IC-87114 is a potent and ATP-competitive PI3K p110δ isoform-selective inhibitor (IC50 = 60 nM). It Inhibits p110α, p110β and p110γ only at much higher concentrations. It does not inhibit other PIK-related kinases such as ATM, ATR, DNA-PK, and mTOR even at concentrations up to 100 ÂµM.
CAS Number: 371242-69-2
Molecular Weight: 397.43
Chemical Name: 2-((6-amino-9H-purin-9-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 0.66 mg/mL(1.66 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
IC-87114 selectively inhibits PI3Kδ and not sensitive to PI3Kα, β, and γ. In human neutrophils, IC87114 (5 µM) potently inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-stimulated phosphatidylinositol triphosphate (PIP3) biosynthesis and chemotaxis. IC87114 (5 µM) also inhibits polarized morphology and spreading of neutrophils. In human acute myeloid leukemia (AML) blast cells, such as bone marrow mononuclear cells (BMMCs), IC87114 (10 µM) inhibits both constitutive and Flt-3-stimulated Akt phosphorylation and cell proliferation. It is also found that IC87114 (5 µM–30 µM) inhibits SCF- or IL-3-stimulated BMMC responses, which are not observed in PI3Kδ mutant (p110δD910A) cells. In anti-CD3-stimulated mice CD62L+ (naive) and CD62L− (effector/memory) CD4+ T cells, IC87114 inhibits proliferation and interferon-gamma (IFN-γ) production. The IC50 values of IC87114 are: (1) 1.2 µM and 40 nM, for CD62L+ and CD62L− cell proliferation, respectively; (2) 120 nM and 1 nM, for IFN-γ production of CD62L+ and CD62L− cells, respectively. Similar effects by IC87114 are also observed in human T cells. A recent study reveals that in chromaffin cells, IC87114 enhances the transient increase of PtdIns(4, 5)P2, which results in a potentiation of exocytosis.
In mice, IC87114 (15 mg/kg–60 mg/kg) inhibits the allergic response in the back skin and ear. In mice induced with anti-CD3 or ConA, IC87114 (30 mg/kg) reduces hypersensitivity responses and decreases plasma levels of cytokines, such as IL-2, IL-4, IL-17, IFN-γ, and tumor necrosis factor-α (TNF-α).
- Ali K, et al. Nature, 2004, 431(7011), 1007-1011.
- Sujobert P, et al. Blood, 2005, 106(3), 1063-1066.
- Sadhu C, et al. J Immunol, 2003, 170(5), 2647-2654.
Products are for research use only. Not for human use.
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