZNmKHerbHSgeJlx\SCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnOjFiY3XscJMh[29vZYjwdoV{e2mwZzDOMZRmem2rbnHsJGhqey22YXfn[YQhcHWvYX6gdFg2[SC3c3nu[{BNNWGucHjhMZBpd3OyaHH0bYR6dGmwb4PpeI9tKHO3YoP0doF1\SCkeTDUUGMh[mG|ZXSgdIhwe3Cqb4KgbY1i\2mwZzygTWM2OD1yLkWg{txO NEKzUXIzOjV{ME[zNC=>
Sf21 cells MWjGeY5kfGmxbjDhd5NigQ>? MoXETY5pcWKrdHnvckBw\iCvb4Xz[UBz\WOxbXLpcoFvfCCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{NWmwZnXjeIVlKFOoMkGgZ4VtdHNuIFnDOVA:OC53IN88UU4> MlPtNVk4PDh{Nkm=
Sf9 cells MnLUSox2d3Knc3PlcpQheG:uYYLpfoF1cW:wIHHzd4F6 NXLxeJJjUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTB;MD61OUDPxE1w MWOyNVEzOTZ|MR?=
THP1 cells M3Tj[GZ2dmO2aX;uJIF{e2G7 NHjJT45KdmirYnn0bY9vKG:oIGPDSlEucW6mdXPl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBVUFBzIHPlcIx{NCCLQ{WwQVEvODFizszNMi=> MWmxOlc5QTd2Mh?=
human PC3 cells MknESpVv[3Srb36gZZN{[Xl? NFvKU|g{OCCvaX6= NGrnWGJKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGFMXCCyaH;zdIhwenmuYYTpc44h[XRic3XybY5mKDR5MzDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVEvO87:TT6= NVj1cFI4OjN2MUCwNFU>
HeLa (human carcinoma) cells. MoXQSpVv[3Srb36gZZN{[Xl? MkLVTY4hfmm2cn:gbY5pcWKrdHnvckBw\iCGTlGt[IVx\W6mZX70JJBzd3SnaX6gb4lv[XOnKFTORU1RUyliZoLvcUBJ\UyjIDjoeY1idiClYYLjbY5wdWFrIHPlcIx{NCCLQ{WwQVEvPCEQvF2u NXHtUpFpOTV4NUi4O|A>
THP1 cells MonQSpVv[3Srb36gZZN{[Xl? MVzJcohq[mm2aX;uJI9nKE2FUEGtbY5lfWOnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDUTHAyKGOnbHzzMEBKSzVyPUGuOlUh|ryPLh?= NHq2b|IyPjd6OUe0Ni=>
HeLa cells NULmSo04TnWwY4Tpc44h[XO|YYm= M4e1fmlvcGmkaYTpc44hd2ZibWTPVkBxem:2ZXnuJIl{d2yjdHXkJIZzd21iSHXMZUBk\WyuczygTWM2OD1{LkWg{txONg>? MnLjNVU3PTh6N{C=
human MCF7 cells M37ZXGN6fG:2b4jpZ:Kh[XO|YYm= MnXPR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSUWwQVIvPjNizszNMi=> MoDiNVg3QTF6OUS=
HeLa cells NI\MbFNHfW6ldHnvckBie3OjeR?= MlziTY5pcWKrdHnvckBw\iCDWD23OVA{KGKrbnTpcochfG9icnXjc41jcW6jboSgVIxsOyCneIDy[ZN{\WRiaX6gTIVN[SClZXzsd{BjgSCZZYP0[ZJvKGKub4SsJGlEPT1|IN88UU4> M1y4XVE4OTN3MkS4
human MCF7 cells Mnq4R5l1d3SxeHnjxsBie3OjeR?= NHGyPZBEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGmwIIDy[ZNmdmOnIH;mJFExKHWPIHPocI9zd3G3aX7lJIJ6KFOUQjDhd5NigSxiR1m1NF0{NjB6IN88UU4> M3r3SlE5PjlzOEm0
human MCF7 cells M2H2RmN6fG:2b4jpZ:Kh[XO|YYm= MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIJ6KFOUQjDhd5NigSxiR1m9N{4yPiEQvF2u NEfwdJEyQDZ7MUi5OC=>
human MDA-MB-231 cells NH3hb2lEgXSxdH;4bYPDqGG|c3H5 M1Xrb2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMkCg{txOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l;Mz6zNkDPxE1w M3HLdlE5PjlzOEm0
human MDA-MB-231 cells M2PRfGN6fG:2b4jpZ:Kh[XO|YYm= Mn7SR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDpckBxemW|ZX7j[UBw\iBzMDD1UUBkcGyxcn;xeYlv\SCkeTDTVmIh[XO|YYmsJGdKPTB;ND6zOUDPxE1w NGewSWIyQDZ7MUi5OC=>
human MDA-MB-468 cells NYPhZ5JRS3m2b4TvfIlkyqCjc4PhfS=> MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3Ojef-8kEBKSzVyPUSuO|Yh|ryPLh?= M3m0[|E5PjlzOEm0
human HCT116 cells M33zfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfDbVhXPDhiaB?= MnjBS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTGNVOTF4IHPlcIx{KG:4ZYLlfJBz\XO|aX7nJHBKO0ujbIDoZUBJOTB2N2KgcZV1[W62IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PS5|IN88US=> NIjlfoUzOjJzMkeyNS=>
human HCT116 cells NGfqZ2RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37DUFQ5KGh? M3TUWmdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2u NIfUPXUzOjJzMkeyNS=>
HeLa cells NV\EPVE5SmmwZHnu[{Bi\m[rbnn0fUBie3OjeR?= M3vXOWJqdmSrbnegZYZncW6rdImg[o9zKFCLMz3rbY5ie2ViaYPvcIF1\WRiZoLvcUBJ\UyjIHPlcIx{NCCNaU22JO69VQ>? M4\DNFE2PjV6OEew
human HCT116 cells NYTGdHhoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEjDWIo1QCCq NGXHd2RIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBJS1RzMU[gZ4VtdHNib4\ldoV5eHKnc4PpcochWEl|S3HsdIhiKGGodHXyJFQ5KGi{czDifUBOXFRiYYPzZZktKEmFNUC9Ok44KM7:TT6= M1Xx[VIzOjF{N{Kx
MDA-MB-231 cells Mm\5R5l1d3SxeHnjxsBie3OjeR?= NX2xWolMS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCVUlKgZZN{[XluIFfJOVA:Pi55MTFOwG0v M3y4PVE5PjlzOEm0
Sf9 cells M4HveGZ2dmO2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKEONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVYvQSEQvF2u M3nudFE5OzJzN{G2
human U87MG cells NWDwcZE{TnWwY4Tpc44h[XO|YYm= Mk\HTY5pcWKrdHnvckBw\iCJU1uzMYJmfGFiaX6gbJVu[W5iVUi3UWch[2WubIOgZpkhTUyLU1GsJGlEPTB;OD6xJO69VS5? MnztNVg{PDV4MEm=
human MDA-MB-468 cells NVTY[XFtS3m2b4TvfIlkyqCjc4PhfS=> NIDWOlNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME24MlIh|ryPLh?= MmruNVg3QTF6OUS=
human A375 cells NYToZVViWHKxbHnm[ZJifGmxbjDhd5NigQ>? MXK0OkBp M3n5XWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB2NjDodpMtKEmFNUC9PE41KM7:TT6= MlXXNVcxPDl{NEi=
human A375 cells M2\reXBzd2yrZnXyZZRqd25iYYPzZZk> MnPGTY5pcWKrdHnvckBw\iC|ZYL1cU1qdmS3Y3XkJJBzd2yrZnXyZZRqd25ib3[gbJVu[W5iQUO3OUBk\WyuczygTWM2OD16LkSg{txONg>? MVKxO|YxOTd|OR?=
human HL60 cells M2\icGN6fG:2b4jpZ:Kh[XO|YYm= NHzTU3I4OiCq NXOxcWRCS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvQTRizszNMi=> MYeyNlQ5ODh3MR?=
mouse Raw264 macrophage NWW1cnJNTnWwY4Tpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKEN3YT3t[YRq[XSnZDDQT2IwSWu2IIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCUYYeyOlQhdWGlcn;wbIFo\SxiSVO1NF0yOCEQvF2u NEfhZWsyPjd6OUe0Ni=>
Sf9 cells MnuySpVv[3Srb36gZZN{[Xl? NFrFTmdKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgZo93cW6nIGDJN2sh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD1zMDFOwG0v NGDRbJkyODl7OEO1NS=>
human MDA-MB-468 cells NICwZ3ZEgXSxdH;4bYPDqGG|c3H5 NFfwOndEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtOFY5KGOnbHzzJIJ6KFOUQjDhd5NigSxiSVO1NF0yOC52IN88UU4> NH;LUVAyQDZ7MUi5OC=>
human PC3 cell NH7YTHFRem:uaX\ldoF1cW:wIHHzd4F6 NF7afY04OiCq NUHBdoZvUW6qaXLpeIlwdiCxZjDoeY1idiCSQ{OgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYOsJGlEPTB;MUKuNUDPxE1w MmPYNlM1OTByMEW=
human HL60 cells NFjUfmFRem:uaX\ldoF1cW:wIHHzd4F6 M13KO|czKGh? MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OThwNEOg{txONg>? MVKyOVY6Ozd6Nx?=
human BT474 cell NWjYWXlyWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn\5O|IhcA>? MlvuTY5pcWKrdHnvckBw\iCqdX3hckBDXDR5NDDj[YxtKHC{b3zp[oVz[XSrb36gZYZ1\XJiN{KgbJJ{KGK7IIPw[YN1em:yaH;0c41mfHKrYzDhcoFtgXOrc,-8kEBKSzVyPUKwMlch|ryPLh?= M3fsTVI{PDFyMEC1
THP1 cells NUXvXYRxTnWwY4Tpc44h[XO|YYm= Ml:3TY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgZ4hmdW:2YYjpd{Bw\iCWSGCxJINmdGy|LDDJR|UxRTN5IN88UU4> NYTPV3F2OTZ5OEm3OFI>
human 184B5 cells M3jGb2N6fG:2b4jpZ:Kh[XO|YYm= NWnzSnRTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOTh2QkWgZ4VtdHNiYomgV3JDKGG|c3H5MEBIUTVyPUO5MlM4KM7:TT6= MVWxPFY6OTh7NB?=
human KB cells Mlz4R5l1d3SxeHnjxsBie3OjeR?= NV;wUHYyPzJiaB?= NGrEXZhEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBMSiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUS0Mlc3KM7:TT6= M1j4[VIyQTR3MkWw
mouse RAW264.7 cells NYjTZmZ7TnWwY4Tpc44h[XO|YYm= MW[yOUDPxE1? MoLqNlAhcA>? MnjhTY5pcWKrdHnvckBw\iCSSUPLM2FMXCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2OgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDJ3IN88UUBi\nSncjCyNEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M4XQTlI1Ojl7NkG2
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human HCT116 cells M2rsbHBzd2yrZnXyZZRqd25iYYPzZZk> MVq3NkBp MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHHid49z[mGwY3WgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD13MT64NkDPxE1w MkHnNlU3QTN5OEe=
human HCT116 cells NI[5PGNEgXSxdH;4bYPDqGG|c3H5 MV63NkBp NUHOT5hWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PTZwMEGg{txONg>? MnfVNlE6PDV{NUC=
human PC3 cells NHLUR3JEgXSxdH;4bYPDqGG|c3H5 M2H1blczKGh? MXHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD14MT6zOUDPxE1w MVKyNlQ5ODh3MR?=
human HuH7 cells Mo\ZVJJwdGmoZYLheIlwdiCjc4PhfS=> MlG1O|IhcA>? MluwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKdVi3JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTZ5LkG4JO69VS5? NWXV[W5ROjV4OUO3PFc>
human A549 cells MV;Qdo9tcW[ncnH0bY9vKGG|c3H5 M1mzfFczKGh? MlLxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDNUS5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiYXLzc5Jj[W6lZTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTh{LkOyJO69VS5? MnvFNlU3QTN5OEe=
human A549 cells M3r5TGN6fG:2b4jpZ:Kh[XO|YYm= NFfRXoI4OiCq MoXIR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 NFP6UIQzOjR6MEi1NS=>
human PC3 cells MY\Qdo9tcW[ncnH0bY9vKGG|c3H5 NIPrOY0zPSEQvF2= MnfyNVIxKGh? MX;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjdDCyOUB2VSCjZoTldkAyOjBiaILzJIJ6KE2WVDDhd5NigSC{ZXzheIl3\SC2bzDEUXNQ NWPtbJV5OTZ4OECxOVk>
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... 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(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

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*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).

Dilution Calculator

Dilution Calculator

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 )

  • C1
    V1
    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID