MilliporeSigma™ Calbiochem™ PAD Inhibitor, Cl-amidine

Description

• A cell-permeable compound that acts as a pan PAD inhibitor (IC 50 = 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.