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 (671)
Related Products (671)
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Antibodies (6)
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Oroxin B (Standard)
0 ImagesOroxin B (Standard) is the analytical standard of Oroxin B. This product is intended for research and analytical applications. Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
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SH543
0 ImagesCat. No.: HY-180112SH543 is a potent anti-osteoporosis agent. SH543 inhibits nuclear factor κB ligand (RANKL)-induced osteoclastogenesis with an IC50 of 3.3 nM. SH543 directly binds to KEAP1, activates the Nrf2-HO-1 antioxidant pathway, reduces ROS levels, and inhibits PI3K-AKT and MAPK signaling pathways. SH543 attenuates pathological bone loss in ovariectomized mice. SH543 can be used for osteoporosis research.
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Tubulin-IN-55
0 ImagesCat. No.: HY-175874CAS No.: 353258-94-3Tubulin-IN-55 is a tubulin inhibitor. Tubulin-IN-55 disrupts the PI3K/Akt signaling pathway in cancer cells. Tubulin-IN-55 exerts broad-spectrum anti-proliferative activity against multiple tumor cells (HeLa, HCT116, 4T1, A549, H1299, MDA-MB231). Tubulin-IN-55 induces G2/M phase arrest and apoptosis, and inhibits tumor cell migration/invasion in cancer cells. Tubulin-IN-55 demonstrates potent antitumor efficacy in orthotopic autologous transplantation mice. Tubulin-IN-55 can be used for the study of cancer.
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BJ-2302
0 ImagesCat. No.: HY-182614CAS No.: 1631056-29-5BJ-2302 is a Src kinase inhibitor with an IC50 of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.
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PI3Kα-IN-16
0 ImagesCat. No.: HY-161140CAS No.: 1448711-61-2
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Creatine-13C monohydrate
0 ImagesCat. No.: HY-W017462S1CAS No.: 286437-18-1Creatine-13C monohydrate is the 13C-labeled Creatine monohydrate (HY-W017462). Creatine monohydrate, an endogenous amino acid derivative, plays an important role in cellular energy, especially in muscle and brain.
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D-myo-Inositol-1,3,4,5,6-pentaphosphate sodium
0 ImagesCat. No.: HY-175068Synonyms: Ins(1,3,4,5,6)P5 sodiumD-myo-Inositol-1,3,4,5,6-pentaphosphate sodium (Ins(1,3,4,5,6)P5 sodium) is a small intracellular signaling molecule. D-myo-Inositol-1,3,4,5,6-pentaphosphate sodium inhibits the PI3K/Akt signaling pathway. D-myo-Inositol-1,3,4,5,6-pentaphosphate sodium inhibits Akt/PKB phosphorylation and kinase activity, inducing apoptosis in cancer cells. D-myo-Inositol-1,3,4,5,6-pentaphosphate sodium inhibits the formation of tubular structures in endothelial cells in an in vitro angiogenesis mouse model. D-myo-Inositol-1,3,4,5,6-pentaphosphate sodium can be used in research on ovarian cancer, lung cancer, breast cancer, and other cancers, as well as in cardiovascular and cerebrovascular diseases such as angiogenesis.
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MTX-241F
0 ImagesCat. No.: HY-149556CAS No.: 3036637-30-3MTX-241F is a selective small molecule inhibitor targeting EGFR and PI3 kinase family members. MTX-241F is able to penetrate the blood-brain barrier and control tumor growth over the long term. MTX-241F exhibits radiosensitizing activity in patient-derived DIPG neurospheres and may be used in the study of diffuse intrinsic pontine glioma (DIPG).
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PI3K-IN-52
0 ImagesCat. No.: HY-161301CAS No.: 3030012-25-7
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Picolinafen
0 ImagesCat. No.: HY-W711035CAS No.: 137641-05-5Synonyms: AC 900001Picolinafen is a pyridine-class herbicide that acts as a phytoene desaturase (PDS) inhibitor. Picolinafen effectively controls broadleaf weeds and disrupts carotenoid biosynthesis. Picolinafen exhibits cytotoxicity to porcine trophectoderm (pTr) and luminal epithelial (pLE) cells. Picolinafen induces (ROS accumulation, calcium depletion, and activates (MAPK and PI3K signaling pathways, leading to decreased cell viability, increased apoptosis, impaired migration, and altered expression of implantation-related genes. Picolinafen has an LD50 value of 2.7 mg/kg in mammals and 7 μg/L in fish. Picolinafen exhibits toxic effects during zebrafish embryogenesis[1][2].
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Dinitramine
0 ImagesCat. No.: HY-W714183CAS No.: 29091-05-2Dinitramine is a herbicide. Dinitramine activates the Erk/P38/JNK/MAPK pathway and inactivates the PI3k/Akt pathway in testicular cells. Dinitramine induces endoplasmic reticulum stress, dysregulation of calcium homeostasis in the cytoplasm and mitochondria, apoptosis, and downregulated expression of cell cycle genes in testicular cells. Dinitramine reduces the viability and proliferation capacity of testicular cells, and inhibits cell division by suppressing the synthesis of tubulin. Dinitramine induces abnormal heart development, inhibited angiogenesis, inflammatory responses, apoptosis, and impaired embryonic growth in zebrafish embryos.
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Fenhexamid-d10
0 ImagesCat. No.: HY-W701943CAS No.: 1246815-53-1Fenhexamid-d10 is the deuterium labeled Fenhexamid (HY-118065). Fenhexamid, a botryticide, is a sterol biosynthesis inhibitor. Fenhexamid shows fungicide efficient against the plant pathogenic fungus Botryotinia fuckeliana (Botrytis cinerea).
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Demethoxyviridiol
0 ImagesCat. No.: HY-135526CAS No.: 56617-66-4Synonyms: DesmethoxyviridiolDemethoxyviridiol is a mycotoxin originally isolated from N. hinnuleum. Demethoxyviridiol induces lethality in day-old cockerels (LD50=4.2 mg/kg). Demethoxyviridiol is also an inhibitor of phosphatidylinositol 3-kinase (PI3K).
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PI3K-IN-26
0 ImagesCat. No.: HY-142676CAS No.: 1918151-65-1PI3K-IN-26 is a potent PI3K inhibitor with an IC50 of 36 nM for SU-DHL-6 cells (WO2016066142A1, compound 1).
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(3R,10R,14aS)-AZD4625
0 ImagesCat. No.: HY-146223APurity: 98.00%(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer.
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Dihydrocapsaicin-d3
0 ImagesCat. No.: HY-N0361SCAS No.: 1330261-21-6Dihydrocapsaicin-d3 is the deuterium labeled Dihydrocapsaicin (HY-N0361). Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.
