phosphatidylinositol 3-kinase

Psoralidin inhibits Akt phosphorylation and phosphatidylinositol 3-kinase activation and transcriptionally. Psoralidin possesses anticancer and chemopreventive properties.

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer.

PI3-Kinase inhibitor targets PI3Kγ with an IC50 of 1.5 nM and shows selectivity over PI3Kα, PI3Kβ, and PI3Kδ, exhibiting IC50 values of 3,333 nM, >10,000 nM, and >1,000 nM, respectively. At 100 mg/kg, it reduces tumor growth in a 4T1 murine mammary cancer model. In a mouse model of experimental autoimmune encephalomyelitis (EAE), it lessens disease severity when administered at doses of 20 or 80 mg/kg.

WAY-299017 is a potent and selective UPPS inhibitor for the treatment of bacterial infections.

Duvelisib (INK1197, IPI-145) is a selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and p100δ, with effects on p110δ (IC50 value is 0.0025 μM), p110γ (IC50 value is 0.274 μM), p110β (IC50 value is 0.85 μM) and p110α (IC50 value is 1.602 μM).

mTOR inhibitor 9b is an enzyme inhibitor of protein kinase mTOR he phosphatidylinositol 3-kinase PIK3CA with IC50s of 0.76 nm and 1.262 µM, respectively.mTOR inhibitor 9b possesses anticancer activity and can be used to study leukemia, skin, breast, lung and colon cancers.

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.

PI4KIIIbeta-IN-9 is a potent inhibitor of PI4KIIIβ [IC50 of 7 nM].

Zandelisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K)(p110δ, IC50 of 3.5 nM), and with antineoplastic activity.

PI-828 is a phosphatidylinositol 3-kinase (PI3K) inhibitor, which is widely used to study the physiological function of PI3K and also promotes stem cell differentiation into mesoderm.

Omipalisib (GSK2126458) is a small-molecule pyridylsulfonamide inhibitor of phosphatidylinositol 3-kinase (PI3K) with potential antineoplastic activity.

GSK-F1 (PI4KA inhibitor-F1) is a novel potent PI4KA inhibitor.

Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.

PIKfyve-IN-4 (Compound 40) is an orally active and selective phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) inhibitor, with an IC50 of 0.60 nM, and demonstrates good systemic tolerability.

PI3K-IN-56 (Compound 1) is an orally active, potent, and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K). It irreversibly blocks the production of phosphatidylinositol-3,4,5-trisphosphate (PIP3) and the downstream AKT signaling pathway. PI3K-IN-56 holds promise for research in PI3Kα-driven cancers, such as breast and ovarian cancer.

Antimalarial agent 41 (Compound 17) exhibits antimalarial activity by inhibiting the malaria parasite Plasmodium falciparum, with IC50 values of 40 nM for NF54 strain and 76 nM for K1 strain. This compound acts as an inhibitor of P. falciparum phosphatidylinositol-4-kinase β (PfPI4K) and hERG channels, with IC50 values of 53 nM and 3 μM, respectively. Additionally, Antimalarial agent 41 shows cytotoxicity against CHO cells, with an IC50 of 34 μM. It can improve malaria infections and demonstrates favorable pharmacokinetic properties in mouse models.

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

PIK-93, the first potent synthetic PI4K inhibitor, exhibits an IC50 of 19 nM and also inhibits PI3Kα with an IC50 of 39 nM.

Dezapelisib is an orally bioavailable, selective inhibitor of the delta isoform of the 110 kDa catalytic subunit of class I phosphoinositide-3 kinases (PI3K). INCB040093 prevents both the production of the second messenger phosphatidylinositol-3,4,5-trisp

Halenaquinone is a phosphatidylinositol 3-kinase inhibitor. Halenaquinone specifically inhibits the secondary DNA binding of RAD51. Halenaquinone inhibits RANKL-induced osteoclastogenesis. Halenaquinone induces apoptosis in PC12 cells.

PIK-108 is an allosteric inhibitor of phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunits β and δ (PI3Kβ/δ).

RV-1729, a phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) inhibitor, is used potentially for the treatment of asthma.

WJD008 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin. WJD008 prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant. WJD008 has antiproliferative and anticlonogeni