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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 |
|---|
| PI3Kγ inhibitor AZ2
PI3Kγ inhibitor AZ2 is a highly selective PI3Kγ inhibitor (The pIC50 value for PI3Kγ is 9.3). |
| NIBR-17
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth. |
| RV-1729
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). |
| Vulolisib
Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. |
| Vps34-IN-4
Vps34-IN-4 is a potent, selective, and orally active inhibitor of VPS34. |
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