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]
All Product Categories
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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 (669)
Related Products (669)
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Antibodies (6)
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PI3K/PIKK-IN-2
0 ImagesCat. No.: HY-181855CAS No.: 3109464-36-7PI3K/PIKK-IN-2 (Compound 2) is an inhibitor of PI3K/PIKK. PI3K/PIKK-IN-2 can be used in preparing antibody-drug conjugates (ADCs).
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Kukoamine B (Standard)
0 ImagesCat. No.: HY-N2393RCAS No.: 164991-67-7Kukoamine B (Standard) is the analytical standard of Kukoamine B. This product is intended for research and analytical applications. Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis.
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Taurolithocholic acid-d5
0 ImagesCat. No.: HY-113308SCAS No.: 1265681-64-8Taurolithocholic acid-d5 is deuterium labeled Taurolithocholic acid. Taurolithocholic acid is an orally active bile acid and antiviral agent. Taurolithocholic acid upregulates FADS2 by activating the TGR5-PI3K/AKT-SREBP2 signaling axis, inhibits SFTSV-induced ferroptosis, viral replication and viral entry of HBV/HDV, while reducing the release of IL-1β, lipid ROS and LDH. While exerting antiviral protective effects, Taurolithocholic acid also stimulates the recycling of hepatocellular membrane transporters, impairs canalicular bile acid secretion function, and induces hepatocyte cholestasis, apoptosis and acute hepatocellular injury. Taurolithocholic acid serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid not only protects mice from lethal SFTSV infection but also is suitable for studies related to severe fever with thrombocytopenia syndrome and cholestasis.
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Anti-osteoporosis agent-4
0 ImagesCat. No.: HY-149472CAS No.: 3046142-30-4Anti-osteoporosis agent-4 (Compound 11h) inhibits differentiation of primary osteoclasts. Anti-osteoporosis agent-4 attenuates RANKL-induced osteoclastogenesis. Anti-osteoporosis agent-4 inhibits osteoclast formation with an IC50 value of 358.29 nM. Anti-osteoporosis agent-4 inhibits PI3K/AKT and IκBα/NF-κB signaling pathway activation.
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Nemiralisib succinate
0 ImagesCat. No.: HY-19535BCAS No.: 1364799-98-3Synonyms: GSK2269557 succinateNemiralisib Succinate is a potent and highly selective PI3Kδ inhibitor with a pKi of 9.9.
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D-87503
0 ImagesCat. No.: HY-108959CAS No.: 800394-83-6D-87503 is a potent inhibitor of PI3k/Akt/mTOR, with the IC50s of 62 nM and 0.76 μM, respectively for PI3k and Erk2. D-87503 effectively suppressed the target downstream substrates Akt and Rsk1 kinase of the PI3k/Akt/mTOR signaling pathway.
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MCX 28
0 ImagesCat. No.: HY-139832CAS No.: 1414453-58-9MCX 28, a triple PI3K/mTOR/PIM inhibitor, displays low nanomolar activity.
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Asperosaponin V
0 ImagesCat. No.: HY-N16118CAS No.: 120481-38-1Asperosaponin V is an indirect modulator of bone metabolism-related targets (e.g., PI3K/AKT, BMP-2/p38, and ERK 1/2 pathways). Asperosaponin V promotes marrow stromal cell proliferation and induces osteoblast differentiation. Asperosaponin V is promising for research of osteoporosis and fracture healing.
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(+)-Nortrachelogenin
0 ImagesSynonyms: Wikstromol(+)-Nortrachelogenin (Wikstromol), a pharmacologically ligand from from wikstroemia indica, possesses antileukemic activity.
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Desmethyl-VS-5584
0 ImagesCat. No.: HY-101776CAS No.: 1246535-95-4Synonyms: Desmethyl-SB2343Desmethyl-VS-5584 is a dimethyl analog of VS-5584 which is an potent and selective mTOR/PI3K dual inhibitor with pyrido [2,3-d] pyrimidine structure.
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ALK/PI3K/AKT-IN-1
0 ImagesCat. No.: HY-173007CAS No.: 3050831-84-7ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids.
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740 Y-P TFA
0 ImagesCat. No.: HY-P0175ASynonyms: 740YPDGFR TFA; PDGFR 740Y-P TFA740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
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6-O-Isobutyrylbritannilactone
0 Images6-O-Isobutyrylbritannilactone is a natural melanogenesis inhibitor. 6-O-Isobutyrylbritannilactone, a sesquiterpene, can be isolated from the flowers of Inula britannica. 6-O-Isobutyrylbritannilactone inhibits IBMX (HY-12318)-induced melanin production in B16F10 cells. 6-O-Isobutyrylbritannilactone also regulates ERK, PI3K/AKT, and CREB, shows antimelanogenic activity in zebrafish embryos models.
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Anticancer agent 235
0 ImagesCat. No.: HY-N13063CAS No.: 2411108-21-7Anticancer agent 235 (Compound 49) is a modulator for PI3K/AKT/mTOR pathway, that promotes the generation of ROS, reduces the mitochondrial membrane potential, and thereby inhibits the proliferation of cancer cells HCT116, Caco-2, AGS and SMMC-772 with IC50 of 0.35-26.9 μM. Anticancer agent 235 arrests the cell cycle at G2/M phase, and induces apoptosis in HCT116.
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Ishophloroglucin A
0 ImagesCat. No.: HY-N12489CAS No.: 2263882-48-8Ishophloroglucin A is an orally active phlorotannin compound found in Ishige okamurae. Ishophloroglucin A can alleviate Dexamethasone (HY-14648)-induced muscle atrophy through muscle protein metabolism. Ishophloroglucin A can improve impaired protein synthesis (PI3K and Akt) or degradation (muscle-specific ubiquitin ligase muscle RING finger and atrogin-1). Ishophloroglucin A can be used for research of muscle atrophy-related diseases.
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Citronellol-d3
0 ImagesCat. No.: HY-W010201S1Synonyms: (±)-Citronelloll-d3; (±)-β-Citronelloll-d3Citronellol-d3 ( (±)-Citronelloll-d3) is the deuterium labeled Citronellol (HY-W010201). Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis.
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PI3K-IN-19 hydrochloride
0 ImagesCat. No.: HY-141690ACAS No.: 2132943-80-5PI3K-IN-19 hydrochloride is a phosphotidylinositol-3-kinase (PI3K) inhibitor extracted from patent WO2017153220, step 5.
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5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone
0 ImagesCat. No.: HY-N12959CAS No.: 927406-46-0Synonyms: DDR5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone (DDR) is an anticancer agent that can be extracted from Indigofera ovata. 5,4'-Dihydroxy-6,8-dimethoxy-7-O-rhamnosyl flavone can inhibit the PI3K/AKT and NF-кB pathways, inhibit the invasion and migration of cancer cells, and has anticancer activity.
