Dactolisib（BEZ235）是一种口服活性的双重抑制剂，对pan-class I PI3K和mTOR激酶的IC50值分别为4 nM、5 nM、7 nM和75 nM，对mTOR的IC50值为20.7 nM。Dactolisib抑制mTORC1和mTORC2。

Pictilisib（GDC-0941）是一种有效的PI3Kα/δ抑制剂，IC50为3 nM，对p110β（11倍）和p110γ（25倍）具有适度选择性。

LY294002 是一种 PI3K 抑制剂，抑制 PI3Kα, PI3Kδ 和 PI3Kβ 的 IC50 分别为 0.5, 0.57, 0.97 μM。LY294002 具有抗肿瘤作用，可用于研究 PI3K/AKT 信号通路和相关癌症治疗。

Idelalisib（CAL-101；GS-1101）是一种高度选择性且口服生物利用度的p110δ抑制剂，IC50为2.5 nM，相对于其他I类PI3K酶展示了40至300倍的选择性。

Buparlisib (BKM120; NVP-BKM120) 是一种泛 I 类 PI3K 抑制剂，对 p110α 的 IC50 为 52 nM，对 p110β 为 166 nM，对 p110δ 为 116 nM，对 p110γ 为 262 nM。

PI-103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. It blocks autophagic flux.

TGX-221 is a p110β-specific inhibitor with IC50 of 5 nM in a cell-free assay, and is 1000-fold selective for p110β than p110α.

IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay.

XL147 analogue is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ.

ZSTK474是一种 ATP 竞争性泛 I 类 PI3K 抑制剂，对 PI3Kα 的 IC50 为 16 nM，对 PI3Kβ 为 44 nM，对 PI3Kδ 为 4.6 nM，对 PI3Kγ 为 49 nM。

AS-605240 selectively inhibits PI3Kγ with IC50 of 8 nM, over 30-fold and 7.5-fold selective for PI3Kγ than PI3Kδ/β and PI3Kα in cell-free assays, respectively.

PIK-75 is a selective p110α inhibitor with IC50 of 5.8 nM with 200-fold more potently than p110β, and also potently inhibits DNA-PK with IC50 of 2 nM.

XL765 analogue is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM, and also inhibits DNA-PK and mTOR.

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

PIK-90 is a PI3Kα/γ/δ inhibitor with IC50 of 11 nM/18 nM/58 nM, respectively, less potent to PI3Kβ (IC50= 350 nM).

PF-04691502 is an ATP-competitive PI3K (α/β/δ/γ)/mTOR dual inhibitor with Ki of 1.8 nM/2.1 nM/1.6 nM/1.9 nM and 16 nM, little activity against either Vps34, AKT, PDK1, p70S6K, MEK, ERK, p38, or JNK.

AZD 6482(KIN-193) 是一种高效且选择性的p110β抑制剂，IC50为0.69 nM。

GSK1059615是一种可逆的PI3Kα/β/δ/γ抑制剂，也抑制mTOR，其IC50值分别为0.4 nM/0.6 nM/2 nM/5 nM和12 nM。

Duvelisib is a selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM, highly selective for PI3K δ/γ than other protein kinases.

TG100-115 is a PI3Kγ/δ inhibitor with IC50 of 83 nM/235 nM, with little effect on PI3Kα/β.