MW 307.3 Da, Purity >99%. A highly selective inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 μM). Selective over a range of other kinases including protein kinase C, protein kinase A, MAPK and PI4- kinase (IC50 > 50 μM).
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- Neoplasma 70:402-4152023TRIM31 promotes the progression of oral squamous cell carcinoma through upregulating AKT phosphorylation and subsequent cellular glycolysis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesSheng-Qi Sang,Yi-Jie Zhao,Meng Wang,Xiao-Qi Zhong,Zhi-Cheng Yang,Meng-Meng LuPubMed 37498068
- Oncology research 30:277-2882023Inhibition of apoptosis-regulatory protein Siva-1 reverses multidrug resistance in gastric cancer by targeting PCBP1.Applications:Unspecified applicationReactive species:Unspecified reactive speciesFanbiao Kong,Kun Wu,Liming Pang,Yuliang Huang,Lei Li,Jing Xu,Feitong Li,Yan Qing,Zhongyu Wang,Xiurong Huang,Sheng Xu,Xiaogang Zhong,Zhou Zhu,Xiaotong Wang,Jianrong YangPubMed 37303491
- Cells 12:2023IRF3 Activation in Mast Cells Promotes FcεRI-Mediated Allergic Inflammation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYoung-Ae Choi,Hima Dhakal,Soyoung Lee,Namkyung Kim,Byungheon Lee,Taeg Kyu Kwon,Dongwoo Khang,Sang-Hyun KimPubMed 37296614
- Frontiers in physiology 13:8619812022Effects of cGMP/Akt/GSK-3β signaling pathway on atrial natriuretic peptide secretion in rabbits with rapid atrial pacing.Applications:Unspecified applicationReactive species:Unspecified reactive speciesShuxia Cao,Chengyong Han,Chunhua Xuan,Xiangdan Li,Jing Wen,Dongyuan XuPubMed 36060704
- BMC cancer 22:6282022Interfering with the expression of EEF1D gene enhances the sensitivity of ovarian cancer cells to cisplatin.Applications:Unspecified applicationReactive species:Unspecified reactive speciesQia Xu,Yun Liu,Shenyi Wang,Jing Wang,Liwei Liu,Yin Xu,Yide QinPubMed 35672728
- Scientific reports 12:40312022Nectin cell adhesion molecule 4 regulates angiogenesis through Src signaling and serves as a novel therapeutic target in angiosarcoma.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYuka Tanaka,Maho Murata,Keiko Tanegashima,Yoshinao Oda,Takamichi ItoPubMed 35256687
- Oxidative medicine and cellular longevity 2022:69338122022Protection of Human Lens Epithelial Cells from Oxidative Stress Damage and Cell Apoptosis by KGF-2 through the Akt/Nrf2/HO-1 Pathway.Applications:Unspecified applicationReactive species:Unspecified reactive speciesShuyu Liu,Zi Jin,Ruyue Xia,Zhuoni Zheng,Yi Zha,Qiang Wang,Xinbei Wan,Hui Yang,Jianqiu CaiPubMed 35222803
- Tissue engineering and regenerative medicine 19:403-4152022Application of Bone Marrow Mesenchymal Stem Cells Effectively Eliminates Endotoxemia to Protect Rat from Acute Liver Failure Induced by Thioacetamide.Applications:Unspecified applicationReactive species:Unspecified reactive speciesTing Jiang,Geng Xia,Bo Yang,Hong-Wei Zhang,Yue-Shan Yin,Cheng-Wei Tang,Jin-Hui YangPubMed 35122584
- Medical science monitor : international medical journal of experimental and clinical research 27:e9281532021Salvianic Acid A Regulates High-Glucose-Treated Endothelial Progenitor Cell Dysfunction via the AKT/Endothelial Nitric Oxide Synthase (eNOS) Pathway.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYanhua Guan,Xu WangPubMed 33770068
Key facts
- CAS number
- 154447-36-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 307.3 Da
- Molecular formula
- C19H17NO3
- PubChem identifier
- 3973
- Nature
- Synthetic
Alternative names
1-phosphatidylinositol 3-kinase, 5 HT 2B receptor, 5 HT(2B), 5 HT2 receptor, 5 Hydroxytryptamine 2C receptor, 5 hydroxytryptamine (serotonin) receptor 2B, 5 hydroxytryptamine (serotonin) receptor 2B G protein coupled, 5 hydroxytryptamine 2B receptor, 5-HT-1C, 5-HT-2, 5-HTR2C, 5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha, 5-bisphosphate 3-kinase 110 kDa catalytic subunit beta, 5-bisphosphate 3-kinase 110 kDa catalytic subunit delta, 5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma, 5-bisphosphate 3-kinase catalytic subunit alpha isoform, 5-bisphosphate 3-kinase catalytic subunit beta isoform, 5-bisphosphate 3-kinase catalytic subunit delta isoform, 5-bisphosphate 3-kinase catalytic subunit gamma isoform, 5-ht-1c receptor, 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled, 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled, 5-hydroxytryptamine 2A receptor, 5-hydroxytryptamine receptor 1C, 5-hydroxytryptamine receptor 2A, 5-hydroxytryptamine receptor 2B, 5-hydroxytryptamine receptor 2C, 5HT2A_HUMAN, 5HT2B_HUMAN, 5HT2C_HUMAN, 5HT2F, APDS, C2 PI3K, C2 containing phosphatidylinositol kinase, C2 domain containing alpha polypeptide, CBX, CBX1_HUMAN, CK II, CK II alpha, CK II alpha', CK II beta, CK2A1, CK2A2, CK2B, CK2N, CLOVE, CNK, CPK, CSK21_HUMAN, CSK22_HUMAN, CSK2B_HUMAN, CSNK 2B, CWS5, Casein kinase 2 alpha prime polypeptide, Casein kinase 2 beta polypeptide, Casein kinase II alpha chain, Casein kinase II alpha' chain, Casein kinase II beta subunit, Casein kinase II subunit alpha, Casein kinase II subunit alpha', Casein kinase II subunit beta, Casein kinase II, alpha 1 polypeptide, Casein kinase II, alpha 1 related sequence 4, Cell cycle regulated protein kinase, Chromobox 1, Chromobox homolog 1 (HP1 beta homolog Drosophila ), Chromobox protein homolog 1, Class 2 alpha polypeptide, Cpk m, Csnk2a1-rs4, Cytokine Inducible Kinase, Cytokine-inducible serine/threonine-protein kinase, DKFZp686L193, DKFZp779K1237, DNA PK, DNA-PK catalytic subunit, DNA-PKcs, DNA-dependent protein kinase catalytic subunit, DNPK 1, Drosophila HP1 beta, FGF-inducible kinase, FK506 binding protein 12 rapamycin associated protein 1, FK506 binding protein 12 rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, FLJ43934, FLJ44809, FNK, FRAP, FRAP1, FRAP2, G5A, GRB 1, GSK-3 beta, GSK3B_HUMAN, GSK3beta isoform, Glycogen synthase kinase-3 beta, HP1 beta, HP1 beta homolog, HP1 beta homolog Drosophila, HP1, Drosophila. homolog of, beta, HP1Hs beta, HTR 2, HTR 2A, HTR2, formerly, HTR2C, HYRC, HYRC 1, Heterochromatin protein 1 beta, Heterochromatin protein 1 homolog beta, Heterochromatin protein p25, Htr 2b, Htr1c, Human heterochromatin protein p25 mRNA complete cds, Hyper radiosensitivity of murine scid mutation, complementing 1, Hyperradiosensitivity complementing 1, mouse, homolog of 1, IMD14, IMD26, Kid 1, Kinase induced by depolarization, M31, MCAP, MCM, MCMTC, MGC102141, MGC133043, MGC138222, MGC138224, MGC142161, MGC142163, MGC142218, MOD 1, MTOR_HUMAN, Mammalian target of rapamycin, Mechanistic target of rapamycin, Modifier 1 protein, NP75 protein, ONCOGENE PIM3, OTTHUMP00000001983, OTTHUMP00000216901, OTTHUMP00000216904, OTTHUMP00000231763, OTTMUSP00000016898;, Oncogene PIM 1, P3C2A_HUMAN, P3C2B_HUMAN, P85A_HUMAN, PI 3 Kinase catalytic subunit alpha, PI 3 Kinase catalytic subunit gamma, PI3 kinase, PI3 kinase p110 subunit alpha, PI3 kinase p110 subunit beta, PI3 kinase p110 subunit delta, PI3 kinase p110 subunit gamma, PI3 kinase p85, PI3 kinase p85 subunit alpha, PI3-K-C2(ALPHA), PI3-K-C2A, PI3-kinase regulatory subunit alpha, PI3-kinase subunit alpha, PI3-kinase subunit beta, PI3-kinase subunit delta, PI3-kinase subunit gamma, PI3-kinase subunit p85-alpha, PI3CG, PI3K, PI3K p85, PI3K regulatory subunit alpha, PI3K-C2-alpha, PI3K-C2-beta, PI3K-alpha, PI3K-beta, PI3K-delta, PI3K-gamma, PI3KC A, PI3KCB, PIK3, PIK3C 2A, PIK3C A, PIK3C1, PIK3R1, PIM, PIM1_HUMAN, PIM3_HUMAN, PK3CA_HUMAN, PK3CB_HUMAN, PK3CD_HUMAN, PK3CG_HUMAN, PKRDC, PLK, PLK1_HUMAN, PLK3_HUMAN, PRKDC_HUMAN, PTDINS-3-kinase, PTDINS-3-kinase C2 beta, Phosphatidylinositol 3 kinase catalytic alpha polypeptide, Phosphatidylinositol 3 kinase associated p 85 alpha, Phosphatidylinositol 3 kinase catalytic 110 KD alpha, Phosphatidylinositol 3 kinase catalytic 110 kD gamma, Phosphatidylinositol 3 kinase catalytic beta polypeptide, Phosphatidylinositol 3 kinase catalytic delta polypeptide, Phosphatidylinositol 3 kinase class 2 alpha, Phosphatidylinositol 3 kinase gamma, p110 gamma, Phosphatidylinositol 3 kinase regulatory 1, Phosphatidylinositol 3 kinase, catalytic, gamma polypeptide, Phosphatidylinositol 3 kinase, regulatory subunit, polypeptide 1 (p85 alpha), Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha, Phosphatidylinositol 3-kinase regulatory subunit alpha, Phosphatidylinositol 4 5 bisphosphate 3 kinase 110 kDa catalytic subunit beta, Phosphatidylinositol 4 5 bisphosphate 3 kinase 110 kDa catalytic subunit gamma, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit alpha, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit alpha isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit beta isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit delta isoform, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit gamma, Phosphatidylinositol 4 5 bisphosphate 3 kinase catalytic subunit gamma isoform, Phosphatidylinositol 4,5 bisphosphate 3 kinase 110 kDa catalytic subunit alpha, Phosphatidylinositol 4,5 bisphosphate 3 kinase 110 kDa catalytic subunit delta, Phosphatidylinositol 4,5 bisphosphate 3 kinase, catalytic subunit delta, Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit beta, Phosphatidylinositol-4, Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha, Phosphoinositide 3 kinase B, Phosphoinositide 3 kinase C, Phosphoinositide 3 kinase catalytic alpha polypeptide, Phosphoinositide 3 kinase catalytic beta polypeptide, Phosphoinositide 3 kinase catalytic delta polypeptide, Phosphoinositide 3 kinase class 2 alpha, Phosphoinositide 3 kinase gamma catalytic subunit, Phosphoinositide 3 kinase, catalytic, delta polypeptide variant p37delta, Phosphoinositide 3 kinase, class 2, alpha polypeptide, Phosphoinositide 3 kinase, regulatory subunit 1 (alpha), Phosphoinositide 3-Kinase class 2, beta, Phosphoinositide 3-Kinase-C2-alpha, Phosphoinositide 3-Kinase-C2-beta, Phosphoinositide-3-k, Phosphoinositide-3-kinase catalytic gamma polypeptide, Phosvitin, Pik3cb, Pik3cd, Pik3cg, Pim 1 kinase, Pim 1 oncogene, Pim 3 oncogene, Pim-3 proto-oncogene, serine/threonine kinase, Polo-like kinase 1, Polo-like kinase 3, Proliferation-related kinase, Protein G5a, Protein Kinase DNA Activated Catalytic Polypeptide, Protein kinase Kid 1, Proto-oncogene serine/threonine-protein kinase Pim-1, Proviral integration site 1, Proviral integration site 2, PtdIns 3 kinase p110, PtdIns 3 kinase p85 alpha, PtdIns-3-kinase C2 subunit alpha, PtdIns-3-kinase C2 subunit beta, PtdIns-3-kinase regulatory subunit alpha, PtdIns-3-kinase regulatory subunit p85-alpha, PtdIns-3-kinase subunit alpha, PtdIns-3-kinase subunit beta, PtdIns-3-kinase subunit delta, PtdIns-3-kinase subunit gamma, PtdIns-3-kinase subunit p110-alpha, PtdIns-3-kinase subunit p110-beta, PtdIns-3-kinase subunit p110-delta, PtdIns-3-kinase subunit p110-gamma, RAFT1, RAPT1, RP23-452D3.3, Rapamycin and FKBP12 target 1, Rapamycin associated protein FRAP2, Rapamycin target protein, Rapamycin target protein 1, SEROTONIN 5HT2B RECEPTOR, STPK 13, Serine/threonine kinase Pim 3, Serine/threonine protein kinase PIK3CA, Serine/threonine protein kinase PIK3CG, Serine/threonine-protein kinase 13, Serine/threonine-protein kinase GSK3B, Serine/threonine-protein kinase PLK1, Serine/threonine-protein kinase PLK3, Serine/threonine-protein kinase Pim-3, Serine/threonine-protein kinase mTOR, Serotonin 5-HT-2C receptor, Serotonin receptor 2A, Serotonin receptor 2B, Serotonin receptor 2C, Stomach fundus serotonin receptor, XRCC 7, caPI3K, chromobox homolog 1, dJ576K7.1 (FK506 binding protein 12 rapamycin associated protein 1), heterochromatin protein p25 beta, p110 BETA, p110 alpha, p110 gamma, p110D, p110delta, p110dp85a, p120-PI3K, p25beta, p350, p460, p85, p85-ALPHA, phosphatidylinositol 3-kinase C2 domain-containing beta polypeptide, phosphatidylinositol-4-phosphate 3-kinase, catalytic subunit type 2 beta, phosphoinositide-3-kinase, class 2, beta polypeptide, pim 1 kinase 44 kDa isoform, pim 1 oncogene (proviral integration site 1), serotonin 1c receptor, serotonin 2c receptor, serotonin 5-HT-2 receptor, formerly, serotonin 5-HT-2A receptor
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MW 307.3 Da, Purity >99%. A highly selective inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 μM). Selective over a range of other kinases including protein kinase C, protein kinase A, MAPK and PI4- kinase (IC50 > 50 μM).
Key facts
- CAS number
- 154447-36-6
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 307.3 Da
- Molecular formula
- C19H17NO3
- PubChem identifier
- 3973
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 25 mM and in ethanol to 5 mM.
- Biochemical name
- 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
- Biological description
A highly selective inhibitor of phosphatidylinositol 3-kinase (IC50 = 1.4 μM). Selective over a range of other kinases including protein kinase C, protein kinase A, MAPK and PI4- kinase (IC50 > 50 μM).
- Canonical SMILES
- C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
- InChI
- InChI=1S/C19H17NO3/c21-17-13-18(20-9-11-22-12-10-20)23-19-15(7-4-8-16(17)19)14-5-2-1-3-6-14/h1-8,13H,9-12H2
- InChIKey
- CZQHHVNHHHRRDU-UHFFFAOYSA-N
- IUPAC name
- 2-morpholin-4-yl-8-phenylchromen-4-one
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
The PI3 kinase family is a group of enzymes involved in key cellular functions and it includes members like PI3 Kinase p110 beta p110 delta PI3K p85 alpha Class 2A (Cpk) and the catalytic subunit gamma (PI3K-gamma) as well as PIK3C2B. These kinases belong to the phosphoinositide 3-kinase (PI3K) family which are lipid kinases known for their role in phosphorylation of the 3' hydroxyl group of the inositol ring of phosphoinositides. They vary in mass for instance PIK3C2B has a mass of approximately 200 kDa. These kinases express widely across tissues with each subtype favoring certain tissues—for example PI3K-gamma is abundant in leukocytes.
- Biological function summary
PI3 kinase enzymes regulate various cellular functions such as growth proliferation and survival. They often function as part of a complex like the PI3K heterodimer which includes regulatory subunits like p85 alpha. The enzymes are important for cellular processes that involve signal transduction from cell surface receptors to downstream effectors resulting in metabolic and gene expression changes. These kinases interact with other signaling proteins to exert influence on the cell’s behavior in response to external stimuli often through the generation of second messengers.
- Pathways
PI3 kinase plays a significant role in the PI3K/AKT signaling pathway a critical pathway for regulating the cell cycle. This pathway includes key proteins like AKT a serine/threonine-specific protein kinase also known as protein kinase B (PKB). PI3 kinase also interacts with the mTOR (mechanistic target of rapamycin) pathway which influences cell growth and metabolism in response to nutrients and other growth signals. PI3K inhibitors like LY294002 and its hydrochloride form target this pathway to modulate signaling and offer therapeutic potential.
- Associated diseases and disorders
PI3 kinase is linked to a variety of conditions notably cancer and diabetes due to its role in cell growth and survival. Dysregulation of the PI3K/AKT pathway often leads to oncogenesis and abnormalities in this pathway relate closely with mutated proteins such as PIK3CA PTEN and AKT in various cancers. In diabetes altered PI3K signaling contributes to insulin resistance affecting glucose metabolism. The relationship of PI3 kinase with these proteins in disease contexts highlights its promise as a therapeutic target for PI3K inhibitors.
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2 product images
Chemical Structure - LY 294002, PI3-kinase inhibitor (ab120243)
2D chemical structure image of ab120243, LY 294002, PI3-kinase inhibitor
Western blot - LY 294002, PI3-kinase inhibitor (ab120243)
Performed under reducing conditions; Samples loaded at 30 µg/lane. Membrane blocking and secondary antibody incubation performed in 5% milk/PBST. Primary antibody incubation performed in 5% BSA/PBST.
Lane 1: Marker
Lane 2: A431 lysate starved
Lane 3: A431 lysate starved treated with 100 ng/mL of EGF for 30 min
Lane 4: A431 lysate starved and pretreated for 2 hours with 10µM U0126 (U0126, Selective MKK inhibitor ab120241)
Lane 5: A431 lysate starved and pretreated for 2 hours with 30µM Ly294002 (ab120243)
Primary: AKT/MAPK signaling pathway antibody cocktail at 1/250 dilution
Secondary: HRP conjugated Goat anti-Rabbit secondary antibody at 1:10,000 dilution.
Observed bands:
RSK1p90 (pS380) band size: 83 kDa
AKT1 (pS473) band size: 56 kDa
ERK1 (pY204) and ERK2 (pY187) band size: 43 kDa
RPS6 (pS235/236) band size: 31 kDa
Rab11a band size: 24 kDa
Unknown band: 130kDa
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