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Sigma-Aldrich

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.

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Synonym(s):
PAD Inhibitor, Cl-amidine, N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
Empirical Formula (Hill Notation):
C16H20ClF3N4O4
Molecular Weight:
424.80
NACRES:
NA.77

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

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This Item
526526164606407325
form

solid

form

solid

form

solid

form

solid

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

storage condition

OK to freeze, protect from light

storage condition

OK to freeze

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

white

color

pale yellow

color

white

color

white

solubility

DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

solubility

0.1 M NaOH: 1 mg/mL, DMSO: 1 mg/mL (Only partially soluble), water: 1 mg/mL (only partially soluble)

solubility

DMSO: 50 mg/mL, clear, colorless

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.

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


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