PIK-293 (IC87114), the parent compound of PIK-294, is a novel, potent, and the first isoform-selective PI3K (phosphatidylinositol 3-kinase) inhibitor with with potential anticancer activity.

Dactolisib (formerly also known as NVP-BEZ235; BEZ235; BEZ-235) is a novel, potent and dual ATP-competitive inhibitor of PI3K (phosphatidylinositol 3-kinase) and mTOR for p110α/γ/δ/β and mTOR(p70S6K) with anticancer activity.

CZ415 is a potent, cell-permeable (Kd app = 6.9 nM), and ATP-competitive mTOR inhibitor with high selectivity over any other kinase (IC50 = 14.5 nM IC50 for pS6RP and 14.8 nM for pAKT) and very good pharmacokinetic properties which include moderate clearance and good oral bioavailability.

Pilaralisib analog (XL-147 analog, SAR-245408) is novel, selective, potent, orally bioavailable and reversible small molecule inhibitor of Class 1 PI3K (phosphatidylinositol 3 kinase) family of kinases with potential anticancer activity.

AMG-511 is a potent and selective pan class I PI3K inhibitor exhibiting IC50 of 8, 11, 2, and 6 nM against the PI3K β, α, β, and ≤ isoforms respectively.

BKM120 (also known as NVP-BKM120, or Buparlisib) is a selective, orally bioavailable and potent Pan-class I PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively.

AS041164 is a novel and potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM).

MLS2052 (also known as BIO, GSK3 Inhibitor IX, 6-Bromoindirubin-3′-oxime) is a novel, potent, cell-permeable bis-indolo and specific inhibitor of GSK-3 (glycogen synthase kinase-3) with potential antitumor activity.

Taselisib (formerly also known as GDC-0032 or RG-7606), an imidazobenzoxazepin compound, is a novel and potent β-sparing small molecule inhibitor of PI3K with Ki values of 0.29 nM, 0.91 nM, 0.97 nM for PI3Kα, PI3Kβ and PI3Kγ, respectively.

Pilaralisib (formerly XL-147; SAR-245408) is a novel, potent, orally bioavailable, ATP-competitive, selective and reversible inhibitor of class I PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity.