PI3K
PI3K signaling regulates cellular function by linking growth factors, GPCRs, and oncogene products to intracellular lipid signaling[1]. Mechanistically, class I PI3K isoforms generate PIP3, a second messenger that controls cell movement, growth, survival, and differentiation[2][3]. Therefore, PI3K biology provides a practical framework for studying metabolism, immune-system function, cancer, and inflammation[1][2]. In disease-focused models, PI3K pathway activation supports cancer-cell growth, survival, motility, and metabolism, making pathway inhibition relevant for genetically and clinically defined cancers[2]. Compared with related isoforms, PI3Kα inhibition is most effective in cancers with genetic activation of this isoform, whereas PI3Kδ inhibition acts mainly through B-cell antigen receptor signaling and tumor-stroma interactions[4]. PI3Kδ and PI3Kγ also function prominently in leukocytes, and dual blockade with IPI-145 suppressed immune responses in autoimmune and inflammatory disease models[5]. For experimental applications, IPI-145 inhibited PI3K/AKT/S6 signaling, reduced CLL-cell chemokine secretion and chemotaxis, and promoted apoptosis in BCR-stimulated or stromal co-cultured primary CLL cells[6].
References:
- [1]. Vanhaesebroeck B, et al. PI3K signalling: the path to discovery and understanding. Nat Rev Mol Cell Biol. 2012 Feb 23;13(3):195-203. [Content Brief]
- [2]. Fruman DA, et al. The PI3K Pathway in Human Disease. Cell. 2017 Aug 10;170(4):605-635. [Content Brief]
- [3]. Hawkins PT, et al. PI3K signalling in inflammation. Biochim Biophys Acta. 2015 Jun;1851(6):882-97. [Content Brief]
- [4]. Vanhaesebroeck B, et al. PI3K inhibitors are finally coming of age. Nat Rev Drug Discov. 2021 Oct;20(10):741-769. [Content Brief]
- [5]. Winkler DG, et al. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74. [Content Brief]
- [6]. Balakrishnan K, et al. The phosphoinositide-3-kinase (PI3K)-delta and gamma inhibitor, IPI-145 (Duvelisib), overcomes signals from the PI3K/AKT/S6 pathway and promotes apoptosis in CLL. Leukemia. 2015 Sep;29(9):1811-22. [Content Brief]
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PI3K Inhibitors
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PI3K Agonists
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PI3K Antagonist
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PI3K Activators
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PI3K Modulators
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PI3K Inducers
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PI3K Degraders
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PI3K Controls
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PI3K Ligands
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PI3K Related Products (659)
Related Products (659)
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Antibodies (6)
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PI3K-IN-28
0 ImagesCat. No.: HY-145432CAS No.: 2747100-02-1PI3K-IN-28 (Compound 6c) is a potent inhibitor of PI3K. PI3K-IN-28 displays the most potent activity with lower toxic effects on MCF-10a. PI3K-IN-28 displays half-maximal inhibitory concentration (IC50, μM) values of 5.8, 2.3, and 7.9. PI3K-IN-28 is the most potent one with a selectivity index (SI) of 39 and is considered as a latent lead for further optimization of anticancer agents.
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Myrislignan-13C,d2
0 ImagesCat. No.: HY-N0608SMyrislignan-13C,d2 is the 13C, d2 deuterated-labeled Myrislignan (HY-N0608). Myrislignan is a PI3K/AKT/NF-κB inhibitor that can cross the blood-brain barrier. Myrislignan exerts anticancer activity by inducing apoptosis and ferroptosis. Myrislignan inhibits the replication and invasion of Toxoplasma gondii; it induces reactive oxygen species (ROS) imbalance, autophagy, and the death of Toxoplasma gondii tachyzoites. Myrislignan inhibits mitochondrial function and ERK1/2 phosphorylation to improve ovariectomy-induced osteoporosis. Myrislignan can be used in studies related to gastric cancer, glioblastoma, osteoporosis, and toxoplasmosis.
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BPH-628
0 ImagesCat. No.: HY-113869CAS No.: 1059677-40-5BPH-628 is an aromatic geranylgeranyl diphosphate synthase (GGPPS) inhibitor, with a pIC50 of 6.1.
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Dezapelisib
0 ImagesCat. No.: HY-109029CAS No.: 1262440-25-4Synonyms: INCB040093Dezapelisib (NCB040093) is a potent inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ). Dezapelisib is a promising research strategy for select R/R B-cell lymphomas.
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Wortmannin (Standard)
0 ImagesSynonyms: SL-2052 (Standard); KY-12420 (Standard)Wortmannin (Standard) is the analytical standard of Wortmannin. This product is intended for research and analytical applications. Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.
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20-5,14-HEDE-d2-2
0 ImagesCat. No.: HY-160099S2Synonyms: WIT003-d2-220-5,14-HEDE-d2 (WIT003-d2) is the deuterated-labeled 20-5,14-HEDE (HY-160099). 20-5,14-HEDE (WIT003) is an analog of 20-HETE. 20-5,14-HEDE activates PI3K/Akt signaling pathway, thereby exhibiting anti-apoptotic and cell survival promoting effects. 20-5,14-HEDE is the agonist for 20-HETE that increases intracellular Ca2+ concentrations, thereby enhancing vasoconstriction.
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Gedatolisib-d6
0 ImagesCat. No.: HY-10681S1Synonyms: PKI-587-d6; PF-05212384-d6Gedatolisib-d6 (PKI-587-d6) is the deuterium labeled Gedatolisib (HY-10681). Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
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JE-133
0 ImagesCat. No.: HY-163151CAS No.: 2579171-69-8JE-133 is an optically active isochromane-2H-chromene conjugate. JE-133 exhibits antioxidant and anti-inflammatory activities. JE-133 is a neuroprotective agent that effectively inhibits neuronal oxidative damage associated with PI3K/Akt and MAPK signaling pathways. JE-133 can also inhibit lipopolysaccharide (LPS) (HY-D1056)-induced neuroinflammation by regulating JAK/STAT and Nrf2 signaling pathways.
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Levomilnacipran-d10 hydrochloride
0 ImagesCat. No.: HY-14794ASCAS No.: 2747914-23-2Synonyms: (1S,2R)-Milnacipran-d10 hydrochloride; F2695-d10 hydrochlorideLevomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran hydrochloride (HY-B0168B). Levomilnacipran ((1S,2R)-Milnacipran) hydrochloride is the enantiomer of Milnacipran (HY-B0168) and a strong substrate of P-gp that can cross the blood-brain barrier. Levomilnacipran hydrochloride is a serotonin and norepinephrine reuptake inhibitor, with IC50 values of 10.5 nM and 19.0 nM, and Ki values of 92.2 nM and 1.2 nM for human norepinephrine transporter (NET) and serotonin transporter (SERT), respectively. Levomilnacipran hydrochloride has antidepressant and anxiolytic activities. Levomilnacipran hydrochloride can be used for the research of depression.
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PI3K-IN-48
0 ImagesCat. No.: HY-156080CAS No.: 3052306-60-9PI3K-IN-48 is a PI3K inhibitor with IC50 value of 1.55 ± 0.18 μM for A549 cells. PI3K-IN-48 can induce G0/G1 phase arrest, cell apoptosis, and down-regulate expression of p-PI3K and p-Akt. PI3K-IN-48 can be used for human lung cancers diseases research.
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RMC-4998 TFA
0 ImagesCat. No.: HY-156671BPurity: 99.02%RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRASG12C mutant. RMC-4998 TFA can form a ternary complex with intracellular CYPA and the activated KRASG12C mutant, with an IC50 value of 28 nM. RMC-4998 TFA can inhibit ERK signaling in KRASG12C mutant cancer cells and induce apoptosis. RMC-4998 TFA can be used for for non-small cell lung cancer (NSCLC) research.
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PI3Kα-IN-22
0 ImagesCat. No.: HY-161373CAS No.: 2925030-26-6PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3KαH1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice.
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Antitumor agent-86
0 ImagesCat. No.: HY-152774CAS No.: 2907704-65-6
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Fenitrothion-d6
0 ImagesCat. No.: HY-B1885SCAS No.: 203645-59-4Fenitrothion-d6 is the deuterium labeled Fenitrothion (HY-B1885). Fenitrothion is a broad-spectrum and orally active insecticide/acaricide. Fenitrothion inhibits cholinesterase, AMPKα and IRS1/PI3K/AKT. Fenitrothion causes Apoptosis, reduces SOD activity. Fenitrothion shows insecticidal effect against Rhyzopertha dominica and Tribolium castaneum adults. Fenitrothion is widely used in cotton crops, vegetable crops, fruit crops and field crops, especially rice. Fenitrothion can be used for brain and spleen toxicology studies.
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D-Allose-13C
0 ImagesCat. No.: HY-128741SCAS No.: 70849-28-4D-Allose-13C is the 13C labeled D-Allose (HY-128741). D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities.
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JZ19
0 ImagesCat. No.: HY-173005JZ19 reduces the LDH and ROS levels, and exhibits antioxidant activity against oxygen-glucose deprivation (OGD)-induced cardiomyocyte injury. JZ19 reverses Isoproterenol (HY-B0468)-induced cardiomyocyte hypertrophy and apoptosis through PI3K-AKT-GSK3β signaling pathway. JZ19 alleviates Isoproterenol (HY-B0468)-induced heart failure in mouse models.
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JRN73958
0 ImagesCat. No.: HY-182236CAS No.: 171773-95-8Synonyms: Reduced scytoneminJRN73958 (Reduced scytonemin) is a PI3K/Akt, MAPK, and NF-κB inhibitor found in Nostoc commune. JRN73958 inhibits nitric oxide production, induce reactive oxygen species (ROS) generation, and lead to autophagy. JRN73958 decreases LPS (HY-D1056)/IFNγ-induced PI3K/Akt, MAPK, and NF-κB activity. JRN73958 can be used for the research of leukemia.
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(+)-Licarin
0 ImagesCat. No.: HY-N12338CAS No.: 42016-15-9(+)-Licarin (Compound 7) is a compound derived from Ocotea macrophylla Kunth. leaves octanoid neolignans.
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LASSBio-2337
0 ImagesCat. No.: HY-181710LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer.
