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506282 PAD Inhibitor, Cl-amidine - Calbiochem

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.

PAD Inhibitor, Cl-amidine - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide

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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆H₂₀ClF₃N₄O₄

Products

Catalogue NumberPackaging Qty/Pack
506282-10MGCN 玻璃瓶 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
HS Code2925 29 90
Structure formula ImageStructure formula Image
Quality LevelMQ200
Applications
Biological Information
Purity>95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
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.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
506282-10MGCN 04055977272444

Documentation

PAD Inhibitor, Cl-amidine - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

PAD Inhibitor, Cl-amidine - Calbiochem Certificates of Analysis

TitleLot Number
506282

References

Reference overview
Knuckley, B., et al. 2010. Biochemistry 23, 4852.
Li, P., et al. 2010. Oncogene 21, 3153.
Luo, Y., et al. 2006. Biochemistry 39, 11727.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision04-November-2011 RFH
SynonymsN-α-benzoyl-N5-(2-chloro-1-iminoethyl)-L-Orn amide
DescriptionA 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.
FormWhite solid
Chemical formulaC₁₆H₂₀ClF₃N₄O₄
Structure formulaStructure formula
Purity>95% by HPLC
SolubilityDMSO (50 mg/ml)
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.
Toxicity Regulatory Review
ReferencesKnuckley, B., et al. 2010. Biochemistry 23, 4852.
Li, P., et al. 2010. Oncogene 21, 3153.
Luo, Y., et al. 2006. Biochemistry 39, 11727.