GSK2606414

SKU: orb1305265

Description

GSK2606414

Research Area

Cell Biology

Key Properties

• CAS Number: 1337531-36-8
• MW: 451.44
• Purity: 98.63%
• Formula: C₂₄H₂₀F₃N₅O
• SMILES: NC1=C2C(=CN(C)C2=NC=N1)C=3C=C4C(=CC3)N(C(CC5=CC(C(F)(F)F)=CC=C5)=O)CC4
• Target: PERK,Apoptosis,Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.86 mM);DMSO:130 mg/mL (287.97 mM)

Bioactivity

• Target IC50:
  EIF2AK3 (PERK):0.4 nM|N2A cells:5.3 μM|EIF2AK1 (HRI):420 nM|KIT (tyrosine kinase receptor):154 nM|EIF2AK2 (PKR):696 nM|ARPE-19 cells:1.7 µM
• In Vivo:
  METHODS: GSK2606414 (50, 150 mg/kg, oral, twice a day, 21 days) was used to treat mice bearing subcutaneous pancreatic human BxPC3 tumors and the effect on tumor growth was observed. RESULTS GSK2606414 inhibited tumor growth in a dose-dependent manner, with the tumor growth inhibition rates of 20% and 59% at the two doses, respectively.
• In Vitro:
  METHODS: S1-M1-80 vector and S1-M1-80 sgABCG2 cells were treated with GSK2606414 (0.1, 1, 3, 10, 30, 100 μM, 72 hours), and cytotoxicity was determined by MTT assay. RESULTS GSK2606414 showed dose-dependent cytotoxic effects on both cell lines. METHODS: N2A cells were treated with GSK2606414 (0.5, 1 μM, 24 hours) and high glucose (30 mM), cells were lysed, and Western blot analysis was performed. RESULTS N2A cells treated with GSK2606414 reduced the phosphorylation of eIF2α in cells and significantly reduced p-PERK levels in a dose-dependent manner, and GSK2606414 could inhibit the PERK/p-eIF2α/ATF4/CHOP signaling axis.

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

eIF-2AK2 (PKR), eIF-2AK1 (HRI), eIF-2AK3 (PERK), GSK2606414, GSK-2606414, GSK 2606414, inhibit, Inhibitor, Autophagy, Apoptosis, PERK, PKR-like endoplasmic reticulum kinase, Protein kinase R-like endoplasmic reticulum kinase

Compound Identifiers

PubChem CID

53469448