A multi-kinase inhibitor
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Alternative(s)
70920LY294002
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LY294002 (hydrochloride)

Item No. 39171

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one, monohydrochloride
CAS Number
934389-88-5
Molecular Formula
C19H17NO3 • HCl
Formula Weight
343.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly solubleDMSO: SolubleWater: Slightly soluble
SMILES
O=C1C=C(N2CCOCC2)OC3=C(C4=CC=CC=C4)C=CC=C31.Cl
InChi Code
InChI=1S/C19H17NO3.ClH/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;1H
InChi Key
OQZQSRICUOWBLW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $152

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    25 mg

    $275

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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).