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LY-294002 hydrochloride

Catalog No. T4079 CAS 934389-88-5

Synonyms: SF 1101, LY 294002, NSC 697286

LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.

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LY-294002 hydrochloride Chemical Structure

LY-294002 hydrochloride, CAS 934389-88-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 37.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 179.00
50 mg	In stock	$ 298.00
100 mg	In stock	$ 471.00
1 mL * 10 mM (in DMSO)	In stock	$ 68.00

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Purity: 99.95%

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Description	LY-294002 hydrochloride (NSC 697286) is a synthetic molecule inhibitor of PI3Kα/δ/β (IC50: 0.5/0.57/0.97 μM, in cell-free assays); more stable than Wortmannin in solution, and also is a blocker of autophagosome formation.
Targets&IC50	PI3Kα:0.5μM, PI3Kβ:0.97 μM, PI3Kδ:0.57μM
In vitro	LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. In these colon cancer cell lines, LY294002 shows a remarkable growth-inhibitory and apoptosis-inducing effect and decreases expression of phosphorylated Akt (Ser473)[2]. LY294002 induces diminished cytoplasmic volume and obvious nuclear pyknosis in the tumor cells. 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[3].
In vivo	LY294002 can suppress tumor growth and induce apoptosis, especially in the LoVo tumors. Thus, It shows remarkable effectiveness in the mouse peritonitis carcinoma tosa model [2]. LY294002 markedly inhibits growth and ascites formation of ovarian carcinoma [3].
Kinase Assay	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 are established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.[4]
Cell Research	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,Premix WST-1 (10 μL) is 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.[2]
Animal Research	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: i.p.[3]

Synonyms	SF 1101, LY 294002, NSC 697286
Molecular Weight	343.81
Formula	C19H17NO3·HCl
CAS No.	934389-88-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (145.43 mM)

Ethanol: 5 mM

References and Literature

1. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. 2. Semba S, et al. The in vitro and in vivo effects of 2-(4-morpholinyl)-8-phenyl-chromone (LY2942002), a specific inhibitor of phosphatidylinositol 3'-kinase, in human colon cancer cells. Clin Cancer Res. 2002 Jun;8(6):1957-63. 3. Hu L, et al. In vivo and in vitro ovarian carcinoma growth inhibition by a phosphatidylinositol 3-kinase inhibitor (LY2942002). Clin Cancer Res. 2000 Mar;6(3):880-6. 4. Gharbi SI, et al. Exploring the specificity of the PI3K family inhibitor LY2942002. Biochem J. 2007 May 15;404(1):15-21.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library PI3K-AKT-mTOR Compound Library Anti-Ovarian Cancer Compound Library Anti-Pancreatic Cancer Compound Library Anti-Cancer Metabolism Compound Library Oxidation-Reduction Compound Library Bioactive Compound Library Anti-Breast Cancer Compound Library Metabolism Compound Library

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Keywords

LY-294002 hydrochloride 934389-88-5 PI3K/Akt/mTOR signaling PI3K Phosphoinositide 3-kinase NPC tumor nuclear DNA-PK Casein Kinase Inhibitor SF 1101 CNE-2Z Human inhibit LY-294002 Hydrochloride Lysophosphatidic acid nasopharyngeal DNA-dependent protein kinase Leptin NSC-697286 LY294002 Hydrochloride phosphatidylinositol 3-kinase spermatozoa broad-spectrum LY 294002 translocation SF1101 LY 294002 hydrochloride LY-294002 SF-1101 LY294002 LY294002 hydrochloride Apoptosis NSC697286 reversibly carcinoma LY 294002 Hydrochloride NSC 697286 inhibitor

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