GSK621

SKU: orb1300405

Description

GSK621 is a potent and selective small molecule activator of AMP-activated protein kinase (AMPK). It is widely used in metabolic and cancer research, demonstrating efficacy in both cellular assays and animal models to study energy homeostasis and cell growth.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1346607-05-3
• MW: 489.91
• Purity: 99.01% (May vary between batches)
• Formula: C₂₆H₂₀ClN₃O₅
• SMILES: COc1cccc(c1)-n1c(=O)[nH]c2cc(Cl)n(-c3ccc(cc3)-c3cccc(OC)c3O)c2c1=O
• Target: Apoptosis,Autophagy,AMPK
• Solubility: 10% DMSO+90% Corn Oil:1 mg/mL (2.04 mM);DMSO:90 mg/mL (183.71 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• In Vivo:
  In nude mice bearing MOLM-14 xenografts, GSK621 (30 mg/kg, i.p.) reduces leukemia growth and significantly extends survival by enhancing AMPK activity and the induction of apoptosis.
• In Vitro:
  In AML cell lines and primary AML samples, GSK621 markedly increases phosphorylation at AMPKα T172, a marker of AMPK activation. In a set of 20 cell lines, GSK621 reduces the proliferation of all 20 lines with IC50 ranged from 13-30 μM, and increases apoptosis in 17 (85%) lines. In addition, GSK621 also triggers autophagy, which partially contributes to AML cell death.
• Cell Research:
  Twenty AML cell lines are treated with log10 dilutions of GSK621 and relative viability is determined by CellTiter-Glo assay. IC50 of GSK621 among these 20 cell lines is calculated using the Prism software and are presented as log[C] with [C] in mol/l (M). Results are presented for 5 different cell lines per panel.(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

PERK, UPR, ER Stress, GSK621, GSK-621, GSK 621, Inhibitor, inhibit, Apoptosis, AMPK, AMP-activated protein kinase, ATF4, Autophagy, CHOP

Compound Identifiers

PubChem CID

54577153