GNE-235 | PBRM1(2) inhibitor | Probechem Biochemicals

Chemical Structure : GNE-235

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GNE-235 (GNE235, GNE 235)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	244.30
分子式	C13H16N4O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-6-(Furan-2-yl)-4-(2-methylpyrrolidin-1-yl)pyridazin-3-amine

参考文献

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

GNE-235 (GNE235, GNE 235)

生物&药学活性

物理化学性质&存储条件

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GNE-235 (GNE235, GNE 235)

生物&药学活性

物理化学性质&存储条件

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