PI3K-IN-38 is an orally available and potent PI3K inhibitor with an IC50 value of 0.541 µM for PI3K-α. PI3K-IN-38 exhibits anticancer and anti-inflammatory activity and inhibits tumor growth in vivo.

PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 12.5 nM and 10.6 nM for mTOR and PI3Kα in a cell free assay , respectively.

PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function.

PI3K/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor.PI3K/Akt/mTOR-IN-2 has anticancer effects and is selective for MDA-MB-231 cells with an IC50 of 2.29 μM.PI3K/Akt/mTOR-IN-2 exhibits anticancer activity and induces cycle arrest and apoptosis in cancer cells. PI3K/Akt/mTOR-IN-2 has anticancer activity and can induce cycle arrest and apoptosis in cancer cells.

PI3K/mTOR Inhibitor-14 (compound Y-2) serves as a dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 171.4 nM and 10.1 nM , respectively, and demonstrates antitumor activities [1].

PI3Kδ-IN-17 (Compound S5) is a potent PI3K δ inhibitor, exhibiting an IC50 value of 2.82 nM and demonstrates significant efficacy in suppressing the proliferation of SU-DHL-6 cells with an IC50 of 0.035 μM [1].

PI3K-IN-46 is a specific inhibitor of PI3Kγ.

PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in cell cycle arrest at the G1 phase and apoptosis in U87-MG cells. Additionally, it demonstrates significant antiproliferative effects against various tumor cell lines, including PC-3 with an IC50 of 0.28 μM, HCT-116 with an IC50 of 0.57 μM, and U87-MG with an IC50 of 1.37 μM [1].

Se15, a selective PI3Kδ inhibitor, exhibits potency with an IC50 value of less than 0.1nM and is utilized in autoimmune research [1].

PI3Kδ-IN-15 (compound 6b) is a potent and selective inhibitor of PI3Kδ, exhibiting an IC50 of 0.5 nM for p110δ and demonstrating over 30-fold selectivity compared to PI3K isoforms γ, β, and α [1].

PI3K-IN-41 (compound 2), a photocaged PI3K inhibitor (IC50=18.92 nM) with anticancer properties, demonstrates potent PI3K inhibition following UV light irradiation and has been shown to enhance antitumor effects [1]. This compound has potential for use in precisely controlled cancer therapeutics.

PI3K-IN-47 (Compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (PI3K) family, exhibiting inhibitory concentration (IC50) values of 0.44 nM for PI3Kα, and 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ respectively. It is effective in inducing G1 phase cell cycle arrest, and exhibits anti-neoplastic properties by restraining colony formation and cell migration. Additionally, PI3K-IN-47 has demonstrated the ability to suppress tumor growth in HGC-27 xenograft mouse models [1].

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM)

PI3K-IN-35 (Compound 6l) is a highly selective inhibitor of PI3K, acting on PI3K-α (IC50: 13.98 μM), PI3K-β (IC50: 7.22 μM) and PI3K-δ (IC50: 10.94 μM). PI3K-IN-35 blocks the cell cycle in G2/M phase and induces apoptosis. PI3K-IN-35 can be used to study leukaemia.

PI3K/AKT-IN-2, a dual inhibitor of PI3K and AKT, prevents the epithelial-mesenchymal transition (EMT) and promotes apoptosis. Additionally, it impedes tubulin polymerization.

PI3K/mTOR Inhibitor-12, a potent and selective orally active inhibitor, exhibits IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR, indicating significant antitumor activity with reduced liver toxicity [1].

PI3K/mTOR Inhibitor-7 is a potent dual PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-7 is 4.7-fold more potent than gedatolisib, with IC50 values of 1.4 μM and 0.3 μM, respectively. 10 μM of PI3K/mTOR Inhibitor-7 is able to significantly inhibit the PI3K/Akt/mTOR signalling pathway. PI3K/mTOR Inhibitor-7 has shown potential for research in cancer diseases.

PI3K/Akt-IN-C89 is a novel Inhibitor of the PI3K-Akt Pathway, Inducing Autophagy of Female Germline Stem Cells.

MEK/PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ). This compound effectively reduces pAKT and pERK1/2 levels, exhibiting anti-proliferative activity against various tumor cell lines [1].

PI3K-IN-22 is a dual kinase inhibitor of PI3Kα and mTOR, with IC50s of 0.9 and 0.6 nM respectively. PI3K-IN-22 could be used in cancer.

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor, capable of acting on PI3Kα (IC50: 226 nM), PI3Kβ (IC50: 279 nM), PI3Kγ (IC50: 467 nM), PI3Kδ (IC50: 29 nM), HDAC1 (IC50: 1.3 nM), and PI3K/HDAC-IN-2 is PI3Kδ and class I and IIb HDAC selective and exhibits significant anticancer effects.

PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibitory effects on PI3K and mTOR. This compound exhibits notable anti-cancer activity [1].

PI3K/mTOR Inhibitor-4 is an orally active pan-I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 is an enzyme inhibitor that acts on PI3Kα (IC50: 0.63 nM), PI3Kγ (IC50: 22 nM), PI3Kδ (IC50: 9.2 nM) and mTOR (IC50: 13.85 nM). PI3K/mTOR Inhibitor-4 can be used to study cancer.

PI3K-IN-30 (compound 6d) is a potent inhibitor of PI3K, acting on PI3Kα (IC50: 5.1 nM), PI3Kβ (IC50: 136 nM), PI3Kγ (IC50: 30.7 nM) and PI3Kδ (IC50: 8.9 nM).

PI3K/Akt/CREB Activator 1 is a potent, orally active compound that acts as an activator for the PI3K/Akt/CREB pathway. It enhances neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like morphology, and accelerates axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. This compound is utilized in vascular dementia (VaD) research.

PI3K-IN-9 is a potent and selective inhibitor of PI3Kδ(IC50 of 8.9 nM).

PI3K-IN-6 is an oral active and highly selective inhibitor of phosphoinositide 3-kinase (PI3K) β/δ(IC50 values of 7.8 nM/5.3 nM , respectively).

PI3K-IN-2 are orally active PI3Kβ/δ inhibitors with IC50 values of 7.1 nM, 8.6 nM, and higher selectivity than PI3Kσ (IC50: 13 nM) and PI3Kγ (IC50: 190 nM), respectively.

PI3K-IN-1 (Voxtalisib Analogue) is a dual inhibitor of mTOR/PI3K, mostly for p110γ , also inhibits DNA-PK and mTOR.

COX-2/PI3K-IN-2 (compound 5f) has properties of anti-inflammatory and anti-cancer. COX-2/PI3K-IN-2 is a selective inhibitor of COX-2 (Ki = 3.02 nM) as well as a potent inhibitor of PI3K (IC 50 = 2.78 nM) [1].

PI3Kδ-IN-14 (Compound (S)-29), a selective PI3Kδ inhibitor with an IC50 of 0.8 nM and a Kd of 84.8 nM, targets the ATP-binding site within the kinase domain of PI3Kδ. This compound exhibits anti-inflammatory properties by impeding the PI3K/AKT pathway and is noted for alleviating acute lung injury (ALI) [1].

IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ/δ dual inhibitor, demonstrating oral activity, with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ. This compound inhibits AKT phosphorylation and promotes tumor regression through the recruitment and activation of CD8+ T cells. It is utilized in cancer research [1].

PI3Kγ Inhibitor 7 (compound 2) is a potent, orally active agent that selectively inhibits PI3Kγ with an IC50 of 3.42 nM and demonstrates antitumor activity [1]. It also exhibits varying inhibitory effects on other PI3K isoforms, with IC50 values of 4768 nM for PI3Kα, 878.1 nM for PI3Kβ, and 355.2 nM for PI3Kδ.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent inhibitor of both mTOR and PI3K, acting on mTOR (IC50: 38 nM), PI3Kα (IC50: 6.6 nM), PI3Kγ (IC50: 6.6 nM) and PI3Kδ (IC50: 0.8 nM).

PI3K/mTOR Inhibitor-13, an orally active dual inhibitor targeting phosphoinositol 3-kinase (PI3K) and mTOR kinase, holds potential for treating sexual diseases, solid tumors, and idiopathic pulmonary fibrosis (IPF).

PI3K-IN-36 is a potent inhibitor of PI3K, suitable for research applications in follicular lymphoma (FL).

PI3K-IN-23 is a (E)-9-oxooctadec-10-en-12-ynoic acid analogue that promotes glucose uptake (EC50: 7.00 μM).

PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent dual PI3K/mTOR inhibitor that is more stable than gedatolisib in artificial gastric fluid. 10 μM of PI3K/mTOR Inhibitor-6 significantly inhibits the PI3K/Akt/mTOR signalling pathway. PI3K/mTOR Inhibitor-6 has shown potential for research in cancer diseases.

PI3K-IN-33 is a highly selective PI3K inhibitor that acts on PI3K-α (IC50: 11.73 μM), PI3K-β (IC50: 6.09 μM) and PI3K-δ (IC50: 11.18 μM). PI3K-IN-33 is capable of blocking the cell cycle in G2/M phase and can induce apoptosis and can be for the study of leukemia.

PI3Kδ-IN-11 is a potent and selective PI3Kδ inhibitor (IC50: 27.5 nM) that dose-dependently blocks PI3K/Akt pathway activity. PI3Kδ-IN-11 can be used in B- or T-cell-associated malignancy studies.

PARP/PI3K-IN-1 is a novel dual poly (ADP-ribose) polymerase (PARP) and phosphatidylinositol 3-kinase (PI3K) dual inhibitor with anticancer, antitumour and antiproliferative activities for the study of breast, pancreatic and lung cancers.

PI3K-IN-10 is a potent inhibitor of pan-PI3K .

PI3K-IN-27 is a potent inhibitor of PI3K, a large family of lipid signalling kinases that play a key role in cellular processes such as cell growth, differentiation, migration and apoptosis. PI3K-IN-27 has shown research potential in hyperproliferative diseases such as cancer and inflammation or in immune and autoimmune diseases.

PI3K-IN-19 hydrochloride (WO2017153220, step 5) acts as a phosphatidylinositol-3-kinase (PI3K) inhibitor.

PI3K inhibitor C 96 is an inhibitor of phosphatidylinositol 3-kinase. It shows effective activity against multiple myeloma in vitro and in vivo.

PI3K/mTOR Inhibitor-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16,1 and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR. PI3K/mTOR Inhibitor-2 has antitumor activity.

Selective PI3Kδ Inhibitor 1 is a PI3Kδ Inhibitor( IC50 = 0.9 nM).

PI3K-IN-31 (Compound 6b) is a potent inhibitor of PI3K that acts on PI3Kα (IC50: 3.7 nM), PI3Kβ (IC50: 74 nM), PI3Kγ (IC50: 14.6 nM) and PI3Kδ (IC50: 9.9 nM). PI3K-IN-31 has shown anticancer activity. PI3K-IN-31 showed anti-cancer activity.

PI3K-IN-48, a PI3K inhibitor, exhibits an IC50 of 1.55 ± 0.18 μM in A549 cells, demonstrating its potency in this context. It induces G0/G1 phase arrest and cell apoptosis, while also down-regulating the expression of p-PI3K and p-Akt. This compound is relevant for research into the treatment of human lung cancers [1].