877617-46-4 Usage
Description
F-Amidine (trifluoroacetate salt) is a chemical compound that acts as an inhibitor of peptidyl arginine deiminase 4 (PAD4), a key enzyme involved in the post-translational modification of arginine residues on histones, which plays a significant role in regulating gene expression. Its ability to irreversibly inactivate PAD4 by covalently modifying an active site cysteine makes it a promising candidate for therapeutic applications.
Uses
Used in Pharmaceutical Industry:
F-Amidine (trifluoroacetate salt) is used as an inhibitor of PAD4 for its potential therapeutic applications in treating diseases associated with dysregulated PAD4 activity, such as cancer and rheumatoid arthritis. Its IC50 value of 21.6 μM in an in vitro activity assay demonstrates its effectiveness in inhibiting PAD4 activity.
Additionally, F-Amidine (trifluoroacetate salt) is used as an inhibitor of PAD1 and PAD3 with IC50 values of 29.5 and 350 μM, respectively, further expanding its potential applications in the pharmaceutical industry.
Used in Cancer Research:
F-Amidine (trifluoroacetate salt) is used as a cytotoxic agent against various cancer cell lines, including HL-60, MCF-7, and HT-29, with IC50 values of 0.5, 0.5, and 1 μM, respectively. This makes it a valuable tool in cancer research for understanding the mechanisms of PAD4 inhibition and its potential role in cancer treatment.
Check Digit Verification of cas no
The CAS Registry Mumber 877617-46-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,7,7,6,1 and 7 respectively; the second part has 2 digits, 4 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 877617-46:
(8*8)+(7*7)+(6*7)+(5*6)+(4*1)+(3*7)+(2*4)+(1*6)=224
224 % 10 = 4
So 877617-46-4 is a valid CAS Registry Number.
877617-46-4Relevant articles and documents
A fluoroacetamidine-based inactivator of protein arginine deiminase 4: Design, synthesis, and in vitro and in vivo evaluation
Luo, Yuan,Knuckley, Bryan,Lee, Young-Ho,Stallcup, Michael R.,Thompson, Paul R.
, p. 1092 - 1093 (2006)
Protein arginine deiminase 4 (PAD4) is a calcium-dependent transcriptional corepressor that has been implicated in the onset and progression of rheumatoid arthritis. Herein we describe the synthesis and in vitro evaluation of a fluoroacetamidine-containing compound, N-α-benzoyl-N5-(2-fluoro-1-iminoethyl)-l-ornithine amide, 1, hereafter referred to as F-amidine, that is the most potent PAD4 inhibitor ever described. Additional studies described herein indicate that F-amidine can also inhibit PAD4 activity in vivo. The bioavailability of this compound suggests that F-amidine will be a powerful chemical probe of PAD4 function that can be used to dissect the roles of this enzyme in both rheumatoid arthritis and transcriptional control. The fact that inhibition is of an irreversible nature suggests that, with appropriate functionalization, F-amidine analogues will be robust activity-based protein-profiling and proteomic capture reagents. Copyright
