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 NF\NeYhE\WyuIHnueoF{cW:wIHHzd4F6 M3y5eFI1KGh? NEjLR5pKdmirYnn0bY9vKG:oIHXwbZRp\WyrYXyg[5Jwf3SqIH\hZ5Rwei2rbnT1Z4VlKGOnbHygcYloemG2aX;uJI9nKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgdJJmNWmwY4XiZZRm\CCob4KgNlQhcHK|IHL5JINmdGxiaX72ZZNqd25iYYPzZZktKEmFNUC9NE4{QCEQvF2u M3XneVIzQDB2MUC4
Sf21 cells MYPGeY5kfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKG2xdYPlJJdqdGRidInw[UBRUTONYXzwbIEh\XiycnXzd4VlKGmwIGPmNlEh[2WubIOgZ48u\XiycnXzd4lv\yCQLYTldo1qdmGuIFjpd{11[WepZXSgbJVu[W5icEi1ZUB2e2mwZzDMMYFteGijLYDoc5NxcGG2aXT5cIlvd3OrdH;sJJN2[nO2cnH0[UBjgSCWTFOgZoF{\WRicHjvd5Bpd3JiaX3h[4lv\yxiSVO1NF0xNjVizszN NXXlPYNyOjJ3MkC2N|A>
Sf21 cells NGm1TW1HfW6ldHnvckBie3OjeR?= M1fyOGlvcGmkaYTpc44hd2ZibX;1d4UhemWlb33ibY5idnRiUFmzT4FteGijIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkKxJINmdGy|LDDJR|UxRTBwNTFOwG0v MmXJNVk4PDh{Nkm=
Sf9 cells MlLLSox2d3Knc3PlcpQheG:uYYLpfoF1cW:wIHHzd4F6 NYfYfVBYUW6qaXLpeIlwdiCxZjDoeY1idiCSSUPLZYxxcGFiZYjwdoV{e2WmIHnuJHNnQSClZXzsd{BjgSCobIXvdoV{[2WwdDDwc4xiemm8YYTpc44h[XO|YYmsJGlEPTB;MD61OUDPxE1w Mn;zNlEyOjF4M{G=
THP1 cells NXm0Rm8{TnWwY4Tpc44h[XO|YYm= MnL3TY5pcWKrdHnvckBw\iCVQ1[xMYlv\HWlZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gWGhROSClZXzsd{whUUN3ME2xMlAyKM7:TT6= NFfETHkyPjd6OUe0Ni=>
human PC3 cells NGKxN5VHfW6ldHnvckBie3OjeR?= NH[4fXk{OCCvaX6= NGTufHRKdmirYnn0bY9vKG:oIGDJN2shcW5iaIXtZY4hWEN|IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGFMXCCyaH;zdIhwenmuYYTpc44h[XRic3XybY5mKDR5MzDh[pRmeiB|MDDtbY5{KGK7IFXMTXNCNCCLQ{WwQVEvO87:TT6= MXWyN|QyODByNR?=
HeLa (human carcinoma) cells. M4r5RWZ2dmO2aX;uJIF{e2G7 Mk\xTY4hfmm2cn:gbY5pcWKrdHnvckBw\iCGTlGt[IVx\W6mZX70JJBzd3SnaX6gb4lv[XOnKFTORU1RUyliZoLvcUBJ\UyjIDjoeY1idiClYYLjbY5wdWFrIHPlcIx{NCCLQ{WwQVEvPCEQvF2u MkfSNVU3PTh6N{C=
THP1 cells Ml7jSpVv[3Srb36gZZN{[Xl? Ml3wTY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgVGtDN0GtdDDwbI9{eGixconsZZRqd25iaX6gWGhROSClZXzsd{whUUN3ME2xMlY2KM7:TT6= M3f3OFE3Pzh7N{Sy
HeLa cells MmDJSpVv[3Srb36gZZN{[Xl? M1G0bWlvcGmkaYTpc44hd2ZibWTPVkBxem:2ZXnuJIl{d2yjdHXkJIZzd21iSHXMZUBk\WyuczygTWM2OD1{LkWg{txONg>? M1TQNFE2PjV6OEew
human MCF7 cells NYTnXXFVS3m2b4TvfIlkyqCjc4PhfS=> NULnWIpES3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCrbjDwdoV{\W6lZTDv[kAzOCEQvF2gZ4htd3KxcYXpcoUh[nliU2LCJIF{e2G7LDDHTVUxRTJwNkOg{txONg>? MlO3NVg3QTF6OUS=
HeLa cells MVfGeY5kfGmxbjDhd5NigQ>? M{L0T2lvcGmkaYTpc44hd2ZiQWitO|UxOyCkaX7kbY5oKHSxIILlZ49u[mmwYX70JHBtczNiZYjwdoV{e2WmIHnuJGhmVGFiY3XscJMh[nliV3XzeIVzdiCkbH;0MEBKSzV;MzFOwG0v MkHENVcyOzV{NEi=
human MCF7 cells NGrwUm5EgXSxdH;4bYPDqGG|c3H5 MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME2zMlA5KM7:TT6= MVuxPFY6OTh7NB?=
human MCF7 cells NHnUZ3NEgXSxdH;4bYPDqGG|c3H5 M1TyNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[nliU2LCJIF{e2G7LDDHTV0{NjF4IN88UU4> MojBNVg3QTF6OUS=
human MDA-MB-231 cells NHvaeo1EgXSxdH;4bYPDqGG|c3H5 NY\CenpWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BqdiCycnXz[Y5k\SCxZjCyNEDPxE1iY3jsc5JweXWrbnWgZpkhW1KEIHHzd4F6NCCJSU2zMlMzKM7:TT6= NF3kSo8yQDZ7MUi5OC=>
human MDA-MB-231 cells MnzMR5l1d3SxeHnjxsBie3OjeR?= NEPqWlVEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKGOqbH;yc5F2cW6nIHL5JHNTSiCjc4PhfUwhT0l3ME20MlM2KM7:TT6= Moq4NVg3QTF6OUS=
human MDA-MB-468 cells NF:4cYVEgXSxdH;4bYPDqGG|c3H5 MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNE[4JINmdGy|IHnuJJBz\XOnbnPlJI9nKDJyIIXNJINpdG:{b4H1bY5mKGK7IGPSRkBie3Ojef-8kEBKSzVyPUSuO|Yh|ryPLh?= MlTZNVg3QTF6OUS=
human HCT116 cells M2TOOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnS0OFghcA>? M3zZc2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCxdnXy[ZhxemW|c3nu[{BRUTONYXzwbIEhUDFyNEfSJI12fGGwdDDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTVwMzFOwG0> MmLUNlIzOTJ5MkG=
human HCT116 cells MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoXjOFghcA>? M3n5PWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVUvQCEQvF2u MVuyNlIyOjd{MR?=
HeLa cells NEHWdmhDcW6maX7nJIFn\mmwaYT5JIF{e2G7 NVToS21NSmmwZHnu[{Bi\m[rbnn0fUBnd3JiUFmzMYtqdmG|ZTDpd49t[XSnZDDmdo9uKEinTHGgZ4VtdHNuIFvpQVYh|ryP MYexOVY2QDh5MB?=
human HCT116 cells MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mnf6OFghcA>? MWTHdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDIR3QyOTZiY3XscJMhd3[ncnX4dJJme3OrbnegVGk{U2GucHjhJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63JO69VS5? NHzUUJIzOjJzMkeyNS=>
MDA-MB-231 cells NV\tdVhUS3m2b4TvfIlkyqCjc4PhfS=> M1zKNmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZpkhW1KEIHHzd4F6NCCJSUWwQVYvPzFizszNMi=> MmnpNVg3QTF6OUS=
Sf9 cells Mn\lSpVv[3Srb36gZZN{[Xl? NWTTcFBOUW6qaXLpeIlwdiCxZjDDT|Ih\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD14Lkmg{txONg>? NITtWlkyQDN{MUexOi=>
human U87MG cells MoT3SpVv[3Srb36gZZN{[Xl? NXzWOIxiUW6qaXLpeIlwdiCxZjDHV2s{NWKndHGgbY4hcHWvYX6gWVg4VUdiY3XscJMh[nliRVzJV2EtKEmFNUC9PE4yKM7:TT6= NE\me|UyQDN2NU[wPS=>
human MDA-MB-468 cells MYDDfZRwfG:6aXRCpIF{e2G7 M3vVW2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiMUCgeW0h[2iub4LvdZVqdmViYomgV3JDKGG|c3H5MEBIUTVyPUiuNkDPxE1w NVTub3lLOTh4OUG4PVQ>
human A375 cells M2jub3Bzd2yrZnXyZZRqd25iYYPzZZk> NXPIe3c6PDZiaB?= M{nSVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDh[pRmeiB2NjDodpMtKEmFNUC9PE41KM7:TT6= NVqzV3ZSOTdyNEmyOFg>
human A375 cells NULGb4N1WHKxbHnm[ZJifGmxbjDhd5NigQ>? NV;Ob4xnUW6qaXLpeIlwdiCxZjDz[ZJ2dS2rbnT1Z4VlKHC{b3zp[oVz[XSrb36gc4YhcHWvYX6gRVM4PSClZXzsd{whUUN3ME24MlQh|ryPLh?= MUixO|YxOTd|OR?=
human HL60 cells NGTlcmlEgXSxdH;4bYPDqGG|c3H5 NYrYWHBzPzJiaB?= NXW5fI93S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEx4MDDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVkvQTRizszNMi=> M3HNPFIzPDhyOEWx
mouse Raw264 macrophage MWTGeY5kfGmxbjDhd5NigQ>? NFrmSXlKdmirYnn0bY9vKG:oIFO1ZU1u\WSrYYTl[EBRU0JxQXv0JJBpd3OyaH;yfYxifGmxbjDpckBud3W|ZTDSZZczPjRibXHjdo9xcGGpZTygTWM2OD1zMDFOwG0v Mn\hNVY4QDl5NEK=
Sf9 cells NGPDNmhHfW6ldHnvckBie3OjeR?= NXHKVYVkUW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJIJwfmmwZTDQTVNMKGW6cILld5Nm\CCrbjDT[lkh[2WubIOsJGlEPTB;MUCg{txONg>? MYCxNFk6QDN3MR?=
human MDA-MB-468 cells M3f3O2N6fG:2b4jpZ:Kh[XO|YYm= M2\wZWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1FSS2PQj20Olgh[2WubIOgZpkhW1KEIHHzd4F6NCCLQ{WwQVExNjRizszNMi=> M{HMSlE5PjlzOEm0
human PC3 cell NYnCTlB6WHKxbHnm[ZJifGmxbjDhd5NigQ>? MnmyO|IhcA>? MVLJcohq[mm2aX;uJI9nKGi3bXHuJHBEOyClZXzsJJBzd2yrZnXyZZRqd25iYX\0[ZIhPzJiaILzJIJ6KHOyZXP0do9xcG:2b33leJJq[yCjbnHsfZNqeyxiSVO1NF0yOi5zIN88UU4> MlnyNlM1OTByMEW=
human HL60 cells NFjGe2xRem:uaX\ldoF1cW:wIHHzd4F6 M2HGS|czKGh? NIOyc45CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MUiuOFMh|ryPLh?= Mn3mNlU3QTN5OEe=
human BT474 cell NU\odnA5WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUHvTGc2PzJiaB?= M323VGlvcGmkaYTpc44hd2ZiaIXtZY4hSlR2N{SgZ4VtdCCycn;sbYZmemG2aX;uJIFnfGW{IEeyJIhzeyCkeTDzdIVkfHKxcHjveI9u\XS{aXOgZY5idHm|aYRvwKwhUUN3ME2yNE44KM7:TT6= M3WyZ|I{PDFyMEC1
THP1 cells NHq4b|lHfW6ldHnvckBie3OjeR?= NHHWNFJKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KG:oIGTIVFEh[2WubIOsJGlEPTB;M{eg{txONg>? M163UVE3Pzh7N{Sy
human 184B5 cells NXHLZnpCS3m2b4TvfIlkyqCjc4PhfS=> NEG4SYZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckAyQDSENTDj[YxteyCkeTDTVmIh[XO|YYmsJGdKPTB;M{muN|ch|ryPLh?= MlzZNVg3QTF6OUS=
human KB cells NGf3PHJEgXSxdH;4bYPDqGG|c3H5 NXnZOI1iPzJiaB?= M1LQWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGtDKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NESuO|Yh|ryPLh?= M2\DR|IyQTR3MkWw
mouse RAW264.7 cells MV3GeY5kfGmxbjDhd5NigQ>? M4S2[FI2KM7:TR?= M1TqfFIxKGh? MlXmTY5pcWKrdHnvckBw\iCSSUPLM2FMXCCrbjDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGxRWy2rbnT1Z4VlKGmQT2OgdJJwfGWrbjDlfJBz\XO|aX;uJIF1KDJ3IN88UUBi\nSncjCyNEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MXWyOFI6QTZzNh?=
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human BJ cells MnjnSpVv[3Srb36gZZN{[Xl? NHLM[ZczPSEQvF2= NF6wd44zKGh? NFvEfIdC[3SrdnH0bY9vKG:oIFHreEBxcG:|cHjvdplt[XSrb36gZZQhXGi{M{C4JIlvKFCGR1[td5RqdXWuYYTl[EB{\XK3bTDzeIFzfmWmIHj1cYFvKEKMIHPlcIx{KGG2IEK1JJVOKHS{ZXH0[YQhOiCqcoOgZoVnd3KnIGDES2Yh[2ijbHzlcodmKGK7IHntcZVvd2Kub4T0bY5o NYLUcWxOOTZ5NkewPFU>
human HCT116 cells NWnFO|hiTnWwY4Tpc44h[XO|YYm= Mnf4NVAh|ryP MYSxNEBucW5? NH6ySW9KdmirYnn0bY9vKG:oIGDJN2tidHCqYTDpckBpfW2jbjDIR3QyOTZiY3XscJMhfXOrbnegX|MzWF2DVGCgZZQhOTBidV2gZYZ1\XJiMUCgcYlvew>? NYXxVJY{OjJ{MUK3NlE>
human HCT116 cells MVXGeY5kfGmxbjDhd5NigQ>? Ml;KNVAh|ryP MVSxNEBucW5? Ml3PTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNidYPpcochYzN{UG3BWHAh[XRiMUCgeW0h[W[2ZYKgNVAhdWmwcx?= MUCyNlIyOjd{MR?=
human HCT116 cells NVXIflJbTnWwY4Tpc44h[XO|YYm= NUTN[Vk6OTBizszN MlHPTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRYt1KFOnckS3N{BxcG:|cHjvdplt[XSrb36gZZQhOTBidV2gZpkhcW2vdX7vZoxwfCCjbnHsfZNqew>? NHr0S2wzOjJzMkeyNS=>
human HCT116 cells MoPhSpVv[3Srb36gZZN{[Xl? NXXRRlJoOTBizszN MkHNTY5pcWKrdHnvckBw\iCSSUPLZYxxcGFiSEGwOFdTKG23dHHueEBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDa4SgV4VzPDd|IIDoc5NxcG:{eXzheIlwdiCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz Ml:wNlIzOTJ5MkG=
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human H1299 cells MWDGeY5kfGmxbjDhd5NigQ>? NG\pVFkxNjFvM{Cg{txO Ml\FNlQhcA>? MYXJcoR2[3Srb36gc4YhTFJ3IHX4dJJme3Orb36gbY4hcHWvYX6gTFEzQTliY3XscJMh[XRiMD6xJJRwKDNyIIXNJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> M3rjXFIzPjJ{ME[5
human H1299 cells NYq5PJJJTnWwY4Tpc44h[XO|YYm= M3;hOlAvOS1|MDFOwG0> MYmyOEBp Mo\PTY5lfWO2aX;uJI9nKEqQSz3t[YRq[XSnZDDDTG9RKGW6cILld5Nqd25iaX6gbJVu[W5iSEGyPVkh[2WubIOgZZQhOC5zIITvJFMxKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= NYrUTHpsOjJ4MkKwOlk>
HEK293 cells NGPJS|lHfW6ldHnvckBie3OjeR?= M3XUTlEvPSCq NV;jbGh5TGm|cHzhZ4Vu\W62IH;mJHs{UF2OU1Sg[pJwdSCqdX3hckA2UFR4IILlZ4VxfG:{IHX4dJJme3OnZDDpckBJTUt{OUOgZ4VtdHNiYX\0[ZIhOS53IHjyd{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZx?= MU[yNlU{PzF3Mx?=
human U251HRE cells NILadWRHfW6ldHnvckBie3OjeR?= MmXMTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhUEmIMTDhZ5RqfmG2aX;uJIlvKGi3bXHuJHUzPTGKUlWgZ4VtdHNiYomgZ4VtdCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 MXuxPFUxOTZyMR?=
human HCT116 cells MnnrSpVv[3Srb36gZZN{[Xl? MYCxNEDPxE1? MY\Jcohq[mm2aX;uJI9nKEGtdDDlfJBz\XO|aX;uJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEB2VSCkeTDpcY12dm:kbH;0JIFv[Wy7c3nz MVuyNlIyOjd{MR?=
Sf9 cells NGX4[YJndHWxcnXzZ4VvfCCyb3zhdol7[XSrb36gZZN{[Xl? NFvuRpFKdmirYnn0bY9vKG:oIHj1cYFvKFCLM1vnZY1u[SCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJIJ6KG[udX;y[ZNk\W62IIDvcIFzcXqjdHnvckBie3OjeR?= M1XVbVIyOTJzNkOx
human HCT116 cells MV\Qdo9tcW[ncnH0bY9vKGG|c3H5 NUXGRmJ1PzJiaB?= MnPrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NUGuPFIh|ryPLh?= MXGyOVY6Ozd6Nx?=
human HCT116 cells NXn6O2s5S3m2b4TvfIlkyqCjc4PhfS=> M2LTVFczKGh? M4XENmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVU3NjBzIN88UU4> MX:yNVk1PTJ3MB?=
human PC3 cells NID2NXZEgXSxdH;4bYPDqGG|c3H5 NYDXPGVvPzJiaB?= MnTMR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;NkGuN|Uh|ryPLh?= MknVNlI1QDB6NUG=
human HuH7 cells NVLGbVVvWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF\tclk4OiCq MYLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCjYoPvdoJidmOnIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PjdwMUig{txONg>? NXnBWoZWOjV4OUO3PFc>
human A549 cells M1\FOnBzd2yrZnXyZZRqd25iYYPzZZk> MkPqO|IhcA>? NHjEZXVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFG1OFkh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDhZpNwemKjbnPlJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;OEKuN|Ih|ryPLh?= NXTlWlJZOjV4OUO3PFc>
human A549 cells NHu2U|ZEgXSxdH;4bYPDqGG|c3H5 MmC4O|IhcA>? NYOzSVl1S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSTV2OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6 NYCwNoxFOjJ2OEC4OVE>
human PC3 cells M1LzbnBzd2yrZnXyZZRqd25iYYPzZZk> MWOyOUDPxE1? M2PGfVEzOCCq M{XWXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHH0JFI2KHWPIHHmeIVzKDF{MDDodpMh[nliTWTUJIF{e2G7IILlcIF1cX[nIITvJGROW09? NFrCUGUyPjZ6MEG1PS=>
human H460 cells MmPISpVv[3Srb36gZZN{[Xl? MmnlN|Ah|ryP Mnz6TY5pcWKrdHnvckBw\iCSSUPLJIlvKGi3bXHuJGg1PjBiY3XscJMh[XO|ZYPz[YQh[XNiQXv0JJBpd3OyaH;yfYxifGmxbjDheEBU\XJiNEezJJVxKHSxIEOwJJVO MmixNVg2ODF4MEG=
human IGROV1 cells NVHsUpR3TnWwY4Tpc44h[XO|YYm= NGLaSWMzPCCq NID0[5VE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBKT1KRVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexJJBp[XOnIHH0JFEh\m:uZDDJR|UxKGGodHXyJFI1KGi{czDifUBndG:5IHP5eI9u\XS{eR?= MUCyNVIyPjF3MR?=
human IGROV1 cells NHfKTHlHfW6ldHnvckBie3OjeR?= NFy1dpkzPCCq NHf4cXJE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBKT1KRVkGgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFexJJBp[XOnIHH0JFUh\m:uZDDJR|UxKGGodHXyJFI1KGi{czDifUBndG:5IHP5eI9u\XS{eR?= MV6yNVIyPjF3MR?=
human H4 cells MkO5SpVv[3Srb36gZZN{[Xl? NHTGRngzKGh? MVrE[YNz\WG|ZTDpckBHYV[HLWLGVEshfmW|aXPs[UBqdnSnboPpeJkheGW{IHPlcIwhcW5iaIXtZY4hUDRiY3XscJMh[W[2ZYKgNkBpenNicnXsZZRqfmVidH:gZ49vfHKxbB?= NY\vTIRjOThyMkS1PFQ>
human MGC803 cells Mo[2SpVv[3Srb36gZZN{[Xl? MYKyOUDPxE1? NXH3XoxkPDhiaB?= NF3WZVNE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBOT0N6MEOgZ4VtdHNiYYPz[ZN{\WRiYYOgZYNkfW23bHH0bY9vKGG2IFeyM20heGijc3WgZZQhOjVidV2gZYZ1\XJiNEigbJJ{KHW|aX7nJJBzd3CrZHn1cUBqd2SrZHWgd5RicW6rbnegZYZ1\XJiNEigbJJ{KGK7IH\sc5ch[3m2b33leIVzKHKnbHH0bZZmKHSxIHPvcpRzd2x? NVvxRXlZOjRzMUm4Olk>

... 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
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    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
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    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