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GNE-207

Chemical Structure : GNE-207

CAS No.: 2158266-58-9

GNE-207 (GNE207;GNE 207)

Catalog No.: PC-60307Not For Human Use, Lab Use Only.

GNE-207 (GNE207) is a novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GNE-207 (GNE207) is a novel potent, selective, orally active CBP/p300 bromodomain with IC50 of 1.0 nM.
GNE-207 displays >2,500-fold selectivity over BRD4.
GNE-207 suppresses Myc transcript levels in MV-4-11 cellular assays with EC50 of 18 nM.
GNE-207 exhibits a good pharmacokinetic profile.

Physicochemical Properties

M.Wt 510.598
Formula C29H30N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-(8-(5-acetyl-1-(tetrahydro-2H-pyran-4-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)isoquinolin-3-yl)-N-methylpicolinamide

References

1. Lai KW, et al. Bioorg Med Chem Lett. 2018 Jan 1;28(1):15-23.

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