pi3kδ

PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.

PI3Kδ-IN-3 (TC KHNS 11) is a PI3Kδ inhibitor with an IC50 value of 9 nM.PI3Kδ-IN-3 has a favorable pharmacokinetic profile and inhibits B cell function.

PI3K/mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibitory effects on PI3K and mTOR. This compound exhibits notable anti-cancer activity [1].

PI3K/Akt/mTOR-IN-3 is a potent inhibitor of PI3K/Akt/mTOR. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 cells (IC50: 0.77 μM), HeLa cells (IC50: 1.23 μM) and HepG2 cells (IC50: 4.57 μM). PI3K/Akt/mTOR-IN-3 inhibited the migration of MCF-7 and HeLa cells at a concentration of 4 μM. PI3K/Akt/mTOR-IN-3 blocked the cell cycle in S phase and induced apoptosis.

PI3Kδ-IN-17 (Compound S5) is a potent PI3K δ inhibitor, exhibiting an IC50 value of 2.82 nM and demonstrates significant efficacy in suppressing the proliferation of SU-DHL-6 cells with an IC50 of 0.035 μM [1].

Se15, a selective PI3Kδ inhibitor, exhibits potency with an IC50 value of less than 0.1nM and is utilized in autoimmune research [1].

PI3K-IN-38 is an orally available and potent PI3K inhibitor with an IC50 value of 0.541 µM for PI3K-α. PI3K-IN-38 exhibits anticancer and anti-inflammatory activity and inhibits tumor growth in vivo.

PI3Kα/mTOR-IN-1 is a potent dual inhibitor of PI3Kα/mTOR. PI3Kα/mTOR-IN-1 shows 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/Akt/mTOR-IN-2 is a potent PI3K/AKT/mTOR inhibitor.PI3K/Akt/mTOR-IN-2 has anticancer effects and is selective for MDA-MB-231 cells with an IC50 of 2.29 μM.PI3K/Akt/mTOR-IN-2 exhibits anticancer activity and induces cycle arrest and apoptosis in cancer cells. PI3K/Akt/mTOR-IN-2 has anticancer activity and can induce cycle arrest and apoptosis in cancer cells.

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.

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

PI3Kδ/γ-IN-1 is a selective and effective inhibitor of PI3Kδ/γ that can be used in the treatment of hematologic malignancies.

IHMT-PI3Kδ-372 is a selective inhibitor of PI3Kδ with an IC50 of 14 nM and can be used in studies about chronic obstructive pulmonary disease.

PI3Kδ-IN-9 is a selective PI3Kδ inhibitor with an IC 50 value of 3.8 nM.

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-IN-10 is a highly potent and orally active PI3Kδ inhibitor (IC50= 2 nM). In hepatocellular carcinoma models, PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis.

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.

PI3Kδ-IN-14 (Compound (S)-29), a selective PI3Kδ inhibitor with an IC50 of 0.8 nM and a Kd of 84.8 nM, targets the ATP-binding site within the kinase domain of PI3Kδ. This compound exhibits anti-inflammatory properties by impeding the PI3K/AKT pathway and is noted for alleviating acute lung injury (ALI) [1].

PI3Kδ-IN-8 is a powerful and specific oral inhibitor of PI3Kδ, exhibiting an IC50 of 3.3 nM. It demonstrates preferential inhibition of PI3Kδ when compared to PI3Kα, PI3Kβ, and PI3Kγ, with IC50 values of 377.2 nM, 241.6 nM, and 17.9 nM, respectively. Furthermore, PI3Kδ-IN-8 possesses notable anti-tumor efficacy.

PI3Kδ-IN-11 is a potent and selective PI3Kδ inhibitor (IC50: 27.5 nM) that dose-dependently blocks PI3K/Akt pathway activity. PI3Kδ-IN-11 can be used in B- or T-cell-associated malignancy studies.

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

PI3Kδ-IN-13 (compound 89), with an IC50 value of 2.6 nM, is an inhibitor of PI3Kδ, applicable for researching diseases involving cell proliferation, including cancer, infection, inflammation, and autoimmune disorders [1].

PI3Kδ-IN-1 is an efficacious PI3Kδ inhibitor (IC50 of 1.7 nM).

PI3K/mTOR Inhibitor-14 (compound Y-2) serves as a dual inhibitor of PI3K and mTOR, exhibiting IC50 values of 171.4 nM and 10.1 nM , respectively, and demonstrates antitumor activities [1].

PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in cell cycle arrest at the G1 phase and apoptosis in U87-MG cells. Additionally, it demonstrates significant antiproliferative effects against various tumor cell lines, including PC-3 with an IC50 of 0.28 μM, HCT-116 with an IC50 of 0.57 μM, and U87-MG with an IC50 of 1.37 μM [1].

(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/mTOR Inhibitor-4 is an orally active pan-I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 is an enzyme inhibitor that acts on PI3Kα (IC50: 0.63 nM), PI3Kγ (IC50: 22 nM), PI3Kδ (IC50: 9.2 nM) and mTOR (IC50: 13.85 nM). PI3K/mTOR Inhibitor-4 can be used to study cancer.

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor, capable of acting on PI3Kα (IC50: 226 nM), PI3Kβ (IC50: 279 nM), PI3Kγ (IC50: 467 nM), PI3Kδ (IC50: 29 nM), HDAC1 (IC50: 1.3 nM), and PI3K/HDAC-IN-2 is PI3Kδ and class I and IIb HDAC selective and exhibits significant anticancer effects.

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.

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).

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-2 is a potent pan inhibitor of PI3K and mTOR with IC50s of 3.4, 34, 16,1 and 4.7 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR. PI3K/mTOR Inhibitor-2 has antitumor activity.

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].

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.

Linperlisib (PI3Kδ-IN-2) is a potent and selective inhibitor of PI3Kδ

PI3Kα-IN-8 is a selective inhibitor of PI3Kα (IC50: 0.012 μM). PI3Kα-IN-8 increases intracellular levels of reactive oxygen species, decreases mitochondrial membrane potential, and induces apoptosis.

PI3Kγ inhibitor 4 is a selective, potent, orally active PI3Kγ inhibitor (IC50: 40 nM). PI3Kγ inhibitor 4 is ~7-fold more selective for PI3Kγ than the α subtype, 43-fold more selective than the β subtype and 18-fold more selective than the δ subtype. inflammation.

PI3K/mTOR Inhibitor-7 is a potent dual PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-7 is 4.7-fold more potent than gedatolisib, with IC50 values of 1.4 μM and 0.3 μM, respectively. 10 μM of PI3K/mTOR Inhibitor-7 is able to significantly inhibit the PI3K/Akt/mTOR signalling pathway. PI3K/mTOR Inhibitor-7 has shown potential for research in cancer diseases.

PI3K/mTOR Inhibitor-12, a potent and selective orally active inhibitor, exhibits IC50 values of 0.06 nM for PI3Kα and 3.12 nM for mTOR, indicating significant antitumor activity with reduced liver toxicity [1].

PI3K/AKT-IN-2, a dual inhibitor of PI3K and AKT, prevents the epithelial-mesenchymal transition (EMT) and promotes apoptosis. Additionally, it impedes tubulin polymerization.

PI3K/Akt-IN-C89 is a novel Inhibitor of the PI3K-Akt Pathway, Inducing Autophagy of Female Germline Stem Cells.

PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor, and also inhibits PI3Kβ. PI3Kα-IN-7 can reduce cancer cells mitochondrial membrane potential and induce apoptosis.

PI3Kα-IN-4 is a potent, selective, and orally active PI3Kα inhibitor, demonstrating an IC50 of 1.8 nM and exhibiting antitumor activity[1].

PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor that exhibits anticancer effects without toxicity to normal cells. PI3Kα-IN-6 increases ROS production, decreases mitochondrial membrane potential and induces apoptosis.

Cathepsin K Inhibitor 3, exhibiting an IC50 value of 0.5 nM, is a highly selective inhibitor of cathepsin K, featuring a favorable pharmacokinetic profile. It holds potential for use in studies of osteoarthritis (OA).

PI3K/mTOR Inhibitor-8 is a dual inhibitor of PI3K (PI3Kα IC50: 0.46 nM) and mTOR (mTOR IC50: 12 nM). PI3K/mTOR Inhibitor-8 blocks the cell cycle of HCT-116 cells in G1/S phase and induces apoptosis. apoptosis).

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound that consists of a ligand for K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential in the synthesis of PROTAC K-Ras Degrader-1, a potent PROTAC K-Ras degrader that demonstrates a degradation efficacy of ≥70% in SW1573 cells[1].

Heterocyclic compounds as covalent inhibitors of G12C mutant K-Ras protein useful for treating cancers.K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.

PI3Kα-IN-13 (Compound 18a), a PI3Kα inhibitor with an IC50 of 2.5 nM, effectively induces apoptosis and hampers the proliferation of various cancer cell lines, exhibiting IC50 values of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), and 9.85 μM (SW620). This compound also impedes tumor cell colony formation, migration, and invasion [1].

Quercetin pentaacetate (Pentaacetylquercetin) has diverse biological activities, including antioxidant, anti-inflammatory, and anticancer properties. Quercetin pentaacetate interacts with RSV and inhibit the viral adhesion on cell surface.