LY294002 化学構造
分子量: 307.34

品質と確認

カスタマーレビュー(8)

Quality Control & MSDS

製品情報

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製品の説明

生物活性

情報 LY294002は、p110α、p110δとp110βのPI3K阻害剤で、IC50 がそれぞれ 0.5 μM、0.57 μM、0.97 μMです。
目標 p110α p110δ p110β
IC50 0.5 μM 0.57 μM 0.97 μM[1]
In vitro試験 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試験 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]
臨床試験 LY294002 is currently in Phase I clinical trials in patients with cancers.
特集

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [4]

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.

細胞アッセイ: [2]

細胞系 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
処理時間 0–48 hours
方法 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.

動物実験: [3]

動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
製剤 Dissolved in DMSO plus 0.25 ml of PBS
投薬量 0–100 mg/kg
管理 Administered via i.p.
1

参考

化学情報

Download LY294002 SDF
分子量 307.34
化学式

C19H17NO3

CAS No. 154447-36-6
別名 N/A
溶解度 (25°C)
  • DMSO 36 mg/mL
  • 水 <1 mg/mL
  • エタノール 21 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 2-morpholino-8-phenyl-4H-chromen-4-one

研究分野

カスタマーレビュー (8)


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Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Immunofluorescence
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time 1 h
Results whole ADRP levels, estimated by Western blot , decreased only in the presence of MK -2206 and LY294002. In most cases, ADRP decorated the surface of small lipid droplets and appeared as little patches on large cytoplasmic lipid droplets. With the exception of SP600125, which induced a strong ADRP coating of almost all cytoplasmic lipid droplets (although this inhibitor did not increase ADRP synthesis), variation in the distribution of ADRP at the surface of lipid droplet was difficult to estimate, notably because the signal was faint and uneven.

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Rating
Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Western blot
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time
Results Addition of 50μM LY294002, a PI3-kinase inhibitor with higher stability and specificity provoked the complete arrest of PRL-induced β-casein synthesis and a drastic inhibition of that of ADRP.

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Source Molecular Oncology, 2012. LY294002 purchased from Selleck
Method Xenograft
Cell Lines SCC61, Detroit 562
Concentrations 100 mg/kg
Incubation Time 20 day
Results In female nude mice injected with SCC61 or Detroit 562 cells, both gefitinib and LY294002 inhibited tumor growth (Figure 5). However, the most effective way to inhibit tumor growth in EGFR resistant cell line tumors in vivo was to block both EGFR and PI3K activity with gefitinib and LY294002.

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Source Molecular Oncology, 2012 . LY294002 purchased from Selleck
Method Cell growth inhibition assay with MTT
Cell Lines SQ20B/SCC61/SCC35/SCC25/HN31/MSK921/Detroit 562/HN5 cell
Concentrations 10 uM
Incubation Time 4 h
Results LY294002 effectively reduced cell viability while the combination of LY294002 and gefitinib had an additive effect (Figure A).

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Rating
Source Oncogene, 2012, 31, 3277–3286. LY294002 purchased from Selleck
Method Western Blot
Cell Lines HEK-293 cells
Concentrations 30 uM
Incubation Time
Results We cultured HEK-293 cellsstably overexpressing p37d or p110d with the general PI3K –inhibitor, LY294002, or the MAPK-inhibitor, AZD6244. The inhibitors strongly affected the levels ofphosphorylated AKT S473 and ERK.

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Source Saraswati Sukumar of Johns Hopkins University School of Medicine. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

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Rating
Source Clin Cancer Res, 2011, 17, 7116-7126. LY294002 purchased from Selleck
Method Western blot
Cell Lines FaDu cells
Concentrations 20 μmol/L
Incubation Time 0-30 min
Results Both BGT226 and LY294002 attenuated p-AKT and p-p70 Thr389 expression after short-term treatment, whereas rapamycin diminished the phosphorylation of p70S6K but not AKT.

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Rating
Source Dr. Zhang of Tianjin Medical University. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0.1-20 μM
Incubation Time 24 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

製品表彰状 (22)

  • Dynamic expression profiling of Type I and Type III Interferon-stimulated hepatocytes reveals a stable hierarchy of gene expression. [Bolen CR, et al. Hepatology 2013;10.1002/hep.26657]

    PubMed: 23929627
  • Phosphoinositide 3 kinase inhibition restores neutrophil accuracy in the elderly: towards targeted treatments for immunesenescence. [Sapey E, et al. Blood 2014;123(2):239-48]

    PubMed: 24191150
  • Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. [Chang KY, et al. Clin Cancer Res 2011;17(22):7116-26]

    PubMed: 21976531
  • p37δ is a new isoform of PI3K p111δ that increases cell proliferation and is overexpressed in tumors. [Fransson S, et al. Oncogene 2012;31(27):3277-86]

    PubMed: 22020336
  • Molecular Phenotype Predicts Sensitivity of Squamous Cell Carcinoma of the Head and Neck to Epidermal Growth Factor Receptor Inhibition. [Young NR, et al. Mol Oncol 2012;7(3):359-68]

    PubMed: 23200321
  • Targeting the ABCG2-overexpressing multidrug resistant (MDR) cancer cells by PPARγ agonists. [Kenneth K.W. To, et al. British Journal of Pharmacology 2013;170(5):1137-51]

    PubMed: 24032744
  • Prolactin and epidermal growth factor stimulate adipophilin synthesis in HC11 mouse mammary epithelial cells via the PI3-kinase/Akt/mTOR pathway. [Pauloin A, et al. Biochim Biophys Acta 2012;1823(5):987-96]

    PubMed: 22426621
  • Membrane Depolarization Increases Membrane PtdIns (4, 5) P2 Levels through Mechanisms Involving PKC βII and PI4 Kinase. [Chen X, et al. J Biol Chem 2011;286(46):39760-7]

    PubMed: 21953466
  • Synergistic induction of human cathelicidin antimicrobial peptide gene expression by vitamin D and stilbenoids. [Guo C, et al. Mol Nutr Food Res 2013;10.1002/mnfr.201300266]

    PubMed: 24039193
  • Bilirubin mediated oxidative stress involves antioxidant response activation via Nrf2 pathway. [Qaisiya M, et al. Cell Signal 2013;26(3):512-20]

    PubMed: 24308969
  • Phosphatidylinositol 3- kinase is involved in Toll-like receptor 4-mediated BST-2/Tetherin regulation [Jones PH, et al. Cell Signal 2013;25(12):2752-61]

    PubMed: 24036213
  • Aquaporin3 Is Required for FGF-2-Induced Migration of Human Breast Cancers. [Cao XC, et al. PLoS One 2013;8(2):e56735]

    PubMed: 23468877
  • Expression of SLP-2 Was Associated with Invasion of Esophageal Squamous Cell Carcinoma. [Cao W, et al. PLoS One 2013;8(5):e63890]

    PubMed: 23667687
  • Nuclear Translocation of B-Cell-Specific Transcription Factor , BACH2, Modulates ROS Mediated Cytotoxic Responses in Mantle Cell Lymphoma. [Zheng Chen, et al. PLoS ONE 2013;8(8):e69126]

    PubMed: 23936317
  • Heregulin induces resistance to lapatinib-mediated growth inhibition of HER3-amplified cancer cells. [Sato Y, et al. Cancer Sci 2013;104(12):1618-25]

    PubMed: 24112719
  • Atorvastatin Sensitises Vascular Smooth Muscle Cells, but not Endothelial Cells, to TNF--induced Cell Death. [Giordano A, et al. Curr Pharm Des 2012;18(38):6331-8]

    PubMed: 23092297
  • Differential effects of exogenous and autocrine growth hormone on LNCaP prostate cancer cell proliferation and survival. [Nakonechnaya AO, et al. J Cell Biochem 2012;114(6):1322-35]

    PubMed: 23238889
  • Alpha-melanocyte stimulating hormone protects retinal pigment epithelium cells from oxidative stress through activation of melanocortin 1 receptor-Akt-mTOR signaling. [Cheng LB, et al. Biochem Biophys Res Commun 2013;443(2):447-52]

    PubMed: 24316214
  • RANKL downregulates cell surface CXCR6 expression through JAK2/STAT3 signaling pathway during osteoclastogenesis. [Li C, et al. Biochem Biophys Res Commun 2013;429(3-4):156-62]

    PubMed: 23142594
  • The dual mTORC1 and mTORC2 inhibitor AZD8055 inhibits head and neck squamous cell carcinoma cell growth in vivo and in vitro. [Li Q, et al. Biochem Biophys Res Commun 2013;440(4):701-6]

    PubMed: 24103749
  • The PI3K/AKT pathway promotes gefitinib resistance in mutant KRAS lung adenocarcinoma by a deacetylase-dependent mechanism [Victor Jeannot, et al. Cancer Cell Biology 2013;10.1002/ijc.28594]

    PubMed: 24374738
  • Phosphorylation of PRAS40-Thr246 Involves in Renal Lipid Accumulation of Diabetes. [Hao J ,et al. J Cell Physiol 2013;10.1002/jcp.24533]

    PubMed: 24347388

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