A selective inhibitor of p110δ
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IC-87114

Item No. 11589

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(6-amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
CAS Number
371242-69-2
Molecular Formula
C22H19N7O
Formula Weight
397.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
229, 262, 310 nm
SMILES
NC1=C2C(N(CC(N3C4=C(C)C=CC=C4)=NC5=C(C(C)=CC=C5)C3=O)C=N2)=NC=N1
InChi Code
InChI=1S/C22H19N7O/c1-13-6-3-4-9-16(13)29-17(27-15-8-5-7-14(2)18(15)22(29)30)10-28-12-26-19-20(23)24-11-25-21(19)28/h3-9,11-12H,10H2,1-2H3,(H2,23,24,25)
InChi Key
GNWHRHGTIBRNSM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    Product Description

    IC-87114 is a cell-permeable selective inhibitor of the PI3K catalytic subunit p110δ (IC50 = 0.5 μM).1 It less effectively inhibits p110γ and p110β (IC50 = 29 and 75 μM, respectively) and has no significant effect on p110α and several other kinases.1,2 This product is used to elucidate the role of p110δ in cells, including neutrophils, natural killer cells, and other types of leukocytes.1,2,3,4,5 It has also been used in mice.6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sadhu, C., Masinovsky, B., Dick, K., et al. Essential role of phosphoinositide 3-kinase δ in neutrophil directional movement. J. Immunol. 170(5), 2647-2654 (2003).

    2. Sadhu, C., Dick, K., Tino, W.T., et al. Selective role of PI3Kδ in neutrophil inflammatory responses. Biochem. Biophys. Res. Commun. 308(4), 764-769 (2003).

    3. Saudemont, A., Garçon, F., Yadi, H., et al. p110γ and p110δ isoforms of phosphoinositide 3-kinase differentially regulate natural killer cell migration in health and disease. Proc. Natl. Acad. Sci. USA 106(14), 5795-5800 (2009).

    4. Niedermeier, M., Hennessy, B.T., Knight, Z.A., et al. Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: A novel therapeutic approach. Blood 113(22), 5549-5557 (2009).

    5. Sujobert, P., Bardet, V., Cornillet-Lefebvre, P., et al. Essential role for the p110δ isoform in phosphoinositide 3-kinase activation and cell proliferation in acute myeloid leukemia. Blood 106(3), 1063-1066 (2005).

    6. Lee, K.S., Lee, H.K., Hayflick, J.S., et al. Inhibition of phosphoinositide 3-kinase δ attenuates allergic airway inflammation and hyperresponsiveness in murine asthma model. The FASEB Journal 20(3), 455-465 (2006).