pi3k in 1

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

EGFR/PI3Kα-IN-1 (compound 30k), a dual EGFR/PI3Kα inhibitor, exhibits potent activity with IC 50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα). It effectively inhibits tumor cell proliferation and demonstrates significant anticancer activity.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR, with 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.

PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K and HDAC, with IC50 values of 8.1 nM and 1.4 nM, respectively.

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active dual inhibitor of PI3Kδ and HDAC6, with IC50 values of 2.4 nM and 6.2 nM, respectively. It exhibits potent antiproliferative effects against non-Hodgkin's lymphoma (NHL) cells and demonstrates antitumor activity in vivo without significant toxicity. PI3Kδ/HDAC6-IN-1 induces cell cycle arrest at the G0/G1 phase and triggers apoptosis. Additionally, it inhibits the PI3K/AKT/mTOR signaling pathway and enhances the acetylation levels of α-tubulin and histone H3.

PI3K/AKT-IN-1 is a dual PI3K and AKT inhibitor with anti-cancer activity. It inhibits PI3Kγ, PI3Kδ, and AKT, suppressing the PI3K/AKT pathway and inducing caspase 3-dependent apoptosis, suitable for cancer research.

PI3K/Akt/CREB activator 1 (AE-18) is a selective inducible nitric oxide synthase (iNOS) inhibitor that crosses the blood-brain barrier, reduces infarct size and restores blood supply deficits after ischemia-reperfusion in rats, and is used in studies of vascular dementia and Parkinson's disease.

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting PI3K (IC50: 2.21 μM) and VEGFR2 (IC50: 68 μM), which induces apoptosis and is utilized in cancer research [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-IN-1 is an efficacious PI3Kδ inhibitor (IC50 of 1.7 nM).

PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).

PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.

PI3Kγ ligand 1 serves as a PROTAC target protein ligand (Ligand for Target Protein for PROTAC).

PI3Kδ/BET-IN-1 (compound 10b) exhibits excellent and balanced activity against PI3Kδ (IC50= 112 nM) and BRD4-BD1 (IC50= 19 nM), while also demonstrating strong antiproliferative effects in DLBCL cells.

PROTACPI3K/110β degrader-1 (J-9) acts as a PROTAC degrader specifically targeting PI3K/110β.

PI3KαLigand-1 is a ligand for PI3Kα, and it is useful for synthesizing PROTACs, such as PROTAC PI3Kα degrader-1.

PROTACPI3Kα degrader-1 is a PI3Kα-targeting PROTAC degrader (DC50= 0.08 μM) that demonstrates notable selectivity in degrading PI3Kα over the PI3Kβ, PI3Kγ, and PI3Kδ isoforms. It degrades PI3Kα effectively in a time- and concentration-dependent manner and significantly inhibits the phosphorylation of AKT at the Ser473 site. Additionally, PROTACPI3Kα degrader-1 exhibits significant in vivo anticancer efficacy in HGC-27 and DOHH2 xenograft models.

PROTACPI3Kδ degrader-1 is a covalent PI3Kδ-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). Additionally, PROTACPI3Kδ degrader-1 effectively degrades p-AKT, induces cell cycle arrest in the G1 phase, and promotes apoptosis and autophagy. It also significantly suppresses tumor growth in the SU-DHL-6 xenograft mouse model.

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

PI3Kβ-IN-1 is a selective, orally active PI3Kβ inhibitor (IC50: 2 nM).

PI3Kδ/γ-IN-1 is a selective and efficacious inhibitor of PI3Kδ/γ, suitable for treating hematologic malignancies.

PI3Kα/HDAC6-IN-1 (compound 21j) is a dual inhibitor of PI3Kα and HDAC6, with IC50 values of 2.9 nM and 26 nM, respectively. It hinders AKT(Ser473) phosphorylation and promotes the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. The compound exhibits potent anti-cancer efficacy, inhibiting the L-363 cell line with an IC50 of 0.17 μM [1].