MilliporeSigma™ Calbiochem™ PAD Inhibitor, Cl-amidine

Description

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.

A cell-permeable compound that acts as a pan PAD inhibitor (IC₅₀ = 0.8μM, 6.2μM and 5.9μM 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 25μM and 200μM, in vivo . Furthermore, this compound (200μM) together with HDAC inhibitor SAHA (0.4μM) has shown additive effects in inducing p21, GADD45, and PUMA expression and inhibiting cancer cell growth in a p53-dependent manner in U2OS cells.

Specifications

• Color: White
• Description: >95% by HPLC
• Molecular Formula: C₁₆H₂₀ClF₃N₄O₄
• Formula Weight: 424.8g/mol
• Solubility: DMSO
• Form: Solid
• Quantity: 10 mg