Idelalisib (CAL-101, GS-1101; trade name Zydelig), an approved anticancer drug, is a potent and selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; it has 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

GNE-317, an oxetane analog of GDC-0980, is a novel, potent, and selective PI3K/mTOR dual inhibitor with excellent BBB (blood-brain barrier) penetrating ability.

LY294002, a morpholine-containing compound designed based on the flavonoid quercetin, is a potent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively.

Brevianamide F is a novel and potent 2,5-diketopiperazines.

AS-604850 is a novel, potent, selective, and ATP-competitive inhibitor of PI3Kγ (phosphatidylinositol 3-kinase γ) with IC50 of 250 nM and a Ki of 180 nM.

PI3K/mTOR Inhibitor-2 is a novel and potent dual pan-PI3K/mTOR inhibitor with antitumor activity and with IC50 values of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR.

PIK-294 is a novel, potent and highly selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ (IC50 = 10 nM) with potential anticancer activity, showed 1000-, 49- and 16-fold less potency against PI3Kα/β/γ, respectively.

Tenalisib (also known as RP6530) is a new, potent and selective dual PI3Kδ/γ inhibitor with anticancer activity.

Quercetin, a naturally occuring polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects.

Eganelisib (IPI 549; IPI549; IPI-549) is a novel, potent and selective small molecule PI3Kγ (phosphoinositide-3-kinase) inhibitor with potential anticancer and immunomodulatory activity.