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F-Amidine TFA

CAT: 0931-T84479-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T84479-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
877617-46-4
Target
Others, PAD
Related Pathways
Chromatin/Epigenetic, Others
Bioactivity
F-amidine is a selective inhibitor of protein arginine deiminases (PADs), specifically targeting PAD1 and PAD4 with in vitro IC50 values of 29.5, 350, and 21.6 μM for PAD1, PAD3, and PAD4, respectively. It irreversibly inactivates all four PAD subtypes by covalently modifying an active site cysteine crucial for enzymatic activity, with kinact/KI values of 2,800, 380, 170, and 3,000 M^-1min^-1. Additionally, F-amidine demonstrates cytotoxicity against HL-60, MCF-7, and HT-29 cancer cell lines, with IC50s of 0.5, 0.5, and 1 μM, respectively.
Smiles
C(C(O)=O)(F)(F)F.C(N[C@@H](CCCNC(CF)=N)C(N)=O)(=O)C1=CC=CC=C1
Molecular Formula
C14H19FN4O2?CF3COOH
Molecular Weight
408.4
Shipping Conditions
Ice Packs
Storage Temperature
-20°C