Linperlisib (YY20394; PI3Kδ-IN-2)is a novel, potent, orally bioavailable, and highly selective PI3Kδ inhibitor that was being investigated in a phase I trial for patients with relapse or refractory B-cell malignancies.

GDC-0084 (Paxalisib; RG7666) is a novel, potent and brain penetrant inhibitor of phosphatidylinositol 3-kinase (PI3K) and mTOR with potential antineoplastic activity.

Wortmannin (SL2052; KY12420), a steroid metabolite of the fungi Penicillium funiculosum, is the first described, potent selective and irreversible PI3K inhibitor with potential anticancer activity.

Voxtalisib analogue (also known as PI3K-IN-1, SAR-245409 Analog, XL-765 Analog), a Voxtalisib derivative, is a novel, potent and orally bioavailable dual inhibitor of mTOR/PI3K with potential anticancer activity.

Umbralisib (formerly TGR-1202; RP-5264; TGR1202; RP5264; Ukoniq) is a novel, highly specific, orally bioavailable and potent PI3Kδ inhibitor approved in 2021 by FDA to treat marginal zone lymphoma and follicular lymphoma.

3-Methyladenine (also called 3-MA; Autophagy Inhibitor) is a novel, potent, cell-permeable and selective PI3K inhibitor.

Nemiralisib (GSK-2269557) is a novel, potent and selective PI3Kδ inhibitor with pKi of 9.9.

PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity.

Apitolisib (formerly also known as GDC0980, RG7422, GNE390) is a novel, potent, selective and orally bioavailable class I PI3K inhibitor with potential anticancer activity.

Voxtalisib (also known as SAR245409, XL765) is a potent, orally bioavailable small molecule and dual inhibitor of mTOR/PI3K (mammalian target of rapamycin/phosphatidylinositol 3 kinase) with anticancer activity.