NVP-BKM120, PI3K Inhibitor BKM120

Bioss

NVP-BKM120, PI3K Inhibitor BKM120

16

Research Use Only

98.0

BKM120 (NVP-BKM120) is a potent and selective, orally available pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. It inhibits all four class-I PI3K isoforms in biochemical assays with IC50 ~50-250 nM, but exhibits selectivity of >100 folds against other protein kinases. It is also active against the most common somatic PI3Ka mutations but does not significantly inhibit the related class-III (Vps34) and class-IV (mTOR, DNA-PK) PI3K kinases. BKM120 has shown to significantly inhibit cell growth and induce apoptosis in a variety of tumor cell lines as well as in animal models. Consistent with its mechanism of action, NVP-BKM120 decreases the cellular levels of p-Akt in relevant models, as well as modulates downstream effectors in a concentration dependent and pathway-specific manner.

-20°C

51202000