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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Sophocarpine (Standard)
0 ImagesSophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
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Umckalin
0 ImagesCat. No.: HY-N8712CAS No.: 43053-62-9
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PI3K-IN-23
0 ImagesCat. No.: HY-132898CAS No.: 2755651-17-1PI3K-IN-23 is an (E)-9-oxooctadec-10-en-12-ynoic acid analogue to promote glucose uptake with an EC50 value of 7.00 μM. PI3K-IN-23 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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EpskA21
0 ImagesCat. No.: HY-161858EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction.
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D-Allose (Standard)
0 ImagesCat. No.: HY-128741RCAS No.: 2595-97-3D-Allose (Standard) is the analytical standard of D-Allose (HY-128741). This product is intended for research and analytical applications. 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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Brevianamide F (Standard)
0 ImagesCat. No.: HY-100385RCAS No.: 38136-70-8Synonyms: Cyclo(L-Pro-L-Trp) (Standard)Rebaudioside C (Standard) is the analytical standard of Rebaudioside C. This product is intended for research and analytical applications. Rebaudioside C (Dulcoside B) is a natural sweetener that can be used in controlled diets for diabetic patients.
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WNY1613
0 ImagesCat. No.: HY-147792CAS No.: 2650546-39-5WNY1613 is a potent and selective PI3Kδ inhibitor with piperazinone-containing purine scaffold. WNY1613 induces cancer cell apoptosis and inhibits the phosphorylation of PI3K downstream components in NHL cell lines. WNY1613 exhibits anti-NHL activity in vitro and in vivo.
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Vernodalin
0 ImagesCat. No.: HY-N19029CAS No.: 21871-10-3Vernodalin is an orally active, cytotoxic sesquiterpene lactone with a Kd value of 9.55 μM for p38 MAPK. Vernodalin downregulates the expression of phosphorylated ERK, JNK, AKT, PI3K, mTOR, p38MAPK, FAK, MMP-2, MMP-9, and uPA, while upregulates the expression of TIMP-1 and TIMP-2. Vernodalin increases ROS production, upregulates the expression of Bax and caspase 3, downregulates the expression of Bcl-2, and induces apoptosis (apoptosis), oxidative stress response and cell cycle arrest. Vernodalin inhibits the proliferation, adhesion and metastasis of cancer cells. Vernodalin enhances the activity of VEGF-B, AMPK and eNOS signaling pathways. Vernodalin alleviates myocardial injury and restores hemodynamic parameters. Vernodalin inhibits the growth of Trypanosoma brucei rhodesiense. Vernodalin can be used in research related to various cancers including gastric cancer, colorectal cancer and lung cancer, as well as African human trypanosomiasis and myocardial infarction.
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HYS-072
0 ImagesCat. No.: HY-172175HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer.
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PI3K-IN-49
0 ImagesCat. No.: HY-160282CAS No.: 2922415-69-6PI3K-IN-49 is a potent PI3K inhibitor. PI3K-IN-49 shows antiproliferative activity for Avg T-47D and Avg SKBR3 cells (WO2023239710A1; example 29).
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Anticancer agent 271
0 ImagesCat. No.: HY-173367Anticancer agent 271 (compound 5C) has antiproliferative activity against lung (A549), colon (Caco-2) cancer cell lines, and human lung fibroblast (WI38) with an IC50 value of 9.18 μM on A549 cells. Anticancer agent 271 downregulates PI3K and mTOR gene expression that can be used for cancer research.
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COH-19
0 ImagesCat. No.: HY-184167COH-19 is a potent mTOR inhibitor. COH-19 binds to the ATP-binding pocket of mTOR, reduces mTOR protein levels, and suppresses the PI3K/Akt/mTOR signaling pathway. COH-19 induces apoptosis via the mitochondrial pathway. COH-19 causes G0/G1 phase cell cycle arrest and suppresses cancer cell proliferation. COH-19 can be used for the research of breast cancer.
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BYBC-1
0 ImagesCat. No.: HY-181284CAS No.: 2563902-57-6BYBC‑1 is a selective G4‑RNA‑targeting ligand with high affinity forKRAS and NRAS G4‑RNAs (Kd = 0.05-0.28 μM). BYBC‑1 stabilizes G4‑RNA structures in KRAS and NRAS mRNA, blocks thePI3K/AKT and MAPK/ERK pathways, activates the DNA damage response (DDR), suppresses energy metabolism, and induces S‑phase arrest and apoptosis. BYBC‑1 exhibits high selectivity over non‑malignant fibroblasts and significantly inhibits the growth of HCT‑116 xenograft tumors in vivo. BYBC‑1 can be used for the study of colorectal cancer.
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Kukoamine B-d5 dihydrochloride
0 ImagesCat. No.: HY-N2393SKukoamine 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-d4-1 sodium
0 ImagesCat. No.: HY-113308AS2Taurolithocholic acid-d4-1 (sodium) is the deuterium labeled Taurolithocholic acid. Taurolithocholic acid sodium is an orally active bile acid and antiviral agent. Taurolithocholic acid sodium 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 sodium 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 sodium serves as an experimental model compound for hepatocellular cholestasis. At concentrations ≤200 μM, Taurolithocholic acid sodium shows no cytotoxicity and does not activate the interferon pathway. Taurolithocholic acid sodium 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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Astringin (Standard)
0 ImagesCat. No.: HY-N4093RCAS No.: 29884-49-9Synonyms: trans-Astringin (Standard)Astringin (trans-Astringin) (Standard) is the analytical standard of Astringin (HY-N4093). This product is intended for research and analytical applications. Astringin (trans-Astringin) is an orally active natural flavonoid compound. Astringin can inhibit the production of oxidative stress, inflammatory factors, etc. Astringin has multiple activities such as anti-oxidation, anti-inflammation, and anti-apoptosis. Astringin is also an inhibitor of ferroptosis. Astringin can be used in the research of diseases such as acute lung injury.
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KRAS-IN-55
0 ImagesCat. No.: HY-181883KRAS-IN-55 is a pan-KRAS inhibitor with IC50 values of 4.3, 9.6 and 1.6 nM against KRASG12C, KRASG12D and KRASG12V, respectively. KRAS-IN-55 induces the formation of a new binding pocket on KRAS, thereby forming a high-affinity ternary complex with cyclophilin A (CYPA), inhibiting the interactions of KRAS with downstream effectors RAF and PI3K, and blocking oncogenic MAPK and PI3K signaling pathways. KRAS-IN-55 is applicable to cancer research such as colorectal cancer and non-small cell lung cancer.
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Acetyl-Exenatide
0 ImagesCat. No.: HY-P4790CAS No.: 305815-28-5Acetyl-Exenatideyes is an acetylated derivative of Exenatide. Exenatide has the function similar to insulin, which can be used for research of type 2 diabetes. Exenatide can promote Th17 differentiation, inhibits Tregs differentiation, downregulates PI3K/Akt/FoxO1 phosphorylation.
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Nic-15
0 ImagesCat. No.: HY-159577CAS No.: 2896739-91-4Nic-15 (compound 4n) is an anti-constrictive agent used to antagonize the hypovascularity of pancreatic tumors. The hypovascularity allows cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop drug resistance. Nic-15 can regulate the PI3K/Akt/mTOR pathway and alleviate ER stress induced by Gemcitabine (HY-17026). Nic-15 can significantly inhibit the migration and colony formation of MIA PaCa-2 and PANC-1 pancreatic cancer cells. The combination of Nic-15 and Gemcitabine can effectively solve the problem of pancreatic tumor resistance. In an in vivo xenograft model, Nic-15 can significantly enhance the efficacy of Gemcitabine.
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PI3Kβ-IN-1
0 ImagesCat. No.: HY-145338CAS No.: 2215098-77-2PI3Kβ-IN-1 (compound (P)-14) is a selective and orally active PI3Kβ inhibitor, with an IC50 of 2 nM.
