LY294002 | CAS:154447-36-6 | Manufacturer ChemFaces

LY294002

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Description:

LY294002 (SF 1101, NSC 697286) 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. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.

Targets:

CK2 | PI3Kα/δ/β | Autophagy

In vitro:

Biochem J. 2007 May 15; 404(Pt 1): 15–21.

Exploring the specificity of the PI3K family inhibitor LY294002[Pubmed: 17302559]

The PI3Ks (phosphatidylinositol 3-kinases) regulate cellular signalling networks that are involved in processes linked to the survival, growth, proliferation, metabolism and specialized differentiated functions of cells. The subversion of this network is common in cancer and has also been linked to disorders of inflammation.
METHODS AND RESULTS:
The elucidation of the physiological function of PI3K has come from pharmacological studies, which use the enzyme inhibitors Wortmannin and LY294002, and from PI3K genetic knockout models of the effects of loss of PI3K function. Several reports have shown that LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. Since this inhibitor still remains a drug of choice in numerous PI3K studies (over 500 in the last year), it is important to establish the precise specificity of this compound. We report here the use of a chemical proteomic strategy in which an analogue of LY294002, PI828, was immobilized onto epoxy-activated Sepharose beads. This affinity material was then used as a bait to fish-out potential protein targets from cellular extracts. Proteins with high affinity for immobilized PI828 were separated by one-dimensional gel electrophoresis and identified by liquid chromatography–tandem MS.
CONCLUSIONS:
The present study reveals that LY294002 not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family.

LY294002 Description

Source:	Chemical synthesis
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Biochem J,2007 May 15;404(1):15-21.

Exploring the specificity of the PI3K family inhibitor LY294002.[Pubmed: 17302559]

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 Research:

Clin Cancer Res,2002 Jun;8(6):1957-63.

The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY294002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells.[Pubmed: 12060641]

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 Research:

Clin Cancer Res,2000 Mar;6(3):880-6.

In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY294002).[Pubmed: 10741711]

Animal Models: Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
Dosages:0–100 mg/kg
Administration: Administered via i.p.

Product Name	LY294002
Price:
CAS No.:	154447-36-6
Catalog No.:	CFN60015
Molecular Formula:	C₁₉H₁₇NO₃
Molecular Weight:	307.34 g/mol
Purity:	>=98%
Type of Compound:	Alkaloids
Physical Desc.:	Powder
Source:	Chemical synthesis
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS
Similar structural:	Comparison
Guestbook:

Size /Price /Stock	10 mM * 100 uL in DMSO / Inquiry / In-stock 10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries	Alkaloids Compound Library Autophagy Inhibitor Library

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	3.2537 mL	16.2686 mL	32.5373 mL	65.0745 mL	81.3431 mL
5 mM	0.6507 mL	3.2537 mL	6.5075 mL	13.0149 mL	16.2686 mL
10 mM	0.3254 mL	1.6269 mL	3.2537 mL	6.5075 mL	8.1343 mL
50 mM	0.0651 mL	0.3254 mL	0.6507 mL	1.3015 mL	1.6269 mL
100 mM	0.0325 mL	0.1627 mL	0.3254 mL	0.6507 mL	0.8134 mL

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