LY 294002 (Synonyms: LY294002/PI3K) |
| Catalog No.GC15485 |
LY294002, a well-known PI3K signaling pathway inhibitor, is the first synthetic PI3Kα, δ and β inhibitor with IC50 of 500nM, 570nM and 970nM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 154447-36-6
Sample solution is provided at 25 µL, 10mM.
- J Ethnopharmacol 314 (2023)：116637.PMID:37187363
- Food Sci Nutr 13.1 (2025)：e4656.
- Reprod Biol Endocrin 22.1 (2024)：1-13.PMID:39272165
- Faseb J 39.2 (2025)：e70314.PMID:39825721
- Brain Res (2024)：148796.PMID:38341169
- Anti Cancer Agent Me 23.17 (2023)：1944-1957.PMID:37497684
- Reprod Biol 24.3 (2024) 100898.PMID:38889545
- Eur J Pharmacol 955 (2023)：175930.PMID:37479014
- Kidney dis basel 9.1 (2023)：58-72.PMID:36756085
- Int J Mol Sci 21.16 (2020)：5687.
- Andrology-Us (2023).PMID:38095276
- Cancer Sci (2023).PMID:38071753
- J Funct Foods 114 (2024)：106076.
- Iscience (2024).
- Phytochem Lett 47 (2022)：174-179.
- Eur J Gynaecol Oncol 42.5 (2021)：957-965.
- Phytomedicine (2024)：156168.
- J Pharmacol Sci 147.4 (2021)：348-357.
LY294002, a well-known PI3K signaling pathway inhibitor, is the first synthetic PI3Kα, δ and β inhibitor with IC50 of 500nM, 570nM and 970nM, respectively. LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins[1]
When LY294002 was added to NPC cells with different concentrations, levels of phosphorylation (S473) Akt were decreased in treated NPC cells, exhibiting a dose-response effect. LY294002 markedly inhibited NPC CNE-2Z cell growth, proliferation, and induced apoptosis in vitro and in vivo[2]. The PI3k/AKT pathway is constitutively activated in a majority of human pancreatic cancer cell lines and the pathway is a promising target for therapeutic intervention. LY294002 produce apoptosis and antiproliferative effects on pancreatic carcinoma cells in vivo and in vitro[3]
LY294002(1.2 mg/kg) was given together with leptin (60 µg/kg) once daily for 14 days via the intraperitoneal (i.p.) route. The result found that body weight in leptin+LY294002-treated rats decreased significantly and STEH was higher (p < 0.001). Ratio of testicular phosphor-Akt/total Akt was significantly higher in leptin+LY294002-treated rats (p < 0.001). The adverse effects of leptin were prevented by concurrent administration of LY294002, suggest the potential involvement of the PI3K signaling pathway in leptin-induced detrimental effects on spermatozoa[4]
References:
[1]. Gharbi SI, Zvelebil MJ, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21.
[2]. Jiang H, Fan D, et al. Phosphatidylinositol 3-kinase inhibitor (LY294002) induces apoptosis of human nasopharyngeal carcinoma in vitro and in vivo. J Exp Clin Cancer Res. 2010 Apr 22;29(1):34.
[3]. Bondar VM, Sweeney-Gotsch B, et al. Inhibition of the phosphatidylinositol 3'-kinase-AKT pathway induces apoptosis in pancreatic carcinoma cells in vitro and in vivo. Mol Cancer Ther. 2002 Oct;1(12):989-97. PMID: 12481421.
[4]. Almabhouh FA, et al. LY294002, a PI3K pathway inhibitor, prevents leptin-induced adverse effects on spermatozoa in Sprague-Dawley rats. Andrologia. 2019 Apr;51(3):e13196.
| Kinase experiment [1]: | |
|
Preparation Method |
PI3K inhibition by LY294002 was determined in a radiometric assay using purified, recombinant enzymes (class IA and class IB) with 1 µM ATP. The kinase reaction was carried out for 1 h at room temperature (24 ℃) and was terminated by addition of PBS. |
|
Reaction Conditions |
10µM, 1 h at room temperature |
|
Applications |
LY294002 not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets unrelated to the PI3K family. |
| Cell experiment [2]: | |
|
Cell lines |
K562 |
|
Reaction Conditions |
10µM/L，incubate for 24 and 48h at 37 ℃, 5% CO2 |
|
Applications |
LY294002 and DNR were able to inhibit the growth of K562 cells and promote apoptosis in time- and concentration-dependent manner (P＜0.05), both the cell proliferation-inhibiting rate and apoptosis rate in combination therapy group were higher than that in DNR-monotherapy group (P＜0.05). After K562 cells treated by LY294002 combined DNR for 36 h, the cells were statistically significantly reduced in G2/M phase (P＜0.05), as compared with control group and DNR group. Compared with DNR group, the cell level of G0/G1 phase raised (P＜0.05) and cell level of S phase decreased (P＞0.05). Compared with DNR group, the expression of SKP2 and BCL-2 mRNA decreased, and the expression of P27 mRNA increased in the combination therapy group (P＜0.05). |
| Animal experiment [3]: | |
|
Animal models |
Male Wistar rats, weighting 180~200g |
|
Preparation Method |
Rats were randomly separated into four groups (with 10 rats in each group): control group, DOI treated group, DOI treated with tiapride group, DOI treated with LY294002 group. Tourette Syndrome was induced in rats by DOI intraperitoneal injection at dosage of 1 mg/kg, once daily for 21 days continuously. |
|
Dosage form |
25µg/kg dissolved in 10% dimethyl sulfoxide，intracerebroventricularly injected |
|
Applications |
LY294002 treatment significantly relieved Tourette syndrome induced by DOI, 5HT2A/c receptor agonist and reduced PI3K/Akt/NF-κB mediated neuroinflammation. |
|
References: [1]. Gharbi SI, Zvelebil MJ, et al. Exploring the specificity of the PI3K family inhibitor LY294002. Biochem J. 2007 May 15;404(1):15-21. [2]. Geng YH, Wu WJ, et al. LY294002 Enhaces Chemosensitivity of K562 Cells to Daunorubicin. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2020 Feb;28(1):110-118. [3]. Hongyan L, et al. LY294002, a PI3K inhibitor, attenuates Tourette syndrome in rats. Metab Brain Dis. 2017 Oct;32(5):1619-1625. |
|
| Cas No. | 154447-36-6 | SDF | |
| Synonyms | LY294002/PI3K | ||
| Chemical Name | 2-morpholin-4-yl-8-phenylchromen-4-one | ||
| Canonical SMILES | C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4 | ||
| Formula | C19H17NO3 | M.Wt | 307.34 |
| Solubility | ≥ 40.37mg/mL in DMSO, ≥ 13.55mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2537 mL | 16.2686 mL | 32.5373 mL |
| 5 mM | 0.6507 mL | 3.2537 mL | 6.5075 mL |
| 10 mM | 0.3254 mL | 1.6269 mL | 3.2537 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
Aligned hMSCs arrangement promoted osteogenic differentiation by activating the PI3K-AKT signaling pathway and stimulating cytoskeleton tension.e) Fluorescent images showing the morphology of hMSCs on the aligned group after using LY294002. F-actin was stained red, Focal adhesion was stained green, and nuclei were stained blue.
The PI3K broad spectrum inhibitor LY294002 (1 mM,Glpbio, USA) concentration used was 1 and 10 μM.
Advanced Healthcare Materials (2023): 2202868. PMID: 37171209 IF: 9.9995 -
Related Biological Data
PI3K inhibitor (PI3Ki) could depress the proliferative and migratory phenotype of SCs induced by EC-EXO. C Representative EdU staining images in different groups.
LY294002, a PI3K inhibitor (PI3Ki, GLPBIO) was also used as a well-known PI3K signaling pathway inhibitor.
Journal of Nanobiotechnology 21.1 (2023): 1-25. PMID: 36624511 IF: 9.4287 -
Related Biological Data
NMU regulates glycolytic metabolism in tumor cells through the PI3K/AKT signaling pathway.(C, D) Panc02 cells were stimulated with 10 ng/mL NMU recombinant proteins for 24 h in the presence or absence of 30 μM PI3K inhibitor. The activities of PK and LDH in tumor cells as well as the concentration of lactic acid in the supernatants were measured using detection kits.
Meanwhile, 30 μM inhibitor LY294002 (GlpBio GC15485, USA) was utilized for blockade of PI3K activity in the cultured Panc02 cells.
Cancer Science (2023) PMID: 38071753 IF: 5.6998 -
Related Biological Data
Fucoidan protects muscle atrophy in T2DM rats and PA-induced C2C12 myotubes through activating PI3K. (I) Relative mRNA expression of PI3K p85, Atrogin-1 and MuRF1 in C2C12 cells.
PI3K inhibitor (LY 2940002, Cat. no.GC15485) was obtained from Glpbio (Montclair, CA, USA).
Journal of Functional Foods 114 (2024): 106076. IF: 5.5999 -
Related Biological Data
Effects of ZSD on inflammatory signaling pathways.In the same way, ZSD regulated STAT3, NF-κB, and HIF-1α mRNA expression (C) and p–NF–kB, p-STAT3, and HIF-1α protein expression (D).
ZSD-H + LY294002 group(rats were intranasal administration of LY294002 (2 mg/kg) 2 h before each OVA atomization inhalation, then gavage ZSD-H (3.7 g/kg/day)).
Journal of Ethnopharmacology 314 (2023): 116637. PMID: 37187363 IF: 5.3999 -
Related Biological Data
CircMYOF facilitates glycolysis via the PI3K/AKT pathway in PDA. A, B Overexpression of circMYOF enhanced glucose uptake (A) and lactate production (B), and LY294002 counteracted the enhancing effect of circMYOF.
Cells incubated with LY294002 (10 μM) for 24 h before the following experiments.
Cell Death Discovery 7.1 (2021): 1-11. PMID: 34811346 IF: 5.242
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *