pi3

NVS-PI3-4 is a highly selective inhibitor of the enzyme PI3Kγ. It is specifically designed for use in scientific investigations related to allergies, inflammatory conditions, and cancerous diseases[1][2].

PI3-Kinase α Inhibitor 2 (hydrochloride) is a PI3-Kinase α inhibitor.

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It inhibits PKA, KDR, PKCα, and cyclin E/Cdk2 significantly less effectively (IC50 = 91, 3.4, 466, and 28 μM, respectively). PI3Kα inhibitor 2 inhibits A375 melanoma cell proliferation with an IC50 value of 580 nM.

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.

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

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.

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.

PI3Kα Inhibitor 7 is a useful organic compound for research related to life sciences. The catalog number is T9312 and the CAS number is 1239978-63-2.

PI3K Akt mTOR-IN-2 is a potent PI3K AKT mTOR inhibitor with anticancer effects and selectivity for MDA-MB-231 cells (IC50 2.29 μM). It induces cell cycle arrest and apoptosis in cancer cells.

PI3Kδ-IN-15 is a selective PI3Kδ inhibitor that inhibits PI3Kδ more than 30-fold more effectively than PI3Kγ, PI3Kβ, and PI3Kα.

Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor. Safingol hydrochloride inhibits PKC and PI3k.

(2S,3R,4S)-4-Hydroxyisoleucine (Hydroxyisoleucine) from fenugreek (Trigonella foenum-graecum) seeds is a potential insulinotropic (anti-diabetic) and anti-obesity amino acid that stimulates glucose-dependent insulin secretion from pancreatic cells, activates insulin receptor substrate-associated phosphoinositide 3 (PI3) kinase activity, and reduces plasma levels of triglycerides, free fatty acids, and cholesterol.

CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting over 10-1500 fold selectivity over other class I, II, and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM), and PI4KIIIB (IC50, 300.2 nM). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.

PI3K-IN-46 is a specific inhibitor of PI3Kγ.

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

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, respectively. PI3K mTOR Inhibitor-2 demonstrates antitumor activity.

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

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase AKT mTOR pathway and delays sensitive cells in late mitosis.

PI3K-IN-47 (Compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (PI3K) family, with IC50 values of 0.44 nM for PI3Kα, and 7.18 nM, 13.92 nM, and 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ respectively. It induces G1 phase cell cycle arrest and exhibits anti-neoplastic properties by restraining colony formation and cell migration. Additionally, PI3K-IN-47 has demonstrated the ability to suppress tumor growth in HGC-27 xenograft mouse models [1].

PI3K-IN-41 (compound 2), a photocaged PI3K inhibitor (IC50=18.92 nM) with anticancer properties, demonstrates potent PI3K inhibition following UV light irradiation and has been shown to enhance antitumor effects [1]. This compound has potential for use in precisely controlled cancer therapeutics.

MEK PI3K-IN-2 (compound 6s), a potent inhibitor of both MEK and PI3K, demonstrates IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), effectively reducing pAKT and pERK1 2 levels and exhibiting anti-proliferative activity against various tumor cell lines [1].

PI3K-IN-30 (compound 6d) is a potent PI3K inhibitor with IC50 values of 5.1 nM for PI3Kα, 136 nM for PI3Kβ, 30.7 nM for PI3Kγ, and 8.9 nM for PI3Kδ.

PI3K-IN-22 is a dual kinase inhibitor of PI3Kα and mTOR, with IC50s of 0.9 and 0.6 nM respectively. PI3K-IN-22 could be used in cancer.

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.

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

PI3K HDAC-IN-2 is a potent dual PI3K HDAC inhibitor with IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, 29 nM for PI3Kδ, and 1.3 nM for HDAC1. PI3K HDAC-IN-2 is selective for PI3Kδ and class I and IIb HDACs, exhibiting significant anticancer effects.

PI3K mTOR Inhibitor-3 (compound 12) is an imidazoline compound with potent dual inhibition of PI3K and mTOR, exhibiting notable anti-cancer activity [1].

PI3Kδ-IN-17 (Compound S5) is a potent PI3K δ inhibitor with an IC50 value of 2.82 nM, significantly inhibiting SU-DHL-6 cell proliferation with an IC50 of 0.035 μM [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).

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.

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.

PI3Kγ inhibitor 2 is an orally bioavailable inhibitor of PI3Kγ(Ki of 4 nM).

(S)-PI3Kα-IN-4, a potent inhibitor of PI3Kα with an IC50 of 2.3 nM, demonstrates 38.3-, 4.25-, and 4.93-fold selectivity over PI3Kβ, PI3Kδ, and PI3Kγ, respectively, and is suitable for cancer research[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1].

PI3Kα-IN-7 (Compound A12) is a potent inhibitor of PI3Kα and PI3Kβ, capable of reducing mitochondrial membrane potential in cancer cells and inducing apoptosis.

PI3K-IN-35 (Compound 6l) is a highly selective inhibitor of PI3K, targeting PI3K-α (IC50: 13.98 μM), PI3K-β (IC50: 7.22 μM), and PI3K-δ (IC50: 10.94 μM). It blocks the cell cycle in the G2 M phase and induces apoptosis, making it useful for studying leukemia.

PI3K mTOR Inhibitor-4 is an orally active pan-I PI3K mTOR enzyme inhibitor, acting 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/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 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].

PI3Kα-IN-19 (Compound 1) serves as an inhibitor of PI3Kα, specifically targeting the p110α catalytic subunit. PI3Kα, a frequently dysregulated kinase, is extensively utilized in cancer research [1].

PI3K-IN-55 (Compound 6a) serves as a potential inhibitor of PI3K. It modulates the PI3K Akt p53 signaling pathway and inhibits proliferation in cancer cell lines A549, Hela, HepG2, MCF-7, and HT-29, with IC50 values ranging from 1.03 to 6.78 μM. Additionally, PI3K-IN-55 induces apoptosis in MCF-7 cells.

PI3Kα-IN-21 (compound 8) is a selective inhibitor of PI3Kα, demonstrating greater selectivity over PI3Kβ, PI3Kγ, and PI3Kδ by factors of 10.41, 16.99, and 37.53 respectively (IC50: 96.89 568.24 397.48 nM). This compound inhibits cancer cell activity, proliferation, and migration while inducing mitochondrial apoptosis through the PI3K Akt mTOR pathway. Additionally, PI3Kα-IN-21 has shown in vivo antitumor efficacy in a mouse model of non-small cell lung cancer.

PI3K-IN-51, characterized as a PI3K inhibitor, exhibits IC50 values below 500 nM for p120γ and p110δ p85α (WO2016204429A1; Example 10) [1].

PI3K mTOR Inhibitor-14 (compound Y-2) is a dual inhibitor of PI3K and mTOR, with IC50 values of 171.4 nM and 10.1 nM, respectively, and exhibits antitumor activities [1].

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 used in researching chronic respiratory conditions, including asthma and chronic obstructive pulmonary disease (COPD) [1].

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].