LY 294002

• CAT Number: I001950
• CAS Number: 154447-36-6
• Molecular Formula: C₁₉H₁₇NO₃
• Molecular Weight: 307.34
• Purity: ≥95%
• Synonyms: 2-morpholin-4-yl-8-phenylchromen-4-one
• Target: PI3K
• Solubility: DMSO: ≥ 49 mg/mL
• Storage: -20°C
• IC50: 0.5 μM/0.57 μM/0.97 μM (PI3Kα/δ/β)
• 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
• SMILES: C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4

LY 294002（Cat No.:I001950）is a potent and selective inhibitor of phosphoinositide 3-kinase (PI3K), a critical enzyme involved in the PI3K/Akt signaling pathway. By blocking PI3K activity, LY 294002 disrupts key cellular processes such as proliferation, survival, and metabolism, making it a widely used tool in cancer research. This compound is essential for studying the role of PI3K in tumor growth and progression, as well as exploring potential therapeutic strategies targeting PI3K-related pathways. Its versatility extends to studies on insulin signaling, neurodegenerative diseases, and inflammation.

Reference

1:PI3K inhibitor LY294002, as opposed to wortmannin, enhances AKT phosphorylation in gemcitabine-resistant pancreatic cancer cells. Wang Y, Kuramitsu Y, Baron B, Kitagawa T, Tokuda K, Akada J, Maehara SI, Maehara Y, Nakamura K.Int J Oncol. 2017 Feb;50(2):606-612. doi: 10.3892/ijo.2016.3804. Epub 2016 Dec 14. PMID: 28000865 2:[LY294002 blocks the effect of dexamethasone in reducing urine protein in rats by inhibiting PI3K/Akt signaling pathway]. Zhou ZG, Wu WL, Liu TT, Peng Y, Lao WQ, Liang M, Zhu MH.Nan Fang Yi Ke Da Xue Xue Bao. 2016 Dec 20;36(12):1727-1731. Chinese. PMID: 27998873 3:Autophagy inhibitors chloroquine and LY294002 enhance temozolomide cytotoxicity on cutaneous melanoma cell lines in vitro. Ryabaya OO, Inshakov AN, Egorova AV, Emelyanova MA, Nasedkina TV, Zasedatelev AS, Khochenkov DA, Stepanova EV.Anticancer Drugs. 2017 Mar;28(3):307-315. doi: 10.1097/CAD.0000000000000463. PMID: 27941537 4:Kinetic modelling of in vitro data of PI3K, mTOR1, PTEN enzymes and on-target inhibitors Rapamycin, BEZ235, and LY294002. Goltsov A, Tashkandi G, Langdon SP, Harrison DJ, Bown JL.Eur J Pharm Sci. 2017 Jan 15;97:170-181. doi: 10.1016/j.ejps.2016.11.008. Epub 2016 Nov 8. PMID: 27832967 5:Co-treatment of LY294002 or MK-2206 with AZD5363 Attenuates AZD5363-induced Increase in the Level of Phosphorylated AKT. Choi AR, Kim JH, Woo YH, Cheon JH, Kim HS, Yoon S.Anticancer Res. 2016 Nov;36(11):5849-5858. PMID: 27793908 6:Comprehensive attenuation of IL-25-induced airway hyperresponsiveness, inflammation and remodelling by the PI3K inhibitor LY294002. Huang P, Li Y, Lv Z, Wang J, Zhang Q, Yao X, Corrigan CJ, Huang K, Wang W, Ying S.Respirology. 2017 Jan;22(1):78-85. doi: 10.1111/resp.12880. Epub 2016 Aug 24. PMID: 27556731 7:Phosphoinositide 3-kinase inhibitor LY294002 ameliorates the severity of myosin-induced myocarditis in mice. Liu HS, Zhang J, Guo JL, Lin CY, Wang ZW.Curr Res Transl Med. 2016 Jan-Mar;64(1):21-7. doi: 10.1016/j.retram.2016.01.012. Epub 2016 Mar 7. PMID: 27140596 8:LY294002 induces in vitro apoptosis and overexpression of p75NTR in human uterine leiomyosarcoma HTB 114 cells. Pistilli A, Rende M, Crispoltoni L, Montagnoli C, Stabile AM.Growth Factors. 2015;33(5-6):376-83. doi: 10.3109/08977194.2015.1118096. Epub 2015 Dec 10. PMID: 26653825 9:LY294002 prevents lipopolysaccharide‑induced hepatitis in a murine model by suppressing IκB phosphorylation. Chen Z, Liu H, Lei S, Zhao B, Xia Z.Mol Med Rep. 2016 Jan;13(1):811-6. doi: 10.3892/mmr.2015.4574. Epub 2015 Nov 19. PMID: 26647861 10:The effect of PI3K inhibitor LY294002 and gemcitabine hydrochloride combined with ionizing radiation on the formation of vasculogenic mimicry of Panc-1 cells in vitro and in vivo. Bai R, Ding T, Zhao J, Liu S, Zhang L, Lan X, Yu Y, Yin L.Neoplasma. 2016;63(1):80-92. doi: 10.4149/neo_2016_010. PMID: 26639237