LY294002

Catalog No.S1105 Batch:S110507

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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 10 mg/mL (32.53 mM)
Water Insoluble
* <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.)

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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. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 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. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. 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. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]
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. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]

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. LY294002 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.

Customer Product Validation

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

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

Data from [Data independently produced by Sci Rep, 2015, 5, 11634]

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

Selleck's LY294002 has been cited by 1905 publications

A pathological joint-liver axis mediated by matrikine-activated CD4+ T cells [ Signal Transduct Target Ther, 2024, 9(1):109] PubMed: 38714712
A pathological joint-liver axis mediated by matrikine-activated CD4+ T cells [ Signal Transduct Target Ther, 2024, 9(1):109] PubMed: 38714712
Organismal metabolism regulates the expansion of oncogenic PIK3CA mutant clones in normal esophagus [ Nat Genet, 2024, 10.1038/s41588-024-01891-8] PubMed: 39169259
10-hydroxy-2-decenoic acid prevents osteoarthritis by targeting aspartyl β hydroxylase and inhibiting chondrocyte senescence in male mice preclinically [ Nat Commun, 2024, 15(1):7712] PubMed: 39231947
Non-catalytic role of phosphoinositide 3-kinase in mesenchymal cell migration through non-canonical induction of p85β/AP2-mediated endocytosis [ Nat Commun, 2024, 15(1):2612] PubMed: 38521786
Proton pump inhibitors enhance macropinocytosis-mediated extracellular vesicle endocytosis by inducing membrane v-ATPase assembly [ J Extracell Vesicles, 2024, 13(4):e12426] PubMed: 38532609
HBO1 determines SMAD action in pluripotency and mesendoderm specification [ Nucleic Acids Res, 2024, gkae158] PubMed: 38421638
PD-L1-expressing tumor-associated macrophages are immunostimulatory and associate with good clinical outcome in human breast cancer [ Cell Rep Med, 2024, 5(2):101420] PubMed: 38382468
Chemoradiotherapy-induced ACKR2+ tumor cells drive CD8+ T cell senescence and cervical cancer recurrence [ Cell Rep Med, 2024, 5(5):101550] PubMed: 38723624
EBV-associated epithelial cancers cells promote vasculogenic mimicry formation via a secretory cross-talk with the immune microenvironment [ Theranostics, 2024, 14(13):5123-5140] PubMed: 39267775

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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.

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