Cl-Amidine |
N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide 2,2,2-trifluoroacetate |
(CAS 1043444-18-3) |
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Description: |
Protein arginine deiminase 4 (PAD4) catalyzes the post-translational modification of arginine residues on histones to form citrulline, which plays a large role in regulating gene expression. Dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis. Cl-amidine is an inhibitor of PAD4 deimination activity with an IC50 value of 5.9 μM in an in vitro activity assay. It irreversibly inactivates (kinact/KI = 13,000 M-1min-1) PAD4 by covalently modifying an active site cysteine that is important for its catalytic activity. Cl-amidine also inhibits PAD1 and PAD3 with IC50 values of 0.8 and 6.2 μM, respectively. Cl-amidine is cytotoxic to HL-60, MCF7, and HT-29 cancer cell lines (IC50s = 0.25, 0.05 and 1 μM, respectively). In a CIA mouse model of inflammatory arthritis, Cl-amidine dose dependently decreases the citrulline content in serum and joints and reduces the development of IgG autoantibodies.
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Product No. |
KT00277 |
Product Name |
Cl-Amidine |
Synonyms |
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Formal Name |
N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide 2,2,2-trifluoroacetate |
CAS Number |
1043444-18-3 |
Molecular Formula |
C14H19ClN4O2•CF3CO2H |
Formula Weight |
424.8 |
Formulation |
A crystalline solid |
Purity |
98%min |
Stability |
2 years |
Storage |
-20°C |
Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
Price & Availability |
In Stock. Price Negotiated. |
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Related Products: |
Citrulline-specific Probe
F-Amidine (trifluoroacetate salt)
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PAD4 (human recombinant)
PAD4 Inhibitor Screening Assay Kit
AS703026
AZD8330
BIX02188
BIX02189
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