WYE-687

SKU: orb1685619

Description

WYE-687 is a potent and selective ATP-competitive mTOR inhibitor with an IC50 of 7 nM. It effectively suppresses mTORC1 and mTORC2 signaling by inhibiting pS6K(T389) and pAKT(S473), respectively, while showing high selectivity over PI3K isoforms. This inhibitor is a valuable tool for studying mTOR-dependent pathways in cancer and metabolic disease research, both in vitro and in vivo.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 1062161-90-3
• MW: 528.61
• Purity: 99.93% (May vary between batches)
• Formula: C₂₈H₃₂N₈O₃
• SMILES: COC(=O)Nc1ccc(cc1)-c1nc(N2CCOCC2)c2cnn(C3CCN(Cc4cccnc4)CC3)c2n1
• Target: mTOR,PI3K,p38 MAPK,Src
• Solubility: H2O:60.2 mg/mL (113.88 mM);DMSO:60.2 mg/mL (113.88 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.78 mM)

Bioactivity

• Target IC50:
  PI3Kα:81 nM|CK1γ1:17.8 μM|PI3Kγ:3.11 μM|mTOR:7 nM|p38α:28.9 μM
• In Vitro:
  Immune-complex kinase assay shows mTORC2-specific substrate His6-AKT or the mTORC1 substrate His6-S6K is dose dependently inhibited by WYE-687. WYE-687 globally inhibits mTOR signaling and AKT function in cellular models dose dependently. WYE-678 profoundly inhibits cap-dependent and global protein synthesis in MDA361, human breast cancer cells. WYE-687 shows antiproliferative effects in various cancer cell lines involving G1 cell cycle arrest and selective apoptosis. WYE-687 down-regulate angiogenic factors, VEGF and HIF-1α, in U87 mg, MDA361 and LNCap cells.
• Cell Research:
  For cell cycle analysis, cells are seeded in 96-well culture plates at 10,000 cells per well for 24 hours, treated with various inhibitors for 24 hours or 48 hours. Following treatment, cells are harvested, washed with PBS and fixed overnight at -20 °C in 70% ethanol. Cells are washed, stained with propidium iodide and analyzed for cell cycle profile (acquired 5000 cells/well) on Guava PCA-96 instrument according to the Guava Cell Cycle Protocol(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, mTOR, Inhibitor, Mammalian target of Rapamycin, p38α, p38MAPK, p38 MAPK, PI3K, WYE687, WYE-687, WYE 687, PI3Kα, PI3Kγ, Phosphoinositide 3-kinase, Src

Compound Identifiers

PubChem CID

25229450