PI3Kγ inhibitor 7 (compound 2) is a potent and orally active PI3Kγ inhibitor with IC50 values of 4768, 878.1, 3.42, 355.2 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively. PI3Kγ inhibitor 7 shows antitumor activity[1].
IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer[1].
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity[1].
PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC50 values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC50 values of 4.0/<3.7/5.0/<4.1, respectively[1].
MSC2360844 is a potent, orally active and selective PI3Kδ inhibitor, with an IC50 of 145 nM. MSC2360844 shows highly selective against a panel of 278 additional kinases[1].
Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM[1].
3-Methyladenine is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
ACT001 is an orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of DMAMCL (a prodrug of Micheliolide), can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects[1][2].
CYH33 (CYH-33) is a novel potent, PI3Kα-selective inhibitor with IC50 of 5.9 nM/598 nM/ 78.7 nM/225 nM aginst class I PI3K isoform α/β/δ/γ, respectively; also displays little to no activity against more than 300 kinases; inhibits PI3K/AKT/mTOR signaling in glioblastoma U87MG and rhabdomyosarcoma Rh30 cells, shows potent anti-proliferative activity in against cell proliferation in a panel cancer cell lines originated from breast, lung, ovary and colon, prostate etc.; shows significant efficacy to inhibit the growth of SKOV-3 xenograft. Solid Tumors Phase 1 Clinical
Flupentixol is a high potency thioxanthene with D1 and D2 dopamine receptor antagonism. Flupentixol is used in therapy of schizophrenia as well as in anxiolytic and depressive disorders[1][2].
Quercetin hydrate, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
Arnicolide D is a sesquiterpene lactone isolated from Centipeda minima. Arnicolide D modulates the cell cycle, activates the caspase signaling pathway and inhibits the PI3K/AKT/mTOR and STAT3 signaling pathways. Arnicolide D inhibits Nasopharyngeal carcinoma (NPC) cell viability in a concentration- and time-dependent manner[1].
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases[1].
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively[1].
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth[1].
PI3K-IN-36 (compound A36) is a potent PI3K inhibitor. PI3K-IN-36 can be used in research of follicular lymphoma (FL)[1].
CGS 15943 is an adenosine A2 receptor antagonist and reduces stroke injury in the Mongolian gerbil[1]. CGS 15943 is a selectively p110γ inhibitor with an IC50 of 1.1 μM, shows inhibitory effect on p110δ (IC50=8.47 μM), has an anti-carcinogenic effect on HCC and PDAC cells[2].
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research[1].
Zandelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor extracted from patent WO2019183226 A1, Compound Example 1. Zandelisib selectively inhibits p110δ with an IC50 of 3.5 nM. Zandelisib functions as an antineoplastic[1][2].
3-Methyladenine-d3 is the deuterium labeled 3-Methyladenine[1]. 3-Methyladenine (3-MA) is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K[2].
Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively[1].
PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC50s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively[1]. Antitumor activity[1].
YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.
PI3Kγ inhibitor 6 (compound 9) is a PI3Kγ inhibitor. PI3Kγ inhibitor 6 can be used for the research of inflammatory and autoimmune diseases[1].
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway[1]. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro[2].
PI3KC2α-IN-2 is a potent and selective PI3KC2α inhibitor (IC50: 121 nM). PI3KC2α-IN-2 interacts with the ATP-binding site of PI3KC2α.. PI3KC2α-IN-2 can be used in the research of thrombosis, diabetes and cancers[1].
NVP-BBD130 is a potent, stable, ATP-competitive and orally active dual PI3K and mTOR inhibitor[1].
4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis[1][2][3].