LY294002

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.

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LY294002 Chemical Structure

LY294002 Chemical Structure
Molecular Weight: 307.34

Validation & Quality Control

Product Citations(29)

Customer Reviews(8)

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation.
Targets p110α [1] p110δ [1] p110β [1]
IC50 0.5 μM 0.57 μM 0.97 μM
In vitro LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
In vivo LY294002 also results 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. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]
Features

Protocol(Only for Reference)

Kinase Assay: [4]

kinase assays PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.

Cell Assay: [2]

Cell lines Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
Concentrations 0–50 μM
Incubation Time 0–48 hours
Method 1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.

Animal Study: [3]

Animal Models Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
Formulation Dissolved in DMSO plus 0.25 ml of PBS
Dosages 0–100 mg/kg
Administration Administered via i.p.
Solubility 1% DMSO/30% polyethylene glycol/1% Tween 80, , 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
1

References

[1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58.

[2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63.

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Chemical Information

Download LY294002 SDF
Molecular Weight (MW) 307.34
Formula

C19H17NO3

CAS No. 154447-36-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms SF 1101, NSC 697286
Solubility (25°C) * In vitro DMSO 36 mg/mL (117 mM)
Water <1 mg/mL (<1 mM)
Ethanol 21 mg/mL (68 mM)
In vivo 1% DMSO/30% polyethylene glycol/1% Tween 80, 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-morpholino-8-phenyl-4H-chromen-4-one

Research Area

Customer Reviews (8)


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Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Immunofluorescence
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time 1 h
Results whole ADRP levels, estimated by Western blot , decreased only in the presence of MK -2206 and LY294002. In most cases, ADRP decorated the surface of small lipid droplets and appeared as little patches on large cytoplasmic lipid droplets. With the exception of SP600125, which induced a strong ADRP coating of almost all cytoplasmic lipid droplets (although this inhibitor did not increase ADRP synthesis), variation in the distribution of ADRP at the surface of lipid droplet was difficult to estimate, notably because the signal was faint and uneven.

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Rating
Source Biochim Biophys Acta, 2012, 1823(5), 987-96. LY294002 purchased from Selleck
Method Western blot
Cell Lines HC11 cells
Concentrations 50 μM
Incubation Time
Results Addition of 50μM LY294002, a PI3-kinase inhibitor with higher stability and specificity provoked the complete arrest of PRL-induced β-casein synthesis and a drastic inhibition of that of ADRP.

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Source Molecular Oncology, 2012. LY294002 purchased from Selleck
Method Xenograft
Cell Lines SCC61, Detroit 562
Concentrations 100 mg/kg
Incubation Time 20 day
Results In female nude mice injected with SCC61 or Detroit 562 cells, both gefitinib and LY294002 inhibited tumor growth (Figure 5). However, the most effective way to inhibit tumor growth in EGFR resistant cell line tumors in vivo was to block both EGFR and PI3K activity with gefitinib and LY294002.

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Source Molecular Oncology, 2012 . LY294002 purchased from Selleck
Method Cell growth inhibition assay with MTT
Cell Lines SQ20B/SCC61/SCC35/SCC25/HN31/MSK921/Detroit 562/HN5 cell
Concentrations 10 uM
Incubation Time 4 h
Results LY294002 effectively reduced cell viability while the combination of LY294002 and gefitinib had an additive effect (Figure A).

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Source Oncogene, 2012, 31, 3277–3286. LY294002 purchased from Selleck
Method Western Blot
Cell Lines HEK-293 cells
Concentrations 30 uM
Incubation Time
Results We cultured HEK-293 cellsstably overexpressing p37d or p110d with the general PI3K –inhibitor, LY294002, or the MAPK-inhibitor, AZD6244. The inhibitors strongly affected the levels ofphosphorylated AKT S473 and ERK.

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Source Saraswati Sukumar of Johns Hopkins University School of Medicine. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations
Incubation Time 1 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

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Source Clin Cancer Res 2011 17, 7116-7126. LY294002 purchased from Selleck
Method Western blot
Cell Lines FaDu cells
Concentrations 20 μmol/L
Incubation Time 0-30 min
Results Both BGT226 and LY294002 attenuated p-AKT and p-p70 Thr389 expression after short-term treatment, whereas rapamycin diminished the phosphorylation of p70S6K but not AKT.

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Source Dr. Zhang of Tianjin Medical University. LY294002 purchased from Selleck
Method Western blot
Cell Lines T47D cells
Concentrations 0.1-20 μM
Incubation Time 24 h
Results Reduction of AKT phosphorylation in T47D cells treated with LY294002 was observed.

Product Citations (29)

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