CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer[1][2].
SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM.
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest[1].
SRX3177 is a potent, triple BRD4/PI3K/CDK4/6 inhibitor with nanomolar potency against PI3Kα (IC50=79 nM), BRD4 bromodomains (BD1 and BD2) (IC50=33 nM and 89 nM, respectively), and CDK4/6 (IC50=2.5/3.3 nM).SRX3177 is capable of targeting BRD4, PI3K and CDK4/6 simultaneously, induces apoptosis and cell cycle arrest and has in vitro efficacy in mantle cell lymphoma, hepatocellular carcinoma and neuroblastoma models.SRX3177 has antitumor efficacy in in vivo xenograft models and is less toxic than the combination of agents that inhibit individual targets.
PI3Kδ/γ-IN-3 (Compound 58) is a potent and orally active PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 16 nM, respectively. PI3Kδ/γ-IN-3 induces tumor cell apoptosis and can be used for B-cell malignancies research[1].
(+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity[1].
PI3Kδ-IN-13 (compound 89) is a PI3Kδ inhibitor (IC50=2.6 nM). PI3Kδ-IN-13 can be used in the research of cell proliferation diseases such as cancer, infection, inflammation and autoimmune diseases[1].
Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
PI3Kδ-IN-9 is a selective PI3Kδ inhibitor with an IC50 value of 3.8 nM.
GSK2292767 is a potent and selective inhibitor of PI3Kδ, with a pIC50 of 10.1. GSK2292767 showing greater than 500-fold selective over the other PI3K isoforms. GSK2292767 can be used for the research of respiratory disease[1].
PI3Kδ-IN-3 (Compound 11) is a PI3Kδ inhibitor (IC50: 9 nM). PI3Kδ-IN-3 inhibits B cell function. PI3Kδ-IN-3 has good pharmacokinetic properties[1].
1-Deoxynojirimycin hydrochloride (Duvoglustat hydrochloride) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin hydrochloride suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin hydrochloride possesses antihyperglycemic, anti-obesity, and antiviral features[1][2].
Taxamairin B is a potent anti-inflammatory agent. Taxamairin B decreases proinflammatory cytokines (TNF-α, IL-1β and IL-6) expression and the production of NO and ROS in LPS-induced RAW264.7 cells. Taxamairin B exhibits significantprotective effects in LPS-induced acute lung injury in mice[1][2].
DS-7423 is a novel potent, small-molecule dual inhibitor of PI3K/mTOR with IC50 of 15.6, 1143, 249, 262 and 34.9 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR respectively; exerts anti-tumor effect against a panel of nine OCCA cell lines with IC50 of <75 nM, regardless of the mutational status of PIK3CA; suppresses the tumor growth of OCCA in a dose-dependent manner in mouse xenograft models. Solid Tumors Phase 1 Discontinued
Heterophyllin B is an active cyclic peptide isolated from Pseudostellaria heterophylla. Heterophyllin B provides a novel strategy for the treatment of esophageal cancer[1].
Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT[1].Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells[2].
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research[1].
GS-9901 is a highly selective and orally active PI3Kδ inhibitor, with an IC50 of 1 nM. Has potential to treat rheumatoid arthritis[1].
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC50 values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC50 values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity [1].
Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ)[1][2].
Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach[1][2][3][4].
PI3K/mTOR Inhibitor-6 (Compound 19c) is a potent and dual inhibitor of PI3K/mTOR. PI3K/mTOR Inhibitor-6 displays better stability in artificial gastric fluids than gedatolisib. PI3K/mTOR Inhibitor-6 significantly suppresses the PI3K/Akt/mTOR signaling pathway at 10 μM. PI3K/mTOR Inhibitor-6 has the potential for the research of cancer diseases[1].
Viridin is a secondary metabolite and naturally occurring furanosteroid. Viridin is potent inhibitor of the lipid kinase PI3K[1][2].
PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1].
NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
Wortmannin is a multi-target inhibitor of PI3K and MLCK with IC50s of 3 nM and 200 nM, respectively. Wortmannin is also a potent inhibitor of DNA-PK (IC50, 16 nM) and ATM (IC50, 150 nM). Wortmannin is also a potent inhibitor of Polo-like kinase (Plk).
PP30, a TORKinib, is a potent, selective, and ATP-competitive inhibitor of mTOR with an IC50 of 80 nM.
Mytoxin B is an ADC cytotoxin. Mytoxin B is a satratoxin-type trichothecene macrolide and is similar to the effect of LY294002 (HY-10108). Mytoxin B induces cell apoptosis via PI3K/Akt pathway[1].
PI3K-IN-35 (Compound 6l) is a highly selective PI3K inhibitor with IC50 values of 13.98, 7.22 and 10.94 μM for PI3K-α、PI3K-β and PI3K-δ, respectively. PI3K-IN-35 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-35 can be used in leukemia research[1].
α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer[1].