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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EGFR-IN-214
0 ImagesCat. No.: HY-184311CAS No.: 3077316-17-4EGFR-IN-214 is an orally active EGFR inhibitor with an EC50 of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma.
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20-5,14-HEDE-d2
0 ImagesCat. No.: HY-160099SSynonyms: WIT003-d220-5,14-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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Toyaburgine
0 ImagesCat. No.: HY-172259Toyaburgine is a unique isoquinoline compound that exhibits anti-tumor activity. It packs a punch by disrupting the PI3K/AKT/mTOR signaling pathway, causing significant morphological changes and cell death in MIA PaCa-2 cells. On top of that, it puts the brakes on cell migration and colony formation. This compound is showing a lot of promise in the realm of pancreatic cancer research.
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PLAGL2-IN-1
0 ImagesCat. No.: HY-180281CAS No.: 3099026-16-8PLAGL2-IN-1 is a inhibitor of pleiomorphic adenoma-like protein 2 (PLAGL2) with a Kd of 2.23 µM. PLAGL2-IN-1 suppresses PLAGL2 transcriptional activity, induces G0/G1 cell cycle arrest, and apoptosis, thereby inhibiting hepatocellular carcinoma (HCC) cell proliferation. PLAGL2-IN-1 disrupts extracellular matrix organization and suppresses the PI3K-AKT pathway by reducing AKT phosphorylation. PLAGL2-IN-1 inhibits tumor growth in an HCCLM3 xenograft mouse model. PLAGL2-IN-1 can be used for the research of HCC.
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1-Monopalmitin (Standard)
0 ImagesSynonyms: Glyceryl palmitate (Standard)1-Monopalmitin (Glyceryl palmitate) (Standard) is the analytical standard of 1-Monopalmitin (HY-W009141). This product is intended for research and analytical applications. 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells.
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1-Monopalmitin-d31
0 ImagesCat. No.: HY-W009141SSynonyms: Glyceryl palmitate-d311-Monopalmitin-d31 (Glyceryl palmitate-d31) is the deuterium labeled 1-Monopalmitin (HY-W009141). 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells.
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PI3Kδ-IN-17
0 ImagesCat. No.: HY-149634CAS No.: 2768181-63-9PI3Kδ-IN-17 (Compound S5) is a potent inhibitor of PI3Kδ, with IC50 of 2.82?nM. PI3Kδ-IN-17 shows strong inhibitory activity of proliferation in SU-DHL-6 cells (IC50 = 0.035 μM).
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Arteanoflavone
0 ImagesCat. No.: HY-133804CAS No.: 68710-17-8Arteanoflavone, a natural compound that can be isolated from A. iwayomogi, possess inhibitory activities on AGEs formation.
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(±)-Armepavine hydrochloride
0 ImagesCat. No.: HY-N6857CCAS No.: 13944-21-3(±)-Armepavine hydrochloride is a compound that has demonstrated immunosuppressive effects on T lymphocytes and in lupus nephritic mice.
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Phellodendrine chloride (Standard)
0 ImagesCat. No.: HY-N0735RCAS No.: 104112-82-5Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
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Bacopaside I (Standard)
0 ImagesCat. No.: HY-N4246RCAS No.: 382148-47-2Bacopaside I (Standard) is the analytical standard of Bacopaside I. This product is intended for research and analytical applications. Bacopaside I is an orally active aquaporin AQP1 inhibitor and PKC modulator with neuroprotective and anticancer activities. Bacopaside I specifically blocks the water channel and cGMP-gated ion channel activities of AQP1 without affecting AQP4, thereby inhibiting the migration of colon cancer cells expressing AQP1. Bacopaside I activates the Akt pathway by interacting with PI3K, specifically inhibits MAO-A, effectively alleviates neuron necrosis and apoptosis induced by oxygen-glucose deprivation, reduces oxidative stress, and regulates the surface expression of neuroreceptors. When combined with Bacopaside II (HY-N6016), Bacopaside I significantly reduces the viability, proliferation and invasion ability of breast cancer cells, and binds to the pregnane X receptor (PXR). Bacopaside I is applicable to the research of colon cancer, breast cancer, vascular dementia, cerebral ischemia and other related diseases.
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Anticancer agent 164
0 ImagesCat. No.: HY-128634CAS No.: 2235393-30-1CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer.
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ML-220
0 ImagesCat. No.: HY-16332CAS No.: 662151-10-2ML-220 is a PI3K modulator that can be used for the study of neoplasms and infectious diseases.
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PI3K-IN-50
0 ImagesCat. No.: HY-160283CAS No.: 3023536-43-5PI3K-IN-50 is a phosphotidylinositol-3-kinase (PI3K) inhibitor extracted from patent WO2023239710A1, example 35.
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SHP2-IN-35
0 ImagesCat. No.: HY-170877SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression.
