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.

Size Price Stock Quantity  
In DMSO USD 191 In stock
USD 147 In stock
USD 270 In stock
USD 770 In stock

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Cited by 70 Publications

13 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.

  • 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.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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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]

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
+ 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
+ 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
+ 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 <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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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.

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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