506282
Cl-amidine
>95% (HPLC), solid, PAD inhibitor, Calbiochem®
Synonyme(s) :
PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
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A propos de cet article
Formule empirique (notation de Hill) :
C16H20ClF3N4O4
Poids moléculaire :
424.80
UNSPSC Code:
12352200
NACRES:
NA.77
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Laissez-nous vous aiderNom du produit
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.
color
white
assay
>95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Catégories apparentées
Disclaimer
Toxicity: Regulatory Review (Z)
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.
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.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Classe de stockage
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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