506282
Cl-amidine
>95% (HPLC), solid, PAD inhibitor, Calbiochem®
Synonym(s):
PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
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About This Item
Empirical Formula (Hill Notation):
C16H20ClF3N4O4
Molecular Weight:
424.80
UNSPSC Code:
12352200
NACRES:
NA.77
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product name
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.
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
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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