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 (664)
Related Products (664)
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Antibodies (6)
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Panulisib
0 ImagesCat. No.: HY-16769CAS No.: 1356033-60-7Synonyms: P7170; AK151761Panulisib (P7170; AK151761) is an orally active inhibitor of PI3K (IC50 = 2.2 nM) and mTOR (IC50 = 4.4 nM). Panulisib inhibits ALK1 and DNA-PK, two enzymes that respectively participate in angiogenesis and DNA repair, with IC50 values of 47 nM and 1.5 nM respectively. Panulisib inhibits cell proliferation and apoptosis. Panulisib can be used for research on breast cancer and non-small cell lung cancer.
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Cajanol
0 ImagesCat. No.: HY-N10342CAS No.: 61020-70-0Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp.. Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections.
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PI3Kγ inhibitor 5
0 ImagesCat. No.: HY-139880CAS No.: 2566569-31-9PI3Kγ inhibitor 5 is an inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with an IC50 value of 34 nM.
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Oxypeucedanin (Standard)
0 ImagesOxypeucedanin (Standard) is a furanocoumarin derivative found in Angelica dahurica. Oxypeucedanin (Standard) is an orally active PI3K/AKT/NF-κB, MAPK, and ROS inhibitor. Oxypeucedanin (Standard) induces cell cycle arrest and apoptosis. Oxypeucedanin (Standard) inhibits hKv1.5 channel currents (IC50: 76 nM). Oxypeucedanin (Standard) exhibits anticancer, anti-inflammatory, antioxidant and antiarrhythmic activities.
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SH-273
0 ImagesCat. No.: HY-177908CAS No.: 3084159-97-4SH-273 is a dual targeting compound. SH-273 has dual function to stimulate STING function (EC50: 100 nM) and inhibits PI3Kγ (IC50: 7 nM). SH-273 can be used in the research of pancreatic cancer.
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ST-162
0 ImagesCat. No.: HY-124615CAS No.: 1883817-83-1
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Erufosine
0 ImagesCat. No.: HY-171777CAS No.: 202867-33-2Synonyms: ErPC3; ErucylphosphohomocholineErufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.
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D-Allose-13C-1
0 ImagesCat. No.: HY-128741S1D-Allose-13C-1 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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RV-1729
0 ImagesCat. No.: HY-106006CAS No.: 1293915-42-0RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). RV-1729 identifies inhibition of the PI3K isotype by quantifying the release of phosphatidylinositol 3,4, 5-triphosphate (PIP3) (IC50=12 nM), showing twice the selectivity for PI3Kδ relative to PI3Kγ. RV-1729 is also 16 times more selective to PI3Kα. RV-1729 regulates immune and inflammatory responses by inhibiting PI3Kδ. RV-1729 can be used in studies of asthma and chronic obstructive pulmonary disease (COPD).
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Nogo-B-IN-1
0 ImagesCat. No.: HY-175317Nogo-B-IN-1 ((S,R)-4v) is a covalent Nogo-B inhibitor. Nogo-B-IN-1 inhibits the progression of osteosarcoma (OS) by suppressing Nogo-B activity and the PI3K/AKT/NF-κB/Bcl-2 signaling pathway. Nogo-B-IN-1 inhibits the proliferation of OS 143B cells (IC50 = 0.28 µM) and induces apoptosis. Nogo-B-IN-1 can be used for OS targeting research.
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Schisanhenol B
0 ImagesCat. No.: HY-N0859ACAS No.: 102681-52-7Schisanhenol B is one of the active ingredients of schisandra chinensis. Schisanhenol B is a tyrosinase inhibitor. Schisanhenol B has good binding activity with PIK3CG and can be used in the study of heart failure.
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WH23
0 ImagesCat. No.: HY-181670WH23 is a dehydrogenase/reductase SDR family member 11 (DHRS11) inhibitor with IC50 values of 0.037 μM. WH23 binds to DHRS11, forming a hydrogen bond with the enzyme’s His210 residue. WH23 suppresses androgen receptor mRNA and protein expression, reduces c-Myc expression, and inhibits cancer cell proliferation. WH23 inhibits PI3K/AKT signaling by reducing phosphorylation of PDK1, AKT, mTOR, and ERK. WH23 enhances Capivasertib (HY-15431)-induced cytotoxicity and apoptosis. WH23 can be used for the research of luminal androgen receptor-positive triple-negative breast cancer.
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Berberine hemisulfate (Standard)
0 ImagesCat. No.: HY-N0716ARCAS No.: 316-41-6Synonyms: Natural Yellow 18 hemisulfate (Standard)Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
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PI3K/Akt/mTOR-IN-3
0 ImagesCat. No.: HY-147913CAS No.: 2457245-94-0PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest.
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NF-κB-IN-19
0 ImagesCat. No.: HY-172201NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
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PIP5K1A Recombinant Human Active Lipid Kinase
0 ImagesCat. No.: HY-E70631PIP5K1A phosphorylates PI4P to synthesize the important signalling phospholipid PI(4,5)P2. This phospholipid also serves as the substrate for PI3K for conversion into PI(3,4,5)P3 to stimulate cell growth and survival. PIP5K1A has been directly implicated in breast cancer and prostate cancer. PIP5K1A Recombinant Human Active Lipid Kinase is a recombinant PIP5K1A protein that can be used to study PIP5K1A-related functions.
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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.
