3-Methyladenine (3-MA) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM.

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.

A novel specific p110β inhibitor with IC50 of 5.74 nM.

A novel VPS34 inhibitor.

A novel, potent, and selective p110δ PI3K inhibitor with IC50 of 0.1 nM in cell-based assays.

A potent, selective, orally bioavailable PI3Kδ inhibitor with IC50 of 2.6 nM.

A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.

Acalisib (GS-9820) is a potent and selective inhibitor of PI3Kδ with IC50 value of 12.7 nM.

AMG 319 is an investigational, highly selective, small molecule inhibitor of PI3Kδ that blocks B cell proliferation following BCR stimulation both in vitro and in vivo, inhibits basal AKT phosphorylation, and inhibits proliferation in lymphoid tumor cells

AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). AS-605240 displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα.

Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

AZD6482 is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ.

AZD8186 is an inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

AZD8835 ia a novel mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).

BAY 1082439 is a highly selective and balanced PI3Kα/β inhibitor demonstrated potent activity in tumors with activated PI3Kα and loss-of-function of PTEN.

BEBT-908（CUDC-908）is a novel PI3K/HDAC inhibitor.

BEZ235 (NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively, and also inhibits ATR with IC50 of 21 nM.

BKM120 is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ.

CAL-101 is a selective p110δ inhibitor with IC50 of 2.5 nM; shown to have 40- to 300-fold greater selectivity for p110δ thanp110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR.

Desmethyl VS-5584 is a PI3K/mTOR kinase inhibitor

ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).

GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.