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IC-87114 (PIK-293) is the first isoform-selective PI3K inhibitor. This quinazolinone purine inhibits p110δ (IC50=0.13µM) at mid-nanomolar concentrations and shows 100-1000-fold selectivity over other class I PI3Ks (p110α, p110β and p110γ ). The selectivity of IC-87114 is remarkable given that the residues that line the ATP binding pocket of the class I PI3Ks are highly conserved. IC-87114 down-regulated p-Akt and p-FOXO3a, reduced proliferation and induced apoptosis in AML primary cells overexpressing p110δ PI3K. Inhibition of PI3K delta with IC-87114 blocked both fMLP- and TNF1 alpha-induced neutrophil superoxide generation and elastase exocytosis. The PI3K delta inhibitor IC-87114 also blocked TNF1 alpha-stimulated elastase exocytosis from neutrophils in a mouse model of inflammation.
| Cell Experiment | |
|---|---|
| Cell lines | human neutrophil |
| Preparation method | Measurement of neutrophil adhesion and migration The adhesion assays were performed by the following modifications of the procedure described by Sadhu et al. Briefly, 96-well plates were coated overnight with 5 μg/ml ICAM-1/Ig, blocked with 1% HSA (no. 12666; Calbiochem, La Jolla, CA) in RPMI 1640, and 2 × 105 neutrophils (untreated or pretreated with the indicated concentration of IC87114) were added in triplicate wells. After incubation at 37°C for the desired time, 5% CO2 glutaraldehyde was added to a 1% final concentration. Unbound cells were removed by washing the wells in water and the adherent cells were stained with crystal violet. Cell adhesion was quantified by reading the intensity of crystal violet on Spectra MAX (Molecular Devices, Sunnyvale, CA) at 570 nm. |
| Concentrations | 1 μ M |
| Incubation time | 3 h |
| Animal Experiment | |
|---|---|
| Animal models | WT B6 and p110δD910A Mice |
| Formulation | 1% methylcellulose (MCL) |
| Dosages | 30 mg/kg once |
| Administration | orally |
| Molecular Weight | 397.43 |
| Formula | C22H19N7O |
| CAS Number | 371242-69-2 |
| Solubility (25°C) | DMSO 8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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