AFM-30a hydrochloride | PAD2 inhibitor | Probechem Biochemicals

Chemical Structure : AFM-30a hydrochloride

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AFM-30a hydrochloride (AFM30a, AMF30a)

货号: PC-25180Not For Human Use, Lab Use Only.

AFM-30a hydrochloride is a potent, selective protein arginine deiminase 2 (PAD2) inhibitor with IC50 of EC50 of 9.5 uM in target engagement assays in HEK293/PAD2 cells.

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生物&药学活性

AFM-30a hydrochloride is a potent, selective protein arginine deiminase 2 (PAD2) inhibitor with IC50 of EC50 of 9.5 uM in target engagement assays in HEK293/PAD2 cells.
AFM-30a hydrochloride displays good selectivity for PAD2 (1.6-fold over PAD1, 47-fold over PAD3 and ~15-fold over PAD4), based on kinact/KI values.
PAD2 inhibitor 30a is a 12–50-fold more potent PAD2 inhibitors than BB-Clamidine in vitro.
AFM-30a hydrochloride inhibits H3 citrullination in HEK293T/PAD2 cells with EC50 of 0.4 uM, >30-fold less cytotoxic than BB-Cl-amidine.
AFM-30a hydrochloride is a powerful tool for validating the therapeutic relevance of inhibiting PAD2 in multiple disease states, i.e., breast cancer, multiple sclerosis and rheumatoid arthritis.

物理化学性质&存储条件

分子量	502.98
分子式	C24H28ClFN6O3
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)-N-(4-(2-fluoroacetimidamido)-1-(4-methoxy-1-methyl-1H-benzo[d]imidazol-2-yl)butyl)-3-oxoisoindoline-4-carboxamide hydrochloride

参考文献

1. Muth A, et al. J Med Chem. 2017 Apr 13;60(7):3198-3211.

AFM-30a hydrochloride (AFM30a, AMF30a)

生物&药学活性

物理化学性质&存储条件

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AFM-30a hydrochloride (AFM30a, AMF30a)

生物&药学活性

物理化学性质&存储条件

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