LY294002

Catalog No.S1105 Batch:S110506

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Technical Data

Formula

C19H17NO3
Molecular Weight 307.34 CAS No. 154447-36-6
Solubility (25°C)* In vitro DMSO 61 mg/mL (198.47 mM)
Ethanol 61 mg/mL (198.47 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%absolute ethyl alcohol 95%Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 1.000mg/ml (3.25mM) Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

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. This compound also inhibits CK2 with IC50 of 98 nM. It is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
Targets
CK2 [5]
(Cell-free assay)		 p110α [1]
(Cell-free assay)		 p110δ [1]
(Cell-free assay)		 p110β [1]
(Cell-free assay)		 DNA-PK [6]
(Cell-free)
98 nM 0.5 μM 0.57 μM 0.97 μM 1.4 μM
In vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. This compound is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1. It inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. This chemical demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). It induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, this compound markedly inhibits ovarian cancer cell proliferation in vitro. It 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 this chemical on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation.

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. This compound significantly inhibits growth and ascites formation of ovarian carcinoma.

Protocol (from 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. This compound 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

  • Dosages

    0–100 mg/kg

  • Administration

    Administered via i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/17362206/
  • https://pubmed.ncbi.nlm.nih.gov/12060641/
  • https://pubmed.ncbi.nlm.nih.gov/10741711/
  • https://pubmed.ncbi.nlm.nih.gov/17302559/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1868829/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3560216/

Customer Product Validation

Inhibition of PI3K, ERK and mTOR prevents the activation of S6K1 and S6 induced by suppression of PKD1 activity. A549 cells were incubated in the absence (-) or presence of either 5 uM Kb or 5 uM Kb and 20 uM LY294002 or 5 uM Kb and 10 uM BKM120 (as indicated) for 1 h prior to stimulation of cells with 50 nM PMA for 30 min and 1 h.

Data from [ Int J Biochem Cell Biol , 2015 , 60, 34-42 ]

IGF1 increases apical fibronectin in late stage blastocysts. Representative confocal images of blastocysts stained for fibronectin (Green) and DAPI (Blue). Day 5 blastocysts were cultured in SS medium for 24 (A and B), 48 (C and D) or 72 h (E-H) in the absence (A, C and E) or presence (B, D and F) of 10 ng/ml IGF1 or in the presence of a PI3 Kinase inhibitor (5 uM LY294002 + 10 ng/ml IGF1) (G) or in the presence of 10 ng/ml IGF1, attached to a coverslip (H). Scale bars represent 20 mm. Red line indicates location of coverslip. Arrow indicates location of the inner cell mass (ICM). The following total number of blastocysts were analysed, from at least 3 experimental repeats in each treatment; 24 in the SS group (24 h), 21 in SS plus IGF1 (24 h), 26 in SS (48 h), 30 in SS plus IGF1 (48 h), 40 in SS (72 h), 59 in SS plus IGF1 (72 h), 13 in SS plus IGF1 + LY294002 (48 h) and 15 blastocysts were analysed that were attached to a coverslip (72 h).

Data from [ Hum Reprod , 2015 , 30(2), 284-98 ]

PTEN transfection or inhibition of the PI3K-AKT and IGF-1R signaling pathways increases the trastuzumab sensitivity of NCI-N87/TR cells. After treating the cells with a PI3K inhibitor (LY294002), the expression of AKT and P-AKT proteins was assessed by Western blotting. Tubulin expression indicated equal loading. All gels run under the same experimental conditions and the experiments were repeated 3 times. The representative images were cropped and shown. Control: cells without any treatment.

Data from [ Sci Rep , 2015 , 5, 11634 ]

<p>Type I IFNs induce ISG expression in a serine phosphorylation-independent manner. Cells were treated with kinase inhibitors (SB203580, rottlerin, Ly294002, PD98059, and SP600125) before stimulation with IFN-a and IFN-b for 6 hours. Cell lysates were used in western blotting and probed for serine phosphorylation.The relative amounts of pSTAT1 S727 in (up-graph) were quantied and normalized to an untreated control (below-graph).</p>

Data from [ Hepatology , 2014 , 59(4), 1262-72 ]

Selleck's LY294002 Has Been Cited by 1728 Publications

Integrated Single-Cell Profiling Reveals TL1A as a Biomarker and Driver of Type 2 Inflammation via Macrophage-Dependent Immunoregulation in Asthma [ Research (Wash D C), 2026, 9:1190] PubMed: 41970030
Kdf1 Regulates Molar Cusp Morphogenesis via the PI3K/AKT/mTOR Signalling Axis [ Cell Prolif, 2026, 59(3):e70108] PubMed: 40739677
Toll signaling controls stem cell proliferation in intestinal regeneration and tumorigenesis [ EMBO Rep, 2026, 27(5):1270-1300] PubMed: 41634381
NGR1 Pretreatment Enhances the Therapeutic Efficacy of Transplanting Cardiomyocytes Derived from Human Induced Pluripotent Stem Cells for Myocardial Infarction [ Int J Mol Sci, 2026, 27(1)475] PubMed: 41516349
Omentum-Derived Mesenchymal Stem Cells Promote Antibacterial Effects and Protect Endothelial Functions via PAI-1 [ Stem Cell Rev Rep, 2026, 22(5):2491-2510.] PubMed: 42018237
SEMA4F Regulates the Malignant Phenotype of Hepatocellular Carcinoma Cells Through the PI3K-Akt Pathway [ J Hepatocell Carcinoma, 2026, 13:596827] PubMed: 42059013
Glucose‑driven TRIB3 enhances the tumorigenic potential of colon cancer via the PI3K/AKT pathway [ Mol Med Rep, 2026, 33(5)132] PubMed: 41823543
Targeting BCL-2 and PI3K signaling pathways enhances cytotoxicity of gemtuzumab ozogamicin against acute myeloid leukemia cells [ Biochem Biophys Res Commun, 2026, 817:153752] PubMed: 41980559
Elucidating the Potential Targets and Mechanisms of Bisphenol A-Induced Prostate Cancer Based on Network Toxicology and Molecular Docking Analyses [ Oncol Res, 2026, 34(5):35] PubMed: 42065064
Epigenetic Activity of Cancer Therapy Drugs Revealed by HeLa TI Cell-Based Assay [ Epigenomes, 2026, 10(1)14] PubMed: 41892363

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.

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