F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 μM for PAD1, PAD3, and PAD4 in vitro, respectively).
Cas No. | 877617-46-4 |
Canonical SMILES | FC(F)(C(O)=O)F.NC([C@@H](NC(C1=CC=CC=C1)=O)CCCNC(CF)=N)=O |
分子式 | C14H19FN4O2•CF3COOH |
分子量 | 408.4 |
溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively). It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active site cysteine that is important for its catalytic activity. F-amidine is cytotoxic to HL-60, MCF-7, and HT-29 cancer cell lines (IC50s = 0.5, 0.5 and 1 μM, respectively). |