EX229

SKU: orb1296258

Description

EX229

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1219739-36-2
• MW: 431.87
• Purity: 99.20% (May vary between batches)
• Formula: C₂₄H₁₈ClN₃O₃
• SMILES: Cc1ccc(Oc2nc3cc(c(Cl)cc3[nH]2)-c2ccc3n(C)ccc3c2)cc1C(O)=O
• Target: AMPK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.32 mM);DMSO:120 mg/mL (277.86 mM)

Bioactivity

• Target IC50:
  AMPK α1β1γ1:0.06 μM (Kd)|AMPK α1β2γ1:0.51 μM (Kd)|AMPK α2β1γ1:0.06 μM (Kd)
• In Vitro:
  Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when 991 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose-dependently increased when coincubation is carried out with EX229. EX229 also dose-dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes .
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Storage & Handling

• Storage: store at low temperature | 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

inhibit, Inhibitor, EX 229, EX229, EX-229, C 991, C991, C-991, AMP-activated protein kinase, AMPK, Compound 991

Compound Identifiers

PubChem CID

45256693