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

LY294002 est un inhibiteur de PI3K à large spectre de avec des IC50s de 0,5, 0,57 et 0,97 μM pour PI3Kα, PI3Kδ et PI3Kβ, respectivement. LY294002 inhibe également CK2 avec un IC50 de 98 nM. LY294002 est un ADN-PK compétitif qui se lie de manière réversible au domaine kinase de l'ADN-PK avec un IC50 de 1,4 μM. LY294002 est un activateur de l'autophagie et de l'apoptose.

LY294002 ist ein Breitspektrum-Inhibitor von PI3K mit IC50s von 0,5, 0,57 und 0,97 μM für PI3Kα, PI3Kδ und PI3Kβ. LY294002 hemmt auch CK2 mit einem IC50 von 98 nM. LY294002 ist ein kompetitiver DNA-PKInhibitor, der reversibel an die Kinasedomäne der DNA-PK mit einem IC50 von 1,4 bindet μM. LY294002 ist ein autophagy- und apoptosis activator.

LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator.

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LY294002 Chemical Structure

LY294002 Chemical Structure

CAS No. : 154447-36-6

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Customer Review

Based on 731 publication(s) in Google Scholar

Other Forms of LY294002:

Top Publications Citing Use of Products

676 Publications Citing Use of MCE LY294002

IHC
WB
IF
Proliferation Assay

    LY294002 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2023 May 22.

    LY294002 (10 µM; 12 h) significantly increases the expression of C-caspase3 protein and decreases the expression of Bcl-2 protein in primary neuronal cells.

    LY294002 purchased from MedChemExpress. Usage Cited in: Exp Ther Med. 2023 May 22.

    LY294002 (10 µM; 12 h) significantly inhibits the proliferation of primary neuronal cells.

    LY294002 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 14.

    Both of LY294002 (LY; 30 μM) and Wortmannin (Wort; 50 nM) can downregulate the expression of ACE2 in HPAEpiC cells.

    LY294002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.  [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Jan 28;10(1):453.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: J Cell Physiol. 2019 Feb;234(2):1567-1577.  [Abstract]

    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 MedChemExpress. Usage Cited in: Biol Trace Elem Res. 2019 Aug;190(2):327-335.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    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.

    LY294002 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Oct;20(4):3811-3819.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2019 Jan;19(1):177-186.   [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: J Neuropathol Exp Neurol. 2019 Feb 1;78(2):157-171.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 8;508(2):398-404.  [Abstract]

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

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

    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 MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 13;37(1):189.  [Abstract]

    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 MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Jun 25;37(1):122.  [Abstract]

    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 MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 5;37(1):46.  [Abstract]

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

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

    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 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2018 Nov;39(11):1787-1796.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    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 MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Oct;106:1348-1356.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2018 Jul;103:729-737.  [Abstract]

    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 MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556.  [Abstract]

    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 MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.  [Abstract]

    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 MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jan 4;8:960.  [Abstract]

    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 MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2018 Sep 1;57(9):1675-1684.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Nov;22(11):5311-5321.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Drug Des Devel Ther. 2018 Jan 11;12:137-148.  [Abstract]

    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 MedChemExpress. Usage Cited in: Neuropharmacology. 2018 Mar 15;131:190-199.  [Abstract]

    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 MedChemExpress. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133.  [Abstract]

    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 MedChemExpress. Usage Cited in: Reprod Biol Endocrinol. 2018 May 31;16(1):55.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: World J Gastroenterol. 2018 Feb 21;24(7):819-832.  [Abstract]

    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 MedChemExpress. Usage Cited in: Toxins (Basel). 2018 Sep 28;10(10). pii: E398.  [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: Onco Targets Ther. 2018 Oct 9;11:6693-6703.   [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: Cytokine. 2018 Jun;106:54-66.  [Abstract]

    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 MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Apr;22(7):2005-2014.  [Abstract]

    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 MedChemExpress. Usage Cited in: Eur Rev Med Pharmacol Sci. 2018 Aug;22(16):5377-5384.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Food Nutr Res. 2018 Oct 12;62.  [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 18;503(4):3212-3218.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2018 Apr;15(4):5685-5693.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2019 Jan;17(1):1372-1378.  [Abstract]

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

    LY294002 purchased from MedChemExpress. Usage Cited in: Exp Neurobiol. 2018 Dec;27(6):472-488.   [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2018;51(4):1566-1583.  [Abstract]

    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 purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2018 Jun 26;2018:6049498.  [Abstract]

    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 MedChemExpress. 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 purchased from MedChemExpress. Usage Cited in: Environ Pollut. 2017 Oct;229:964-975.  [Abstract]

    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 MedChemExpress. Usage Cited in: Exp Gerontol. 2017 Dec 15;100:77-86.  [Abstract]

    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 MedChemExpress. Usage Cited in: Bosn J Basic Med Sci. 2017 May 20;17(2):132-137.  [Abstract]

    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 purchased from MedChemExpress. 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 MedChemExpress. Usage Cited in: J Cancer. 2016 Jun 5;7(9):1114-24.  [Abstract]

    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 MedChemExpress. Usage Cited in: Cell Physiol Biochem. 2016;40(3-4):579-588.  [Abstract]

    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.

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    Description

    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively[1]. LY294002 also inhibits CK2 with an IC50 of 98 nM[2]. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator[3].

    IC50 & Target[1][2][4]

    p110α

    0.5 μM (IC50)

    p110δ

    0.57 μM (IC50)

    p110β

    0.97 μM (IC50)

    human CK2

    98 nM (IC50)

    human CK2α2

    3.869 μM (IC50)

    DNA-PK

    1.4 μM (IC50)

    In Vitro

    LY294002 (0-75 μM; 24 hours and 48 hours) remarkably decreases human nasopharyngeal carcinoma CNE-2Z cells in a dose-dependent fashion[4].
    LY294002 (0-75 μM; 24 hours and 48 hours ) induces CNE-2Z cells apoptosis rate in dose-dependent[4].
    LY294002 (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 (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].

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

    Cell Proliferation Assay[4]

    Cell Line: CNE-2Z cells
    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[4]

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

    Western Blot Analysis[4]

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

    LY294002 (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 (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].

    MedChemExpress (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: Intraperitoneal injection; twice weekly, for 4 weeks
    Result: Mean Nasopharyngeal carcinoma (NPC) tumor burden was remarkably decreased in a dose-dependent manner.
    Molecular Weight

    307.34

    Formula

    C19H17NO3

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (162.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 50 mg/mL (162.69 mM; Need ultrasonic)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.87 mg/mL (9.34 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.25 mg/mL (7.32 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 15.71 mg/mL (51.12 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.95%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 3.2537 mL 16.2686 mL 32.5373 mL 81.3431 mL
    5 mM 0.6507 mL 3.2537 mL 6.5075 mL 16.2686 mL
    10 mM 0.3254 mL 1.6269 mL 3.2537 mL 8.1343 mL
    15 mM 0.2169 mL 1.0846 mL 2.1692 mL 5.4229 mL
    20 mM 0.1627 mL 0.8134 mL 1.6269 mL 4.0672 mL
    25 mM 0.1301 mL 0.6507 mL 1.3015 mL 3.2537 mL
    30 mM 0.1085 mL 0.5423 mL 1.0846 mL 2.7114 mL
    40 mM 0.0813 mL 0.4067 mL 0.8134 mL 2.0336 mL
    50 mM 0.0651 mL 0.3254 mL 0.6507 mL 1.6269 mL
    60 mM 0.0542 mL 0.2711 mL 0.5423 mL 1.3557 mL
    80 mM 0.0407 mL 0.2034 mL 0.4067 mL 1.0168 mL
    100 mM 0.0325 mL 0.1627 mL 0.3254 mL 0.8134 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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