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.
Sinonimo/i:
PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
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About This Item
Formula empirica (notazione di Hill):
C16H20ClF3N4O4
Peso molecolare:
424.80
Codice UNSPSC:
12352200
NACRES:
NA.77
Livello qualitativo
Saggio
>95% (HPLC)
Forma fisica
solid
Produttore/marchio commerciale
Calbiochem®
Condizioni di stoccaggio
OK to freeze
Colore
white
Solubilità
DMSO: 50 mg/mL
Condizioni di spedizione
ambient
Temperatura di conservazione
−20°C
Descrizione generale
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.
Attenzione
Toxicity: Regulatory Review (Z)
Ricostituzione
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Altre note
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.
Note legali
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
Certificati d'analisi (COA)
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