1. PI3K/Akt/mTOR
    Stem Cell/Wnt
    Cell Cycle/DNA Damage
    Apoptosis
  2. PI3K
    Casein Kinase
    DNA-PK
    Apoptosis
  3. LY294002 hydrochloride

LY294002 hydrochloride 

Cat. No.: HY-10108A
Handling Instructions

LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research.

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

LY294002 hydrochloride Chemical Structure

LY294002 hydrochloride Chemical Structure

CAS No. : 934389-88-5

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Top Publications Citing Use of Products

472 Publications Citing Use of MCE LY294002 hydrochloride

    LY294002 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5311-5321.

    The expression of PI3K, Akt, p-Akt, HO-1, LC3-II/LC3-I and Beclin-1 in LY294002 group after pharmorubicin treatment are examined by Western blot. The protein expression in LY294002 group is decreased.

    LY294002 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;40(3-4):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 hydrochloride 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 CGP 48933 (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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Exp Gerontol. 2017 Dec 15;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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Neuropharmacology. 2018 Mar 15;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 hydrochloride 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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Oncol Lett. 2018 Apr;15(4):5685-5693.

    HeLa cells are treated with GST S100A6 and LY294002 for 72 h, and total Akt, total GSK3β, β catenin, p Akt and p GSK3β are detected using western blotting

    LY294002 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Cytokine. 2018 Jun;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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Jul;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 hydrochloride purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498.

    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 hydrochloride 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 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684.

    The hypoxia-aggravated phosphorylation of Akt and mTOR is inhibited by LY294002, a PI3K inhibitor (P<0.01), suggesting that hypoxia-induced Akt phosphorylation was through PI3K activation.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684.

    LY294002 and Rapamycin also down-regulates the HIF-1α expression under hypoxic condition (P<0.01) and inhibits hypoxia-induced expressions of CTGF (P<0.05) and collagen I (P<0.05 or P<0.01).

    LY294002 hydrochloride purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.

    p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.

    LY294002 hydrochloride 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 hydrochloride 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 hydrochloride 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 ZD1839, LY294002, Wortmannin, GSK2334470, BX-795, MK-2206, GSK1120212, and U0126 in the Si RhoA transfected HepG2 and SMMC7721 cells for 48 h in HepG2 and SMMC7721 cells.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356.

    ECa109 and EC9706 cells are treated with various doses of LY294002 (0, 10, 20 μM) for 24 h. Total proteins are extracted for the analysis of key proteins in PI3K/Akt/ mTOR signaling pathway by Western blot.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356.

    ECa109 and EC9706 cells are treated with 20 μM LY294002 for different time (0, 3, 6, 12, 24 h). Total proteins are extracted for the analysis of key proteins in PI3K/Akt/ mTOR signaling pathway by Western blot.

    LY294002 hydrochloride 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 hydrochloride purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Feb;234(2):1567-1577.

    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 hydrochloride 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.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Toxins (Basel). 2018 Sep 28;10(10). pii: E398.

    Expression levels of p-AKT/AKT, p-mTOR/mTOR, and LC3II/LC3I after adding PI3K inhibitors (LY294002) in the experiments.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796.

    Effects of LY294002 or AKT siRNA on the levels of total AKT, pAKT, phosphorylated PRAS40 and pMDM2 are examined by Western blot analysis in MCF-7 cells when HBXIP was overexpressed. Effects of MK-2206 or HBXIP siRNA on the levels of total AKT, pAKT, pPRAS40, and pMDM2 are examined by Western blot analysis in MCF-7-HBXIP cells.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Journal of Nanjing Agricultural University. 2018, 41(4): 708-714.

    Effects of PI3K inhibitors on the expression of Cdc2, Cdc25B and CyclinB1 in sertoli cells.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Food Nutr Res. 2018 Oct 12;62.

    Western blotting of the PI3K/Akt signaling and the fold activation data analysis.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55.

    Western blot analysis of claudin 5, occludin and ZO-1 in TM4 cells, cells are treated with 100 nM Leptin or pre-treated with different inhibitors following a 100 nM Leptin treatment.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Onco Targets Ther. 2018 Oct 9;11:6693-6703. 

    LY294002, an Akt inhibitor, is applied to the inhibition on prolifera¬tion.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 18;503(4):3212-3218.

    Western blot analysis for phospho-PI3K, total PI3K, phospho-Akt, total Akt, phospho-mTOR and total mTOR in control/Brgfl/fl+NS, control/Brgfl/fl+LY294002 group, SFTPC-Cre/Brgfl/fl+LY294002 and SFTPC-Cre/Brgfl/fl+NS group.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Biol Trace Elem Res. 2019 Aug;190(2):327-335.

    Number of cells stained positive for ALP increase significantly after stimulation with orthosilicic acid for 72 h and decrease after stimulation with LY294002 for the last 48 h of this period.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Oncol Lett. 2019 Jan;17(1):1372-1378.

    Pretreatment of C666-1 cells with the phosphatidylinositol 3-kinase/Akt inhibitor LY294002 counteracts the triptolide‑induced inhibition of proliferation and apoptosis.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Jan;19(1):177-186. 

    Western analysis of p-AKT1 and AKT1 in the treatment of MCF7 alone, MCF7 co-cultured, anti-TGF-β1 and LY29400

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 8;508(2):398-404.

    TUNEL staining shows green fluorescence of apoptosis HK-2 cells with the treatment of HG+PPQ or HG+PPQ+LY294002.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;51(4):1566-1583.

    The protein expressions of PI3K, p-PI3K, Akt, p-Akt, Bax, Bcl-2, Cleaved-caspase-3, Caspase-3, are measured by Western blotting with the treatment of LY294002, CDDP or Icariin.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: J Neuropathol Exp Neurol. 2019 Feb 1;78(2):157-171.

    Western analysis the protein expression of PI3K, p-mTOR, mTOR, p-AKT, AKT with or without the treatment of OGD, 450 μM GBP and 10 μM LY294002.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Exp Neurobiol. 2018 Dec;27(6):472-488. 

    LY294002 aggravates the suppression of PI3K/AKT signaling pathway induced by MEHP. CGCs are pre-treated with 5 μM of LY294002, an inhibitor of PI-3K/AKT pathway, for 2 h followed by treatment with 250 MEHP for 24 h.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.

    Protein levels of p53, p21 and MDM2 are upregulated in LNCaP cells after treatment with 2.0 μM concentration of RG7388.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.

    Apoptotic cell death in LNCaP cells shown by Fluorescence image obtained using the DEVD-amc. The results of cell death induced by SAHA and RG7388 treatment for 24 hrs are shown.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.

    Western blot analysis of BAX and PARP (full length and cleaved PARP) expressions in treated LNCaP cells with the treatment of SAHA or RG7388.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.

    Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A) The expression of E-cadherin (green) in each group was determined using immunofluorescence. (B) Quantification of E‑cadherin expression.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.

    Expression of E-cadherin and vimentin is regulated by COX‑2. MG‑63 cells are infected with control or COX-2-overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (C) The expression of vimentin in each group. (D) Quantification of vimentin expression.

    LY294002 hydrochloride purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.

    Expression of NF‑κB p65 protein is regulated by COX‑2. MG‑63 cells were infected with control or COX‑2‑overexpressing lentivirus, and treated with or without the COX‑2 inhibitor NS398 or the PI3K inhibitor LY294002. (A)The expression of NF-κB p65 (green) in each group was determined by immunofluorescence. (B) Quantification of NF-κB p65 expression.

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    Description

    LY294002 hydrochloride is a potent and broad-spectrum PI3K inhibitor, with IC50 values of 0.5, 0.57, and 0.97 μM for P110α, P110δ and P110β, respectively. LY294002 hydrochloride also inhibits CK2 with an IC50 of 98 nM. LY294002 hydrochloride can be used for pancreatic cancer research[1][2][3].

    IC50 & Target

    CK2

    0.098 μM (IC50)

    CK2α2

    3.869 μM (IC50)

    In Vitro

    LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4].
    LY294002 hydrochloride (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4].
    LY294002 hydrochloride (10-75 μM) significantly decreases p-Akt (S473) expression levels and up-regulates caspase-9 activity in CNE-2Z cells. Total Akt protein level is not difference with different concentration[4].
    LY294002 hydrochloride (5, 10, 100 µM; for 2 hours) treatment partially suppresses Lysophosphatidic acid (LPA)-induced (20 µM; for 4 hours) nuclear translocation of YAP, accompanied by a reduction in p-AKT levels[6].

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

    Cell Proliferation Assay

    Cell Line: CNE-2Z cells[4]
    Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
    Incubation Time: 24 hours and 48 hours
    Result: Decreased CNE-2Z cells in a dose-dependent fashion.

    Apoptosis Analysis

    Cell Line: CNE-2Z cells[4]
    Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
    Incubation Time: 24 hours and 48 hours
    Result: Induced apoptosis rate in a dose-dependent manner.

    Western Blot Analysis

    Cell Line: CNE-2Z cells[4]
    Concentration: 0 μM, 10 μM, 25 μM, 50 μM, and 75 μM
    Incubation Time: 24 hours and 48 hours
    Result: Decreased phosphorylated Akt (S473) expression levels were significantly, up-regulated caspase-9 activity in CNE-2Z cells in treated group.
    In Vivo

    LY294002 hydrochloride (10, 25, 50, 75 mg/kg; i.p.; twice weekly; for 4 weeks) significantly reduces mean NPC tumor burden in a dose-dependent manner. LY294002 (10, 25 mg/kg) is less effective in decreasing tumor burden[4].
    LY294002 hydrochloride (1.2 mg/kg per day; i.p.; for 14 days) prevents Leptin (60 ug/kg)-induced adverse effects on spermatozoa in Sprague-Dawley rats[5].

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

    Animal Model: Athymic nude mice (6-8 weeks) with CNE-2Z xenograft[4]
    Dosage: 10 mg/kg, 25 mg/kg, 50 mg/kg, and 75 mg/kg
    Administration: IP; twice weekly, for 4 weeks
    Result: Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.
    Molecular Weight

    343.80

    Formula

    C19H18ClNO3

    CAS No.
    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    LY294002 hydrochloride
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