GSK2606414

SKU: orb1226517

Description

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.(In Vitro):GSK2606414 inhibits PERK activation in cells.(In Vivo):GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.

Key Properties

• CAS Number: 1337531-36-8
• MW: 451.44
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₀F₃N₅O
• SMILES: FC(C1=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3)=O)=CC=C1)(F)F
• Target: PERK
• Solubility: Ethanol: 19 mg/mL (42.08 mM); DMSO: 90 mg/mL (199.36 mM)

Bioactivity

• In Vivo:
  GSK2606414 (50 and 150 mg/kg, p.o.) inhibits the growth of a human tumor xenograft in mice.
• In Vitro:
  GSK2606414 inhibits PERK activation in cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK2606414 | GSK-2606414 | GSK PERK Inhibitor

Quick Database Links

Gene Symbol

PERK