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.
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Cas No.: 154447-36-6
Sample solution is provided at 25 µL, 10mM.
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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]: | |
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Cell lines |
K562 |
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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. |
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| 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 | |||
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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 |
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Quality Control & SDS
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- Purity: >98.00%
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Cells incubated with LY294002 (10 μM) for 24 h before the following experiments.
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