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GNE-235

Chemical Structure : GNE-235

CAS No.:

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GNE-235 (GNE235, GNE 235)

Catalog No.: PC-21166Not For Human Use, Lab Use Only.

GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GNE-235 (GNE235) is a potent, selective inhibitor of the second bromodomain of polybromo-1 (PBRM1; BAF180; PB1) with KD value of 0.28 uM in BROMOscan assays.
GNE-235 displays >20-fold selectivity over PBRM1(5), SMARCA2 and SMARCA4 in BROMOscan assays.
GNE-235 has binding KD value of 1.1 uM against PBRM1(2) in ITC assays, >30-fold selectivity over PBRM1(4) and PBRM1(3).
GNE-235 also shows clear profiles in the nuclear receptor assays, and the low-level PXR activation.

Physicochemical Properties

M.Wt 244.30
Formula C13H16N4O
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

(S)-6-(Furan-2-yl)-4-(2-methylpyrrolidin-1-yl)pyridazin-3-amine

References

1. Andrea G Cochran, et al. J Med Chem. 2023 Sep 13. doi: 10.1021/acs.jmedchem.3c01149.

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