Molecular Weight(MW): 495.53
WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
Cited by 6 Publications
4 Customer Reviews
WYE-354 is cytotoxic and anti-proliferative when adding to cultured human colon cancer cells. Established human colon cancer cell lines (HCT-116, HT-29, Caco-2, LoVo, and DLD-1), three lines of primary human colon cancer cells (P1, P2, and P3), or non-cancerous NCM460 colon epithelial cells were treated with applied concentration of WYE-354 ("WYE") for indicated time period, cell survival was tested by MTT assay (a, b, d, f), and cell proliferation was evaluated by clonogenicity assay (c, e). The data in this and all following figures were representatives of three different experiments. n = 5 for each assay. The values were expressed as the means ± SD (same for all figures). "C" stands for untreated control group (same for all figures). *p<0.05 vs. "C" group
Tumour Biol, 2016, 37(9):11743-11752. WYE-354 purchased from Selleck.
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WYE-354 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.
Dr. Yong-Weon Yi from Georgetown University Medical Center. WYE-354 purchased from Selleck.
Purity & Quality Control
Choose Selective mTOR Inhibitors
|Description||WYE-354 is a potent, specific and ATP-competitive inhibitor of mTOR with IC50 of 5 nM, blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) not P-AKT(T308), selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).|
WYE-354 also inhibits several PI3Ks at micromolar levels. In HEK293 cells, WYE-354 (0.2 μM–5 μM) effectively inhibits both mTORC1 and mTORC2. WYE-354 (0.3 μM–10 μM) significantly blocks mTOR signaling and Akt activation in U87MG and MDA361 cells. Furthermore, WYE-354 potently inhibits proliferation in tumor cell lines including MDA-MB-361, MDA-MB-231, MDA-MB-468, LNCap, A498, and HCT116, with IC50 values ranging from 0.28 μM to 2.3 μM. The apoptosis induced by WYE-354 is accompanied by G1 cell cycle arrest and caspases activation.  In endothelial HUVEC cells, WYE-354 (10 nM–1 μM) also inhibits both mTORC1 and mTORC2 signaling, as revealed by dephosphorylation of S6 ribosomal protein and Akt, respectively. Furthermore, WYE-354 (10 nM–1 μM) activates mitogen-activated protein kinase (MAPK) signaling, which may be due to its inhibition of mTORC1. 
|In vivo||In a mice xenograft model of PTEN-null PC3MM2 tumor, WYE-354 (50 mg/kg) effectively inhibits mTOR signaling and tumor growth. |
mTOR inhibitor assays:The assays are performed in 96-well plates for 2 hours at room temperature in 25 μL containing 6 nM Flag-TOR(3.5), 1 μM His6-S6K, and 100 μM ATP. The assays are performed and detected by DELFIA employing the Eu-phospho-p70S6K T389 antibody. For inhibitor versus ATP matrix competition, mTOR kinase reactions are carried out with varying concentrations of ATP (0, 25, 50 100, 200, 400, and 800 μM) in combination with varying concentrations of WYE-354. The assays contained 12 nM Flag-TOR(3.5), 1 μM His-S6K, and are incubated for 30 min. The assay results are similarly detected by DELFIA and processed for generation of double-reciprocal plots.
|In vitro||DMSO||99 mg/mL (199.78 mM)|
|In vivo||Add solvents individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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