VER-246608

SKU: orb1307620

Description

VER-246608

Research Area

Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 1684386-71-7
• MW: 552.96
• Purity: 98.50%
• Formula: C₂₈H₂₃ClF₂N₄O₄
• SMILES: Cc1cnc(Cl)nc1-c1ccc(cc1)N(Cc1ccc(CNC(=O)C(F)F)cc1)C(=O)c1ccc(O)cc1O
• Target: PDK,Dehydrogenase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.62 mM);DMSO:50 mg/mL (90.42 mM)

Bioactivity

• Target IC50:
  PDK4:91 nM|PDK3:40 nM|PDK1:35 nM|PDK2:84 nM
• In Vitro:
  A novel and selective ATP competitive pan-isoform inhibitor of PDK, VER-246608. Consistent with a PDK mediated MOA, VER-246608 increased pyruvate dehydrogenase complex (PDC) activity, oxygen consumption and attenuated glycolytic activity. However, these effects were only observed under D-glucose-depleted conditions and required almost complete ablation of PDC E1α subunit phosphorylation. VER-246608 was weakly anti-proliferative to cancer cells in standard culture media

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

Inhibitor, inhibit, VER 246608, VER246608, VER-246608, PDK3, PDK-3, PDK4, PDK-4, PDK-1, PDK2, PDK-2, PDK1, PDHK, PDH, PDH kinase, Pyruvate dehydrogenase kinase

Compound Identifiers

PubChem CID

86280454