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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Arginine Deiminase (PAD)-PF-3166
PF-3166

Chemical Structure : PF-3166

CAS No.:

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PF-3166 (PF3166)

货号: PC-23180Not For Human Use, Lab Use Only.

PF-3166 is a potent, selective, noncovalent, cell-active peptidyl arginine deiminase 2 (PAD2) inhibitor with IC50 of 150 nM in fluorescence quenching (FQ) assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PF-3166 is a potent, selective, noncovalent, cell-active peptidyl arginine deiminase 2 (PAD2) inhibitor with IC50 of 150 nM in fluorescence quenching (FQ) assay.
PF-3166 exhibits IC50 of 580 nM in NH3-release assay, with no inhibition of PAD3 or PAD4 activity.
PF-3166 selectively inhibits PAD2 with IC50 values of 610 nM (0.25 mM CaCl2) in GDH-coupled assay.
PF-3166 exhibits cellular activity with IC50 of 3 uM in ionomycin-stimulated human neutrophils.

物理化学性质&存储条件

分子量 870.26
分子式 C43H42BrClN6O5S
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

(R)-1-((1-((S)-1-(2-bromophenyl)-3-((2-methyl-5-(methylsulfonamido)phenyl)amino)-3-oxopropyl)-2-(3-(4-chlorophenoxy)phenyl)-1H-benzo[d]imidazol-6-yl)methyl)-N-methylpyrrolidine-2-carboxamide

参考文献

1. Byrnes LJ, et al. ACS Chem Biol. 2024 Sep 24. doi: 10.1021/acschembio.4c00397.

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