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506282 PAD Inhibitor, Cl-amidine - Calbiochem

506282
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Overview

Key Spec Table

Empirical Formula
C₁₆H₂₀ClF₃N₄O₄

Products

Catalogue NumberPackaging Qty/Pack
506282-10MGCN Glass bottle 10 mg
Description
OverviewA 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.
Catalogue Number506282
Brand Family Calbiochem®
SynonymsN-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
References
ReferencesKnuckley, B., et al. 2010. Biochemistry 23, 4852.
Li, P., et al. 2010. Oncogene 21, 3153.
Luo, Y., et al. 2006. Biochemistry 39, 11727.
Product Information
FormWhite solid
Hill FormulaC₁₆H₂₀ClF₃N₄O₄
Chemical formulaC₁₆H₂₀ClF₃N₄O₄
Structure formula ImageStructure formula Image
Quality LevelMQ200
Biological Information
Purity>95% by HPLC
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Regulatory Review
Storage -20°C
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Global Trade Item Number
Catalogue Number GTIN
506282-10MGCN 04055977272444