Medchemexpress LLC GNE-049 | 1936421-41-8 | 99.7% | 510.58 | 100 MG

Supplier:  Medchemexpress LLC HY1084351G

GNE-049 is a highly potent and selective CBP inhibitor. It demonstrates excellent potency in BRET cellular assays and inhibits MYC expression in MV4-11 cell lines. The compound exhibits acceptable pharmacokinetic properties and selectively targets CBP/P300 with high selectivity over BRD4(1), and can penetrate the central nervous system (CNS).

• Highly potent and selective CBP inhibitor (IC50 of 1.1 nM in TR-FRET assay).
• Inhibits BRET (IC50 12 nM) and BRD4(1) (IC50 4200 nM).
• Acceptable pharmacokinetic properties in mouse, rat, dog, and monkey.
• High selectivity for CBP/P300 (3820-fold over BRD4(1)).
• Penetrates the central nervous system.
• Inhibits MYC expression (EC50 of 14 nM in MV4-11 cell line).
• Selected for balance of liver microsome stability, selectivity, and cellular potency.

Catalog No. 50-003-47471