GNE-495

SKU: orb1296220

Description

GNE-495 is a highly potent and selective small molecule inhibitor of MAP4K4, demonstrating an IC50 of 3.7 nM. This compound is a valuable research tool for investigating MAP4K4's role in cellular signaling, with applications in studying metabolic disorders, cancer biology, and inflammation in both in vitro and in vivo models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1449277-10-4
• MW: 405.42
• Purity: 99.22%
• Formula: C₂₂H₂₀FN₅O₂
• SMILES: Nc1ncc(C(=O)NC2CN(C2)C(=O)C2CC2)c2ccc(nc12)-c1cccc(F)c1
• Target: MAPK
• Solubility: DMSO:2 mg/mL (4.93 mM)

Bioactivity

• Target IC50:
  MAP4K4:3.7nM
• In Vivo:
  GNE-495 is administered at high doses (25 and 50 mg/kg) intraperitoneally to neonatal mice. This compound demonstrates superior potency and favorable pharmacokinetic (PK) profiles across all tested species, characterized by low clearance rates, moderate terminal half-lives, and acceptable levels of oral bioavailability (F=37-47%).
• In Vitro:
  GNE-495 has efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency.

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

GNE 495, GNE495, GNE-495, Inhibitor, MAP4K, MAP4K4, MAPK Kinase Kinase Kinase, inhibit

Compound Identifiers

PubChem CID

89730041