Application
PIK-294 has been used as PI3K inhibitor in drug combination studies and their synergy quantification using the Chou-Talalay method.
Biochem/physiol Actions
PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. For example, in a study of CXCL8-induced neutrophil migration, PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration whereas PI3Kγ inhibitor AS-605240 markedly reduced CXCL8 induced chemokinetic migration but had no effect on CXCL8 induced chemotactic migration.
PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ.
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | H2O: 10 mg/mL, clear,DMSO: 5 mg/mL, clear (warmed) |
| storage temp. | −20°C |
| SMILES string | NC1=C2C(N(CC(N3C4=C(C)C=CC=C4)=NC5=C(C(C)=CC=C5)C3=O)N=C2C6=CC(O)=CC=C6)=NC=N1 |
| InChI | 1S/C28H23N7O2/c1-16-7-3-4-12-21(16)35-22(32-20-11-5-8-17(2)23(20)28(35)37)14-34-27-24(26(29)30-15-31-27)25(33-34)18-9-6-10-19(36)13-18/h3-13,15,36H,14H2,1-2H3,(H2,29,30,31) |
| InChI key | WFSLJOPRIJSOJR-UHFFFAOYSA-N |
