VER-246608, Pan-PDK inhibitor (TBI4224)

Description

Product Details

Formal Name: N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl] methyl]-2,4-dihydroxybenzamide

Molecular Formula: C₂₈H₂₃ClF₂N₄O₄

Formula Weight: 553.0

CAS Number: 1684386-71-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (> 25 mg/ml).

Storage: -20°C

Stability: ≥ 2 years.

Applications

Pan-PDK inhibitor

Functions

Potent (IC₅₀’s: PDK-1 = 35 nM, PDK-2 = 84 nM, PDK-3 = 40 nM, PDK-4 = 91 nM) and selective pan-pyruvate dehydrogenase kinase inhibitor. It decreased oxygen consumption and attenuated glycolytic activity (Warburg metabolism) under D-glucose/L-glutamine-depleted conditions. VER-246608 treatment of four cancer lines (PC-3, SW-1088, UM-22B, and MEF) under depleted D-glucose/L-glutamine conditions resulted in almost complete inhibition of cell growth.  It also acted synergistically with doxorubicin in PC-3 and ES-2 cells.

Application Procedures

First dissolved in DMSO (> 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI4224_VER-246608_datasheet

MSDS:

TBI4224_VER-246608_MSDS

Research use only.