PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.

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

WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).

OSI-027 (ASP4786) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. Phase 1.

DS-7423 is a dual PI3K and mTOR inhibitor, with IC50 values of 15.6 nM, 34.9 nM for PI3Kα and mTOR, respectively. DS-7423 possesses anti-tumor activity[1][2]. DS-7423 increases TP53 expression, the level of p-TP53 on Ser-46, and induced apoptosisrelated TP53 target genes (TP53AIP1 and PUMA) in OCCC cells[1].DS-7423 also inhibits other isoforms of class I PI3K (IC50 values: PI3Kβ = 1,143 nM; PI3Kγ = 249 nM; PI3Kδ = 262 nM)[2]. [1]. Katsutoshi Oda, et al. Characterization of TP53 and PI3K signaling pathways as molecular targets in gynecologic malignancies. J Obstet Gynaecol Res. 2016 Jul;42(7):757-62.[2]. Tomoko Kashiyama, et al. Antitumor activity and induction of TP53-dependent apoptosis toward ovarian clear cell adenocarcinoma by the dual PI3K/mTOR inhibitor DS-7423. PLoS One. 2014 Feb 4;9(2):e87220.

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].

FD2056 is a potent, orally active PI3K inhibitor, with IC50 values of 0.30, 0.80, 1.10, and 0.42 nM against PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. Additionally, it exhibits inhibitory effects on CDK2-CyclinA2 and CDK4-CyclinD3 with IC50s of 115.95 nM and 2782.15 nM. FD2056 effectively inhibits the proliferation of various breast cancer cell lines, such as MDA-MB-231, MDA-MB-468, and MCF-7, with IC50s of 1.06 μM, 0.04 μM, and 1.40 μM, respectively. The compound also promotes apoptosis in cancerous cells and has been shown to suppress tumor growth [1].

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)

PI3Kδ/γ-IN-2 is a potent, orally bioavailable dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 4.3 nM) with potential for use in anti-B-cell malignancy studies.

(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10;11(7):1463-1469.

PI3K/AKT-IN-1 is a potent, dual PI3K/AKT inhibitor that acts on PI3Kγ (IC50: 6.99 μM), PI3Kδ (IC50: 4.01 μM) and AKT (IC50: 3.36 μM). PI3K/AKT-IN-1 induces caspase 3-dependent apoptosis by inhibiting the PI3K/AKT pathway. caspase 3-dependent apoptosis and exhibited anticancer effects.

ATM Inhibitor-1 is a highly potent, selective and orally active ATM inhibito (IC50: 0.7 nM) anti-tumor activity. It shows weak activity against mTOR (IC50, 21 μM), DNAPK (IC50, 2.8 μM), PI3Kα (IC50, 3.8 μM), PI3Kβ (IC50, 10.3 μM), PI3Kγ (IC50, 3 μM) and PI3Kδ (IC50, 0.73 μM).

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).

PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1].

AZ2, a potent PI3Kγ inhibitor (pIC50 value: 9.3), is primarily utilized in the investigation of inflammatory and immune diseases[1].

NVS-PI3-4 is a highly selective inhibitor of the enzyme PI3Kγ. It is specifically designed for use in scientific investigations related to allergies, inflammatory conditions, and cancerous diseases[1][2].

FD2157, a photosensitive PI3K inhibitor, exhibits inhibitory IC50 values of 43 nM for PI3Kα, 83 nM for PI3Kβ, 84 nM for PI3Kγ, and 14 nM for PI3Kδ. Upon exposure to 365 nm UV light, FD2157 effectively inhibits cancer cell proliferation and induces apoptosis [1].

PI3Kδ-IN-12 (compound 13), a PI3Kδ inhibitor with a pIC50 of 5.8, exhibits differential binding affinities with pKi values of 8.0 for PI3Kδ, 6.5 for PI3Kγ, 6.4 for PI3Kβ, and 6.7 for PI3Kα. This compound is utilized in researching chronic respiratory conditions, including asthma and chronic obstructive pulmonary disease (COPD) [1].

PI3Kδ/γ-IN-3 (Compound 58) is an orally active dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 16 nM). PI3Kδ/γ-IN-3 can induce apoptosis of tumor cells, which can be used in the study of B-cell malignant tumors.