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LY294002

Cat. No. M1925
LY294002 Structure
Synonym:

NSC 697286; SF 1101

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 43  USD43 In stock
5mg USD 35  USD35 In stock
10mg USD 54  USD54 In stock
50mg USD 90  USD90 In stock
100mg USD 135  USD135 In stock
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Quality Control & Documentation
Biological Activity

LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitor that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an apoptosis activator. LY294002 inhibits proliferation and induces apoptosis in human colon cancer cells in vitro and in vivo. PI3K inhibitor LY294002 prevents the induction of both D-type cyclin mRNA and protein in T-lymphoblasts, while rapamycin inhibits the induction of protein. LY294002 significantly decreased the activities of Cdk2 and E2F in mES cells. LY294002 induced accumulation of cells in G(1) phase followed by apoptotic cell death. LY294002 also resultes in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model.

Product Citations
Customer Product Validations & Biological Datas
Source J Cell Physiol (2018). Figure 3. LY294002 (AbMole Bioscience Inc.)
Method injected
Cell Lines rats
Concentrations
Incubation Time 72 h
Results The LY294002 group had increased infarct size (p < 0.05); while no such significantdifference was found in the ANXA3-shRNA + LY294002 group
Source Experimental Eye Research (2018). Figure 3. LY294002 (Abmole Bioscience, Houston, TX, USA)
Method Western blot
Cell Lines ONH astrocytes
Concentrations 50 μM
Incubation Time 1 h
Results PD98059 did not significantly reduce the level of p-S6 kinase phosphorylation, but LY294002 showed a robust blockade of its phosphorylation.
Source Journal of Nanchang University (2017). Figure 5. LY294002 (Abmole Bioscience)
Method Western Blotting
Cell Lines A549 Cell
Concentrations 20 μM
Incubation Time 24 h
Results Western Blotting检测结果显示，LY294002处理组的PI3K，p-AKT的表达比对照组显著降低（均P < 0.05）。
Source Journal of Nanchang University (2017). Figure 4. LY294002 (Abmole Bioscience)
Method Western Blotting
Cell Lines A549 Cell
Concentrations 20 μM
Incubation Time 24 h
Results Western Blotting检测结果显示，LY294002处理的A549细胞中Beclin-1蛋白表达和LC3B（Ⅱ／Ⅰ）比率比对照组显著降低（均P < 0.05）。
Source Journal of Nanchang University (2017). Figure 3. LY294002 (Abmole Bioscience)
Method Wound Healing assay
Cell Lines A549 Cell
Concentrations 20 μM
Incubation Time 24 h
Results Wound Healing实验结果显示，LY294002处理组细胞24h迁徙率为（22.4±2.6）%，显著低于对照组（39.1±3.2）%（P < 0.05）。
Source Journal of Nanchang University (2017). Figure 2. LY294002 (Abmole Bioscience)
Method Transwell assay
Cell Lines A549 Cell
Concentrations 20 μM
Incubation Time 24 h
Results Transwell侵袭实验结果显示，LY294002处理组侵出小室的细胞数为（95±7）个/膜，显著低于对照组（130±16）个/膜（P < 0.05）。
Source Int Immunopharmacol. (2017). Figure 6. LY294002 (Abmole Bioscience, Hong Kong, China)
Method qRT-PCR
Cell Lines Th1 and Th17 cells
Concentrations 50 mg/kg
Incubation Time
Results Western blot and quantitative RT-PCR analysis revealed that OMT and LY294002 treatment resulted in dramatic reduction of Tbet and ROR-γt (Fig. 6A and B).
Source Int Immunopharmacol. (2017). Figure 5. LY294002 (Abmole Bioscience, Hong Kong, China)
Method Flow cytometry
Cell Lines CD4+ T cells
Concentrations 50 mg/kg
Incubation Time
Results OMT and LY294002 reduced the percentage of Th1-polarized and Th17-polarized CD4+ T cells (Fig. 5A and B).
Source Int Immunopharmacol. (2017). Figure 2. LY294002 (Abmole Bioscience, Hong Kong, China)
Method Western blot
Cell Lines Specific pathogen-free (SPF) male BALB/c mice
Concentrations 50 mg/kg
Incubation Time
Results Whereas, OMT and LY294002 triggered apoptosis by activated cleaved-caspase3 and cleaved-caspase9 and lowed the expression of Bcl-2 and Bad in colonic tissues (Figs. 2A, B and 3).
Source Int Immunopharmacol. (2017). Figure 1. LY294002 (Abmole Bioscience, Hong Kong, China)
Method Evaluate DAI
Cell Lines Specific pathogen-free (SPF) male BALB/c mice
Concentrations 50 mg/kg
Incubation Time
Results Meanwhile, the DAI score and histological score, reflecting the severity of UC, also decreased obviously in the OMT and LY294002 treated groups (Fig. 1E and F).
Source BMC Genomics (2017). Additional file 7. LY294002 (Abmole Bioscience, USA)
Method qRT-PCR
Cell Lines pupa abdomen
Concentrations
Incubation Time 48 h
Results We performed injection experiments involving several inhibitors of the insulin signaling pathway. It was observed that the development of follicles was clearly delayed and the follicles showed abnormalities (Additional file 7), and the expressions of marker genes, like Cyp18a1 and early chorion gene, were up-regulated at choriogenic stages.
Source Oncology research (2016). Figure 4. LY294002 (Abmole Bioscience, Shanghai, China)
Method MTT assay
Cell Lines MKN-28 and SGC-7901 cells
Concentrations 200 nM
Incubation Time 12 h
Results The Rap1b silencinginduced enhancement of apoptosis and autophagy in MKN-28 and SGC-7901 cells was enhanced by LY294002 but was blocked by IGF-1 treatment (Fig. 4B and C).
Source Mol Immunol (2017) . Figure 5. LY294002 (Abmole Bioscience, USA)
Method LC3 in SMMC-7721 and Huh-7 cells treated with IL-37 (100 ng/ml) or LY294002 (20 μmol/l).
Cell Lines SMMC-7721 and Huh-7 cells
Concentrations 20 μmol/l
Incubation Time
Results The expression of p-AKT and p-mTOR was decreased and the LC3-II/LC3-I ratio was increased in IL-37 treated LY294002-treated SMMC-7721 and Huh-7 cells. The mediated effects of IL-37 on autophagy were similar to those of the inhibitor LY294002 (Fig. 5D).
Source Biochem Pharmacol (2015). LY294002, Figure 5. (Abmole Bioscience Kowloon, Hong Kong, China)
Method Western blot
Cell Lines CD4+ T cells
Concentrations 20 mM
Incubation Time 24 h
Results Fig. 5B showed that PI3K inhibitor LY294002 markedly suppressed p70S6K and RPS6 phosphorylation.
Source Oncotarget (2016). Figure 11. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).
Method western blot
Cell Lines MDA-MB-231 cells
Concentrations PI3K (10 µM LY294002), Akt (10 µM MK-2206) or mTOR (10 µM rapamycin)
Incubation Time 1h
Results As shown in Figure 11. Pretreating MDA-MB-231 cells with the specific inhibitors of PI3K (10 µM LY294002), Akt (10 µM MK-2206) and mTOR (10 µM rapamycin) completely abolished the LSS-induced MT1-MMP expression, indicating that the PI3K/Akt/mTOR pathway is required for LSS-induced MT1-MMP expression.
Source Oncotarget (2016). Figure 1. Inhibitors of PI3K (LY294002), Akt (MK-2206), Src (PP2), FAK (PF573228) and mTOR (rapamycin) were purchased from Abmole Bioscience (Houston, TX, USA).
Method Cell motility assay
Cell Lines MDA-MB-231 cells
Concentrations PI3K (10 μM LY294002), Akt (20 μM MK-2206), mTOR (10 μM rapamycin, Rap), FAK (10 μM PF573228) or Src (10 μM PP2)
Incubation Time 1h
Results "Notably, inhibitors of PI3K (LY294002), Akt (MK-2206) and mTOR (rapamycin) markedly decreased the LSS-induced wound closure activity. However, pretreatment with inhibitors of FAK (PF573228) and Src (PP2) has no effect on the LSS-induced cell motility (Figure 1B). It is suggested that PI3K, Akt and mTOR might be participated LSS-induced cell motility in an FAK and Src-independent manner. "
Source Biochemical Pharmacology (2015). Figure 7. LY294002, MK-2206 and GSK1120212 were gifts from Abmole Bioscience (Kowloon, Hong Kong).
Method Western blot
Cell Lines Purified CD4+ T cells
Concentrations 20 mM LY294002, 10 mM MK-2206 as well as 10 mM GSK1120212
Incubation Time 3 h
Results Arctigenin could inhibit mTORC1 activation via a way independent of PI3K/AKT and ERK.
Source International Immunopharmacology (2015). Figure 7. LY294002 (an inhibitor of GSK3 phosphorylation) was purchased from Abmole Bioscience (Kowloon, Hong Kong)
Method (A) Level of IL-10 was detected by using ELISA assay. (B) Levels of p-GSK3β (Ser9) and GAPDH were detected by using Western blot assay.
Cell Lines RAW 264.7 cells
Concentrations 5 µM
Incubation Time 24 hours
Results LY294002 (5 μM) obviously diminished DGA-mediated IL-10 expression in LPS-stimulated RAW 264.7 cells
Protocol (for reference only)
Cell Experiment
Cell lines DLD-1, LoVo
Preparation method Cells were seeded at a density of 1.0×105 cells/well in a 96-well plate and incubated in completely fresh medium containing 0–50µM LY294002 for 24 h for proliferation assay. Western blot analysis of the level of Akt phosphorylation in DLD-1 and LoVo cells in 6-well plate.
Concentrations 10, 20, 50 µM
Incubation time 24 hours
Animal Experiment
Animal models Both DLD-1 and LoVo cancer cells models in SCID 6-week-old female mice
Formulation Dissolved in DMSO
Dosages 2.0 ng/ml/kg
Administration From days 20–40, i.v. or i.p. injection everyday
Chemical Information
Molecular Weight 307.34
Formula C19H17NO3
CAS Number 154447-36-6
Solubility (25°C) DMSO 32 mg/mL
Ethanol 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lianguzova MS, et al. Cell Biol Int. Phosphoinositide 3-kinase inhibitor LY294002 but not serum withdrawal suppresses proliferation of murine embryonic stem cells.

[2] Gharbi SI, et al. Biochem J. Exploring the specificity of the PI3K family inhibitor LY294002.

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Keywords: LY294002, NSC 697286; SF 1101 supplier, PI3K, inhibitors, activators

 
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