Product Introduction
LY294002 is a potent, cell-permeable, and reversible inhibitor of phosphatidylinositol 3-kinase (PI3K) with an IC₅₀ of 1.4 µM for the p110¦Á catalytic subunit. As a first-generation, broad-spectrum PI3K inhibitor, LY294002 acts by competitively binding to the ATP-binding site of the enzyme, thereby blocking the production of phosphatidylinositol-3,4,5-trisphosphate (PIP3) and inhibiting downstream signaling through the PI3K/Akt/mTOR pathway. LY294002 has been extensively used in cell biology and pharmacology research to elucidate the role of PI3K signaling in cell proliferation, survival, metabolism, and motility. It induces apoptosis and cell cycle arrest in a wide variety of cancer cell lines and sensitizes cells to chemotherapeutic agents and radiation. Additionally, LY294002 has been shown to inhibit other PI3K-related kinases including DNA-PK and mTOR at higher concentrations, making it a valuable but promiscuous pharmacological tool for dissecting PI3K-dependent and independent signaling mechanisms.
Product Features
1. Potent PI3K Inhibitor: Broad-spectrum inhibitor of class I PI3K isoforms with IC₅₀ of 1.4 µM for p110¦Á, competitively targeting the ATP-binding site.
2. Cell-Permeable: Readily crosses cell membranes, enabling effective intracellular PI3K inhibition in live-cell assays.
3. Extensive Literature Validation: One of the most widely cited PI3K inhibitors with established protocols across diverse cell types and experimental systems.
4. Chemosensitizing Activity: Enhances the cytotoxicity of chemotherapeutic agents and ionizing radiation in multiple cancer models.
5. High Purity: Supplied at ¡Ý98% purity for reproducible pharmacological studies.
Specifications
Size: Available in 5 mg, 10 mg, 100 mg, and 500 mg
CAS Number: 154447-36-6
Molecular Weight: 307.34
Molecular Formula: C19H17NO3
Purity: ¡Ý98%
Solubility: DMSO: ¡Ý25 mg/mL; Ethanol: ¡Ý5 mg/mL; aqueous buffers: limited solubility
Storage and Stability
Storage Conditions: Store at -20¡ãC, protected from light and moisture.
Shelf Life: The product is stable for 24 months from the date of manufacture when stored as directed. For reconstituted solutions, aliquot and store at -20¡ãC. Avoid repeated freeze-thaw cycles.
Protocol (For Reference Only)
Important: LY294002 is light-sensitive. Prepare stock solutions in DMSO freshly and protect from light during handling and storage.
1. Stock Solution Preparation: Dissolve LY294002 in anhydrous DMSO to prepare a concentrated stock solution (e.g., 10-50 mM). Aliquot into single-use vials and store at -20¡ãC protected from light.
2. In Vitro Working Solution Preparation: Dilute DMSO stock solution into pre-warmed culture medium to achieve working concentrations typically ranging from 10-50 µM. Limit final DMSO concentration in culture medium to ¡Ü0.1% to avoid solvent-related cytotoxicity.
3. PI3K/Akt Pathway Inhibition: For complete inhibition of the PI3K/Akt pathway, pretreat cells with LY294002 at 10-50 µM for 30-60 minutes before stimulation with growth factors or other pathway activators. Assess pathway inhibition by Western blot for phospho-Akt (Ser473), phospho-S6, or other downstream targets.
4. Apoptosis and Proliferation Assays: Treat cells with LY294002 at 10-50 µM for 24-72 hours and assess cell viability by MTT assay, apoptosis by annexin V/PI flow cytometry, or cell cycle distribution by propidium iodide staining.
5. Chemosensitization Studies: Combine LY294002 (10-25 µM) with chemotherapeutic agents or ionizing radiation at clinically relevant doses. Assess synergistic effects by clonogenic survival assays, apoptosis assays, or cell viability measurements.
Precautions
1. Protect from light during handling and storage; LY294002 is photodegradable and exposure to light reduces potency.
2. LY294002 has limited solubility in aqueous buffers; always prepare concentrated stock solutions in DMSO before dilution into culture medium.
3. Use appropriate vehicle controls in all experiments; DMSO concentration in culture medium should not exceed 0.1% to avoid solvent-related cytotoxicity.
4. LY294002 inhibits multiple PI3K-related kinases at higher concentrations (DNA-PK, mTOR); interpret results with consideration of these off-target effects or use isoform-selective PI3K inhibitors for target validation studies.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended concentration for PI3K inhibition in vitro?
A1: LY294002 at 10-50 µM effectively inhibits PI3K/Akt signaling in most cell types. For complete pathway inhibition, 50 µM is commonly used. Perform dose-response experiments to determine the optimal concentration for specific cell lines and endpoints.
Q2: How does LY294002 differ from other PI3K inhibitors?
A2: LY294002 is a first-generation, broad-spectrum PI3K inhibitor that also inhibits related kinases including DNA-PK and mTOR at higher concentrations. Newer PI3K inhibitors such as wortmannin (irreversible) or isoform-selective inhibitors (e.g., BYL-719 for p110¦Á) provide alternative pharmacological profiles. LY294002 remains widely used due to its extensive literature validation.
Q3: Does LY294002 affect signaling pathways other than PI3K?
A3: Yes. At concentrations above 20-50 µM, LY294002 inhibits DNA-PK, mTOR, and other PI3K-related kinases. Additionally, LY294002 has been reported to modulate calcium signaling and mitochondrial function independently of PI3K. Include appropriate controls and consider isoform-selective inhibitors for mechanistic studies.
Q4: Can LY294002 be used in vivo?
A4: LY294002 has been administered in rodent models via intraperitoneal injection at doses of 50-100 mg/kg. However, its relatively short half-life, limited solubility, and potential toxicity limit its utility for chronic in vivo studies. For in vivo PI3K inhibition, consider alternative inhibitors with improved pharmacokinetic profiles.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product.
Ordering Information
Catalog Number: IC-0227268
Product Name: LY294002
Size: 5 mg / 10 mg / 100 mg / 500 mg
Price: 
5 mg: CNY ¥800.00 / USD $80.00 / EUR €96.00 / JPY ¥14400.00
10 mg: CNY ¥1000.00 / USD $100.00 / EUR €120.00 / JPY ¥18000.00
100 mg: CNY ¥2500.00 / USD $250.00 / EUR €300.00 / JPY ¥45000.00
500 mg: CNY ¥7500.00 / USD $750.00 / EUR €900.00 / JPY ¥135000.00
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