GNE0877

SKU: orb1301135

Description

GNE-0877 is a potent and selective small molecule inhibitor of LRRK2 kinase, exhibiting a Ki of 0.7 nM. It is a valuable research tool for investigating LRRK2 biology in cellular models and has been utilized in preclinical in vivo studies relevant to Parkinson's disease research.

Research Area

Cell Biology

Key Properties

• CAS Number: 1374828-69-9
• MW: 339.32
• Purity: 99.96%
• Formula: C₁₄H₁₆F₃N₇
• SMILES: CNc1nc(Nc2cn(nc2C)C(C)(C)C#N)ncc1C(F)(F)F
• Target: LRRK2
• Solubility: DMSO:45 mg/mL (132.62 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  LRRK2:0.7 nM(Ki)
• In Vivo:
  GNE-0877 significantly inhibits LRRK2 cellular activity (IC50: 3 nM) and demonstrates low turnover in human liver microsomes and hepatocytes. Additionally, GNE-0877 acts as a reversible inhibitor of CYP1A2 (IC50: 0.7 μM).
• In Vitro:
  Within BAC transgenic mice expressing human LRRK2 protein with the Parkinson's disease mutation G2019S, GNE-0877 effectively inhibits LRRK2 Ser1292 autophosphorylation. GNE-0877 demonstrates favorable oral bioavailability and brain penetrance.

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

small molecule, brain-penetrant, oral, LRRK2, inhibit, liver microsomes, Leucine-rich repeat kinase 2, Inhibitor, GNE 0877, GNE0877, GNE-0877

Compound Identifiers

PubChem CID

69093374