Description
PIK-90 can inhibit PI3Kalpha, PI3Kbeta, PI3Kdelta and PI3Kgamma with IC50 of 11 nM, 350 nM, 58 nM and 18 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C18H17N5O3
Solubility
DSMO 0.28 mg/mL Water
In vitro
PIK-90 is unique in their potencies for inhibiting PI3Kgamma in vitro.Treatment of dHL60 cells with PIK-90 impairs consolidation and stability of the leading edge formed after treatment with uniform fMLP(chemoattractants like f-Met-Leu-Phe). PIK-90 is a potnet PI3K-alpha inhibitor and can potently block phosphorylation of Akt.PIK-90 induced a modest G0/G1 arrestat a concentration of 0.5 uM sufficient to inhibit phosphorylation of Akt substantially. PIK-90 is a potent inducer of CLL cell apoptosis. In chronic lymphocytic leukemia (CLL), PI-103 can induce a significant reduction of chemotaxis and actin polymerization to CXCL12 and reduced migration beneath marrow stromal cells by inhibiting phosphorylation of Akt and S6.
In vivo
PIK-90 can significant increase in IgG1/IgE double-positive cells and lead to markedly enhanced B-cell switch to IgE by inhibiting PI3K in vivo. In human glioblastoma xenografts, PIK-90 and Roscovitine, in combination, can acted in a synthetic-lethal manner to induce apoptosis.
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