506282
PAD Inhibitor, Cl-amidine
Cl-amidine is a cell-permeable pan PAD inhibitor (IC₅₀ = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively). Inactivates the calcium bound form of PAD4 in an irreversible manner.
Synonym(s):
PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
Sign Into View Organizational & Contract Pricing
All Photos(1)
About This Item
Empirical Formula (Hill Notation):
C16H20ClF3N4O4
Molecular Weight:
424.80
UNSPSC Code:
12352200
NACRES:
NA.77
Recommended Products
Quality Level
Assay
>95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable compound that acts as a pan PAD inhibitor (IC50 = 0.8 µM, 6.2 µM and 5.9 µM for PAD1, PAD3, and PAD4, respectively) in enzymatic assays. It preferentially inactivates the calcium bound form of PAD4 in an irreversible manner, and is shown to complete with BAEE for the active site residue of this enzyme. A small but significant reduction in the efficiency of p300GDB-GRIP1 interaction is observed in transiently transfected CV-1 cells treated with Cl-amidine at concentrations between 25 µM and 200 µM, in vivo. Furthermore, this compound (200 µM) together with HDAC inhibitor SAHA (0.4 µM) has shown additive effects in inducing p21, GADD45, and PUMA expression and inhibiting cancer cell growth in a p53-dependent manner in U2OS cells.
Warning
Toxicity: Regulatory Review (Z)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Knuckley, B., et al. 2010. Biochemistry23, 4852.
Li, P., et al. 2010. Oncogene21, 3153.
Luo, Y., et al. 2006. Biochemistry39, 11727.
Li, P., et al. 2010. Oncogene21, 3153.
Luo, Y., et al. 2006. Biochemistry39, 11727.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
Customers Also Viewed
Hala Chaaban et al.
Journal of cellular and molecular medicine (2020-06-10)
Necrotizing enterocolitis (NEC) is a devastating gastrointestinal disease affecting primarily premature infants. The disease is characterized by intestinal inflammation and leucocyte infiltration, often progressing to necrosis, perforation, systemic inflammatory response and death. Neutrophil extracellular traps (NETs), denoting nuclear DNA, histone
Dina Ahmed et al.
International journal of molecular sciences, 22(23) (2021-12-11)
This study deals with the process of optimization and synthesis of Poly(3-hydroxybutyrate) microspheres with encapsulated Cl-amidine. Cl-amidine is an inhibitor of peptidylarginine deiminases (PADs), a group of calcium-dependent enzymes, which play critical roles in a number of pathologies, including autoimmune
Florian Wimmers et al.
Cell, 184(15), 3915-3935 (2021-06-27)
Emerging evidence indicates a fundamental role for the epigenome in immunity. Here, we mapped the epigenomic and transcriptional landscape of immunity to influenza vaccination in humans at the single-cell level. Vaccination against seasonal influenza induced persistently diminished H3K27ac in monocytes
Pengchong Li et al.
Nature immunology, 22(9), 1107-1117 (2021-08-14)
The linkage between neutrophil death and the development of autoimmunity has not been thoroughly explored. Here, we show that neutrophils from either lupus-prone mice or patients with systemic lupus erythematosus (SLE) undergo ferroptosis. Mechanistically, autoantibodies and interferon-α present in the
Lijing Kang et al.
Nature communications, 11(1), 2488-2488 (2020-05-20)
Neovascularization and vascular remodeling are functionally important for brain repair after stroke. We show that neutrophils accumulate in the peri-infarct cortex during all stages of ischemic stroke. Neutrophils producing intravascular and intraparenchymal neutrophil extracellular traps (NETs) peak at 3-5 days.
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service