1. PI3K/Akt/mTOR
    Autophagy
  2. PI3K
    Autophagy

LY294002 (Synonyms: NSC 697286; SF 1101)

Cat. No.: HY-10108 Purity: 99.95%
Handling Instructions

LY294002 is a broad-spectrum inhibitor of PI3K, with IC50 of 0.5/0.57/0.97 μM for PI3Kα/PI3Kδ/PI3Kβ, respectively, also potently inhibits CK2 with IC50 of 98 nM.

For research use only. We do not sell to patients.

LY294002 Chemical Structure

LY294002 Chemical Structure

CAS No. : 154447-36-6

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10 mM * 1 mL in DMSO USD 66 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 84 In-stock
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Estimated Time of Arrival: December 31
100 mg USD 108 In-stock
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Estimated Time of Arrival: December 31
200 mg USD 156 In-stock
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Estimated Time of Arrival: December 31
500 mg USD 342 In-stock
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Customer Review

Customer Validation

    LY294002 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.

    MHCC97H cells are treated with either LY294002 (2.5, 5,10, 20, 40 μM) or ZSTK474 (0.5, 1, 2.5, 5, 10 μM) for 24 h. DMSO is used as the control. Cell lysates are subjected to western blot analysis with the indicated antibodies.

    LY294002 purchased from MCE. Usage Cited in: Chem Biol Interact. 2018 May 18;290:44-51.

    U2OS and MG-63 cells are treated with Gemcitabine, Licoricidin, or Gemcitabine+Licoricidin for 24 h, followed by the determination of active caspse-3 protein level using western blot. Cells without treatment are used as Control.

    LY294002 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.

    Huh7 and MHCC97H cells are treated with VPS34-IN1 for 24 h, and cell lysates are subjected to western blot analysis with the indicated antibodies.

    LY294002 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.

    Treatment of MHCC97H cells with AR-A014418 for 24 h inhibits the expression of CD133, detected by RT-PCR.

    LY294002 purchased from MCE. Usage Cited in: Biomed Res. 2017; 28 (8): 3383-3386

    Effects of various protease inhibitors on HO-1 and P-gp protein expressions.

    LY294002 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    Sertoli cells (SC) are pretreated with BAY11-7082 at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium. Expression of p-p65 and MMP-8 is measured by western blotting.

    LY294002 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    Sertoli cells (SC) are pretreated with LY294002 at 20 μM for 1 h followed by a 24-h treatment with MC-LR. Expression levels of p-p65 and MMP-8 are detected by western blotting.

    LY294002 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    Sertoli cells (SC) are pretreated with the PD98059 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

    LY294002 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.

    Sertoli cells (SC) are pretreated with the SP600125 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

    LY294002 purchased from MCE. Usage Cited in: J Cancer. 2016 Jun 5;7(9):1114-24.

    Effects of PI3K inhibition. (A) Protein levels of p-AKT S473 . (B) Inhibition of PI3K dose-dependently decreased the levels of p-EphA2S897 in vitro.

    LY294002 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;40:579-588.

    LY294002, a highly selective AKT inhibitor, completely blocks GSK3β phosphorylation induced by SDT. Effect of SDT on the expression of p-SMAD3, p-AKT and p-GSK3β. Images of p-GSK3β, GSK3β and GAPDH protein and mean values of protein level (relative to GAPDH) in cells.

    LY294002 purchased from MCE. Usage Cited in: Bosn J Basic Med Sci. 2017 May 20;17(2):132-137.

    Effects of Akt/adenosine monophosphate-activated protein kinaseon Valsartan(VAL)-mediated endothelial nitric oxide (NO) synthase (eNOS) phosphorylation and NO production in human umbilical vein endothelial cells (HUVECs). (A) The variation of VAL (10 μM)-induced eNOS activation after HUVECs are incubated with LY294002 [LY] (10 μM), Compound C (1 μM), L-NAME (500 μM) for 3 hours. (B)The variation of VAL (10 μM)-induced nitric oxide (NO) productionafter HUVECs are incubated with LY294002 (10 μM),

    LY294002 purchased from MCE. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975.

    NF-κB-dependent immune responses in testicular cells. Sertoli cells (SC), Leydig cells (LC), and germ cells (GC) are pretreated with BAY11-7082 (BAY) at 2 μM for 1 h, followed by the addition of MC-LR into the culture medium to a final concentration of 1 μM and incubation for 6 h. Expression of phosphorylated NF-κB p65 (p-p65) and total p65 is measured by western blotting. The ratio of p-65/p65 is determined by densitometry and is expressed as means±SEM (n=5).

    LY294002 purchased from MCE. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975.

    Inhibition of PI3K/AKT blocks MC-LR-induced NF-κB activation. SC, LC, and GC are pretreated with the PI3K/AKT inhibitor LY294002 (LY) at 20 μM for 1 h followed by a 6-h treatment with MC-LR. Expression of phosphorylated NF-κB p65 (p-p65) and total p65 are detected by western blotting.

    LY294002 purchased from MCE. Usage Cited in: Exp Gerontol. 2017 Oct 25;100:77-86.

    Cells are treated with LY294002 5 μM for 2 h followed by treated with MANF 200 ng/mL for another 12 h, and then cell lysates are immunoblotted to assess the phosphorylation of Akt, GSK3β, and Nrf2.

    LY294002 purchased from MCE. Usage Cited in: Exp Gerontol. 2017 Oct 25;100:77-86.

    Cells are treated with ML385 at the concentration of 5 μM for 12 h. The expression of Nrf2 and its translocation into nucleus are determined using western blot analysis.

    LY294002 purchased from MCE. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133.

    The regulation of PHP14 on Akt phosphorylation is possibly via PI3Kγ in LX-2 cells. Cells are serum starvation 24 h, then treated TGF-β1 (10 ng/mL) 2 h, then added LY294002 (5 μM) or AS252424 (10 μM) as indicated; after another 2 h incubation, Western blot is performed to assess the protein expression of p-Akt.

    LY294002 purchased from MCE. Usage Cited in: Neuropharmacology. 2017 Dec 7;131:190-199.

    LY294002 blocks the regulatory effects of GLP-1RA on Akt, GSK-3β and GnT-III. The inhibitor LY294002 (10 μM) is added to PC12 cells 1 h before Aβ25-35 and GLP-1RA treatment. The levels of p-Akt、total Akt、p-GSK3β、 total GSK-3β and GnT-III are detected by Western blot (n=3 per group).

    LY294002 purchased from MCE. Usage Cited in: Drug Des Devel Ther. 2018 Jan 11;12:137-148.

    Effects of LY294002 on AKT and p-AKT expression of hPDLCs. (A) The increased expression of osteogenic marker proteins can be interdicted by PI3K pathway inhibitor LY294002 in hPDLCs. The expression level of ALP and Runx2 is tested by Western blot (B).

    LY294002 purchased from MCE. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832.

    HSCs are pretreated with AICAR (500 μM), LY294002 (20 μM), PD98059 (10 μM), or Rapamycin (100 nM) for 2 h and then incubated with or without CoCl2 (150 μM) for 12 h. Expression levels of HIF-1α and VEGF are measured by Western blot analysis;

    LY294002 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 5;37(1):46.

    Treatment with LY294002 reverses Epithelial-mesenchymal transition (EMT) mediated by miR-10b overexpression. GAPDH is used as a loading control.

    LY294002 purchased from MCE. Usage Cited in: Arch Biochem Biophys. 2018 Mar 14;645:54-60.

    SK-BR-3, MCF-7, and MDA-MB-231 cells are treated with 1 μM Saracatinib for 48 h. After treatment, the Src protein expression is determined by western blot.

    LY294002 purchased from MCE. Usage Cited in: Cytokine. 2018 Mar 14;106:54-66.

    Effect of Berberine (BBR) (15-45 μM) on protein expression levels in IL-21 (20 ng/mL) stimulated AA-FLS cells. Western blot analysis of PI3K, mTOR, IL-23 and PTEN are estimated in whole cell lysates using densitometry analysis. Comparisons are made with: FLS versus AA-FLS+IL-21+BBR (15-45 μM)/LY294002 (20 μM).

    LY294002 purchased from MCE. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Apr;22(7):2005-2014.

    Western blot detection of p-AKT and Bcl-2 protein expressions in brain tissue. LY294002 treatment apparently alleviates PI3K/AKT signaling pathway activity, Bcl-2, and VEGF protein expressions.

    LY294002 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Apr 20;103:729-737.

    Representative Western blots show the effect of PI3K inhibitor LY294002 treatment for 24 h on PI3K p110a, Akt phosphorylation (P-Akt) and mTOR phosphorylation (P-mTOR). Total Akt and GAPDH are also detected by Western blot.

    LY294002 purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 16 May 2018.

    Western blot analysis of AKT, p-Akt, mTOR, p-mTOR, FOXO1 and p-FOXO1 expression in U-87 MG cells after treatment with LY294002 (20 μM), Rapamycin (50 nM) or NAC (5 mM) with or without Xihuang pill (XHP).

    LY294002 purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556.

    E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.

    LY294002 purchased from MCE. Usage Cited in: Blood. 2018 Jul 12;132(2):210-222.

    Phosphorylation of p-ERK1/2 and p-Akt in MKs pretreated with 0.5 μM NVP-ADW742, 10 μM U0126 or 20 μM LY294002 followed by rhIGF-1 treatment for 15 minutes.

    LY294002 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.

    Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in T98G-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

    LY294002 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.

    Western blot for p-Akt (Ser-473), Akt, p-GSK3β (Ser-9), GSK3β, β-catenin, and SCD1 in U87-R cells treated with DMSO, A939572, MK2206, A939572 plus MK2206, LY294002 and A939572 plus LY294002.

    LY294002 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 15;9(3):269.

    WB is used to detect the effect of EGF treatment for 4 h on the expression of YAP with the inhibitors of EGFR or its downsream members, including Gefitinib, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, Trametinib, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

    LY294002 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 13;37(1):189.

    H1299 cells transfected with si-MKRN2 are treated or not treated with the PI3K inhibitor LY294002 analyzed by western blot for the expression of proteins involved in cell migration and invasion.

    LY294002 purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Aug 24.

    GRPR-1 gene silencing lowers the positive protein levels of GRPR in kidney tissues of mice detected by immunohistochemistry. The positive protein levels of GRPR by immunohistochemical staining (400×).

    LY294002 purchased from MCE. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Aug;22(16):5377-5384.

    Western blot shows that L-NBP pretreatment significantly up-regulates p-AKT and Bcl2 protein contents in HT22 cells induced by I/R, whereas LY294002 intervention markedly alleviates the influence of L-NBP on p-AKT and Bcl-2 expressions.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    LY294002 is a broad-spectrum inhibitor of PI3K, with IC50 of 0.5/0.57/0.97 μM for PI3Kα/PI3Kδ/PI3Kβ, respectively, also potently inhibits CK2 with IC50 of 98 nM.

    IC50 & Target[1]

    p110α

    0.5 μM (IC50)

    p110δ

    0.57 μM (IC50)

    p110β

    0.97 μM (IC50)

    CK2

    98 nM (IC50)

    Autophagy

     

    In Vitro

    LY294002 (5 μM) completely inhibits the phosphorylation of PKB In HepG2 cells. LY294002 (5 μM) is also shown to block insulin-induced phosphorylation of PKB Ser473 in CHO-IR cells[1]. LY294002 is also a potent inhibitor of CK2 (casein kinase 2) with IC50 of 98 nM. LY294002 is also able to reduce the kinase activity of both isoforms of the serine/threonine kinases GSK3α and β[2]. When the CNE-2Z cell line is cultured in medium containing LY294002(0 μM, 10 μM, 25 μM, 50 μM, and 75 μM) for 24 h and 48 h, cell proliferation is remarkably decreased in a dose-dependent fashion[3].

    In Vivo

    Treatment with LY294002 (i.p.,50 mg/kg, 75 mg/kg) significantly reduces mean NPC tumor burden as compared with the control group. Treatment with 10 mg/kg or 25 mg/kg LY294002 is less effective in decreasing tumor burden. Mean NPC tumor burden treated with LY294002 is remarkably decreased in a dose-dependent manner, whereas mean body weight is no obvious difference between control and treated groups (LY294002, 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg)[3].

    Solvent & Solubility
    In Vitro: 

    DMSO : 14.9 mg/mL (48.48 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2537 mL 16.2686 mL 32.5373 mL
    5 mM 0.6507 mL 3.2537 mL 6.5075 mL
    10 mM 0.3254 mL 1.6269 mL 3.2537 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      LY294002 is dissolved in 0.5% DMSO[5].

       
    References
    Kinase Assay
    [2]

    PI3K inhibition by PI828 and LY294002 is determined in a radiometric assay using purified, recombinant enzymes (class IA and class IB) with 1 μM ATP. The kinase reaction is carried out for 1 h at room temperature (24°C) 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. Inhibitor (10 μM; PI828 and LY294002) is tested against the Upstate panel of kinases in 10 μM ATP[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Human nasopharyngeal carcinoma cell line CNE-2Z is seeded into 96-well plates at 5000 cells/well. Twenty-four hours after cells are seeded, the medium is removed and replaced in the presence of LY294002 (0 μM, 10 μM, 25 μM, 50 μM, and 75 μM) dissolved in DMSO or DMSO only for an additional 24 h and 48 h. To avoid any nonspecific toxic effects of DMSO on cell growth, DMSO concentrations are maintained at 0.5% in all experiments. MTT dye (5 mg/mL) is added to each well. The reaction is stopped by the addition of DMSO, and optical density is measured at 490 nm on a multiwell plate reader. Background absorbance of the medium in the absence of cells is subtracted. All samples are assayed in triplicate, and the mean for each experiment is calculated. Results are expressed as a percentage of control, which is considered to be 100%[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    Athymic nude mice are used when they are 6-8 weeks. Mice are randomly divided into free separated into five groups (n=4 mice). Mice are housed in the same environment with controlled temperature, humidity, and a 12 h light/dark cycle. Mice are inoculated subcutaneously with CNE-2Z cells (1×106 cells/mouse in 200 μL of RPMI-1640) into the flank. The tumor take rate is 100%. After 1 week, an intraperitoneal injection is performed to the xenograft mice with different dosage of LY294002 (10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg twice weekly (n=4 mice), each group for 4 weeks. Treated mice are monitored any signs. Body weight and tumors size are measured twice a week. Tumor size is measured using calipers and tumor volume is calculated (volume=long axis×short axis2). At the end of the treatment, all mice are euthanized. One part of tumor tissue is fixed in formalin and embedded in paraffin, and another part is stored at -70°C.
    Rats[4]
    Male Sprague-Dawley rats weighing 220-240 g are anesthetized by intraperitoneally injecting pentobarbital sodium (50 mg/kg). The animals are divided into 3 groups: NMDA+vehicle (DMSO) (n=46), NMDA+LY294002 (50 nmol) (n=25), and NMDA+Wortmannin (50 nmol) (n=23). Either LY294002 or wortmannin mixed with 200 nmol of NMDA in a total volume of 5 μL is injected into the vitreous cavity of one eye. The same volume of DMSO is injected into the vitreous cavity of the contralateral eye, which is used as a control. The injections are performed under a microscope using a 32-gauge needle, which is connected to a microsyringe. The needle is inserted approximately 1 mm behind the corneal limbus. Damage to neurons and blood vessels in the retina is assessed at 2 and 7 days after the injection. The effects of the intravitreal treatment with either LY294002 or Wortmannin alone on retinal neurons and blood vessels are also examined.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    307.34

    Formula

    C₁₉H₁₇NO₃

    CAS No.

    154447-36-6

    SMILES

    O=C1C=C(OC2=C1C=CC=C2C3=CC=CC=C3)N4CCOCC4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.95%

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    Product Name:
    LY294002
    Cat. No.:
    HY-10108
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    LY294002

    Cat. No.: HY-10108