Chemical Structure : AFM-30a hydrochloride
CAS No.:
AFM-30a hydrochloride
(AFM30a, AMF30a)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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502.98
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Formula
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C24H28ClFN6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-N-(4-(2-fluoroacetimidamido)-1-(4-methoxy-1-methyl-1H-benzo[d]imidazol-2-yl)butyl)-3-oxoisoindoline-4-carboxamide hydrochloride
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References
1. Muth A, et al. J Med Chem. 2017 Apr 13;60(7):3198-3211.
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