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LY 294002Potent PI3K inhibitor

LY 294002

Catalog No. A8250
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
10mg $50.00 In stock
50mg $70.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID:25701119

Quality Control

Chemical structure

LY 294002

Related Biological Data

LY 294002

Related Biological Data

LY 294002

Related Biological Data

LY 294002

Related Biological Data

LY 294002

Related Biological Data

LY 294002

Biological Activity

Description LY294002 is an inhibitor of PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively.
Targets p110α p110δ p110β      
IC50 0.5 μM 0.57 μM 0.97 μM      

Protocol

Cell experiment: [1]

Cell lines

OVCAR-3 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

10 μM, 24 hours

Applications

After 24 h of treatment, the number of cells in 1, 5, and 10 μM LY294002-treated wells was reduced by 27, 56, and 75%, respectively, compared to the control group. LY294002 (1–10 μM) markedly inhibited cell proliferation. When the cells were treated with 10 μM LY294002 for 24 h, the effects appeared toxic. Cellularity was decreased, and the cell clusters appeared shrunken with poor cellular cohesion. Cells had hyperchromatic, pyknotic nuclei, and the amount of cytoplasm was decreased. LY294002 induced nuclear pyknosis and diminished cytoplasmic volume, which was clearly demonstrated in the 5 μM-treated wells.

Animal experiment: [1]

Animal models

Athymic immunodeficient mice injected with OVCAR-3 cells

Dosage form

Intraperitoneal injection, 100 mg/kg body weight, daily for 3 weeks

Applications

At postmortem examination, tumors were found on the surface of the peritoneum, intestines, and uterus in both treatment and control groups. However, in the control group, tumors were also found on the diaphragm and in the hilus of the liver. LY294002 induced pyknosis and nuclear condensation, as well as reduced cytoplasmic volume in the tumor cells. Some nuclei separated from the cytoplasm. Abdominal circumference (7.2 ± 2 cm) significantly increased in the control group compared to the LY294002-treated group (6.35 ± 0.42 cm). Body weight increased in both groups for the first week after inoculation. In the control group, body weight continued to increase, whereas there was no significant change in body weight after treatment with LY294002.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Hu L, Zaloudek C, Mills G B, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clinical Cancer Research, 2000, 6(3): 880-886.

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Chemical Properties

Cas No. 154447-36-6 SDF Download SDF
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 >15.4mg/mL in DMSO Storage Store at -20°C
General tips No
Shipping Condition No

Background

LY294002 is a potent inhibitor of class I phosphoinositide 3-kinases (PI3Ks) [1, 2]. It is cell permeable and reversible, and selective against p110α, p110β, p110γ and p110δ, which acts on ATP binding site of the catalytic subunit.

PI3K family is divided into 3 classes: class I, II and III. LY294002 can inhibit 3 out of 4 isoforms of catalytic subunit of class I group. The IC50s for p110α, β andδ are 500 nM, 973 nM and 570 nM [3]. Even though it is less potent than wortmannin, other PI3K inhibitor, but it is more stable in solution. In addition, LY294002 is a reversible inhibitor whereas wortmannin acts irreversibly. [2]

PI3Ks signal through Akt, activates mTOR and inhibits Bad, leading to cell growth and proliferation. LY294002 potently inactivates PI3K class I catalytic subunit, resulting in induction of apoptosis and suppression of tumor cell growth in vitro and in vivo. [2, 4]

LY294002 is also a potent autophagy inhibitor by blocking autophagosome formation. [5]

Quantitative chemoproteomic profiling shows that LY294002 inhibits the BET bromodomain proteins BRD2, BRD3, and BRD4 with IC50 value of 1-2 µM. [6]

References:
[1]Maira et al. (2009). PI3K inhibitors for cancer treatment: where do we stand?. doi:10.1042/BST0370265.
[2]Vlahos CJ., et al. (1994). A Specific Inhibitor of Phosphatidylinositol 3-Kinase, 2-(4-Morpholinyl)-8-phenyl-4H-l-benzopyran-4-one (LY294002). Journal of Biological Chemistry 269 (7): 5241–5248.
[3]Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J, 2007, 404(3), 449-58.
[4]Hu L, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002). Clin Cancer Res, 2000, 6(3), 880-6.
[5]Blommaart EF., et al., (1997). The phosphatidylinositol 3-kinase inhibitors wortmannin and LY294002 inhibit autophagy in isolated rat hepatocytes. Eur. J. Biochem. 243: 240–246.
[6]Dittmann, A., et al. (2013). The Commonly Used PI3-Kinase Probe LY294002 is an Inhibitor of BET Bromodomains. ACS Chemical Biology: 131210150813004.