LY294002

Catalog No.S1105 Batch:S110508

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Technical Data

Formula

C19H17NO3
Molecular Weight 307.34 CAS No. 154447-36-6
Solubility (25°C)* In vitro DMSO 80 mg/mL (260.29 mM)
Ethanol 15 mg/mL (48.8 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%DMSO 40%PEG300 5%Tween80 50%ddH2O

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

 3.400mg/ml (11.06mM) Taking the 1 mL working solution as an example, add 50 μL of 68 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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
(Cell-free assay)		 p110α
(Cell-free assay)		 p110δ
(Cell-free assay)		 p110β
(Cell-free assay)		 DNA-PK
(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 related. This chemical demonstrates a remarkable growth-inhibitory and Apoptosis related-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 tumour 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/Akt/mTOR activation pathway and cancer cell cycle regulation.

In Vivo

LY294002 also results in suppression of tumour growth and induction of Apoptosis related, especially in the LoVo tumours, 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 (24°C) 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 ]

Sellecks LY294002 Has Been Cited by 1715 Publications

FOXM1 inhibition reduces IL-13-induced epithelial remodelling and inflammation in eosinophilic oesophagitis [ Gut, 2025, gutjnl-2025-335163] PubMed: 41266120
The intrinsic expression of NLRP3 in Th17 cells promotes their protumor activity and conversion into Tregs [ Cell Mol Immunol, 2025, 22(5):541-556] PubMed: 40195474
FGF21 protects against HFpEF by improving cardiac mitochondrial bioenergetics in mice [ Nat Commun, 2025, 16(1):1661] PubMed: 39955281
WNK1 mediates M-CSF-induced macropinocytosis to enforce macrophage lineage fidelity [ Nat Commun, 2025, 16(1):4945] PubMed: 40436823
Reversal of diet-induced obesity by central insulin sensitizer FSTL1 [ Neuron, 2025, S0896-6273(25)00749-4] PubMed: 41125083
Vitamin D Binding Protein, a Ligand of Integrin beta 1, Motivates Both Tumor Cells and Schwann Cells to Promote Perineural Invasion in Pancreatic Ductal Adenocarcinoma [ Adv Sci (Weinh), 2025, 12(44):e11726] PubMed: 40923379
X-linked myopathy with excessive autophagy: characterization and therapy testing in a zebrafish model [ EMBO Mol Med, 2025, 10.1038/s44321-025-00204-8] PubMed: 39994482
Exosomes derived from platelet-rich plasma alleviate synovial inflammation by enhancing synovial lymphatic function [ J Nanobiotechnology, 2025, 23(1):522] PubMed: 40671121
PDPN+ cancer-associated fibroblasts enhance gastric cancer angiogenesis via AKT/NF-κB activation and the CCL2-ACKR1 axis [ MedComm (2020), 2025, 6(1):e70037] PubMed: 39764562
Junctional adhesion molecule A orchestrates endothelial cell-driven angiogenesis and wound healing in diabetes [ Pharmacol Res, 2025, 217:107796] PubMed: 40436082

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