A multi-kinase inhibitor
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Alternative(s)
39171LY294002 (hydrochloride)
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LY294002

Item No. 70920

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
CAS Number
154447-36-6
Synonyms
  • NSC 697286
Molecular Formula
C19H17NO3
Formula Weight
307.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
acidic PBS: <50 µg/mlbasic PBS: <50 µg/mlDMF: >25 mg/mlDMSO: >36 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/mlEthanol: >16.5 mg/mlPBS pH 7.2: <50 µg/ml
λmax
223, 302 nm
SMILES
O=c1cc(oc2c(cccc12)c1ccccc1)N1CCOCC1
InChi Code
InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
InChi Key
CZQHHVNHHHRRDU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $31

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    10 mg

    $59

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    25 mg

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    50 mg

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    Product Description

    LY294002 is a multi-kinase inhibitor.1 It inhibits casein kinase 2 (CK2; IC50 = 0.098 µM), the PI3K subunits p110α, p110β, p110δ, and p110γ (IC50s = 0.497, 0.554, 0.331, and 3.8 µM, respectively), and DNA-dependent protein kinase (DNA-PK; IC50 = 6 µM), among other kinases, as well as CK1, GSK3α, and GSK3β by greater than 40% at 10 µM.1,2,3 LY294002 (20 µM) inhibits LPS-induced activation of NF-κB in a reporter assay using RAW 264.7 macrophages in a PI3K-independent manner.4 It induces apoptosis and autophagy in SGC-7901 human gastric cancer cells when used at a concentration of 50 µM. LY294002 (2 ng/ml/kg) reduces tumor volume in DLD-1 and LoVo mouse xenograft models.5 It also reduces aging-induced increases in the number of aging human vascular smooth muscle cells (VSMCs) positive for senescence-associated β-galactosidase (SA-β-gal) when used at a concentration of 20 µM in the 5th to 15th generations.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gharbi, S.I., Zvelebil, M.J., Shuttleworth, S.J., et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem. J. 404(1), 15-21 (2007).

    2. Izzard, R.A., Jackson, S.P., and Smith, G.C. Competitive and noncompetitive inhibition of the DNA-dependent protein kinase. Cancer Res. 59(11), 2581-2586 (1999).

    3. Bain, J., Plater, L., Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochem. J. 408(3), 297-315 (2007).

    4. Avni, D., Glucksam, Y., and Zor, T. The phosphatidylinositol 3-kinase (PI3K) inhibitor LY294002 modulates cytokine expression in macrophages via p50 nuclear factor κB inhibition, in a PI3K-independent mechanism. Biochem. Pharmacol. 83(1), 106-114 (2012).

    5. Semba, S., Itoh, N., Ito, M., et al. The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells. Clin. Cancer Res. 8(6), 1957-1963 (2002).

    6. Tan, P., Wang, Y.-J., Li, S., et al. The PI3K/Akt/mTOR pathway regulates the replicative senescence of human VSMCs. Mol. Cell Biochem. 422(1-2), 1-10 (2016).

    Product Citations

    Nagakannan, P., Islam, M.I., Conrad, M., et al. Cathepsin B is an excutioner of ferroptosis. Biochim. Biophys. Acta Mol. Cell Res. 1868(3), 118928 (2021).

    Yousefi, B., Azimi, A., Majidinia, M., et al. Balaglitazone reverses P-glycoprotein-mediated multidrug resistance via upregulation of PTEN in a PPARγ-dependent manner in leukemia cells. Tumour Biol. 39(10), (2017).

    Saito, Y., Chikenji, T., Ozasa, Y., et al. PDGFR signaling mediates hyperproliferation and fibrotic responses of subsynovial connective tissue cells in idiopathic carpal tunnel syndrome. Sci. Rep. 7(1), 16192 (2017).

    McDougle, D.R., Watson, J.E., Abdeen, A.A., et al. Anti-inflammatory ω-3 endocannabinoid epoxides. Proc. Natl. Acad. Sci. USA 114(30), E6034-E6043 (2017).

    Yeh, H.-H., Kong, W., Hooper, K.l., et al. Differential effects of IFN-β on IL-12, IL-23, and IL-10 expression in TLR-stimulated dendritic cells. J. Leukoc. Biol. 98(5), 689-702 (2015).

    Reinke, E.N., Ekoue, D.N., Bera, S., et al. Translational regulation of GPx-1 and GPx-4 by the mTOR pathway. PLOS One 9(4), e93472 (2014).

    Gen, Y., Yasui, K., Nishikawa, T., et al. SOX2 promotes tumor growth of esophageal squamous cell carcinoma through the AKT/mammalian target of rapamycin complex 1 signaling pathway. Cancer Sci. 104(7), 810-816 (2013).