132 products were found matching "K01481"!

Cl-Amidine is an irreversible inhibitor of protein arginine deiminases (PADs, IC50s = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively). It is cytotoxic to HL-60, MCF-7, and HT-29 cancer cells (IC50s = 0.25, 0.05, and 1 µM, respectively). Cl-amidine (50 mg/kg) reduces ex vivo extracellular neutrophil...

Peptidyl arginine deiminase 2 (PAD2) catalyzes the conversion of arginine residues to citrulline within cellular protein substrates, resulting in the loss of a positive charge, which can alter protein structure and/or function. It is composed of an alpha/beta propeller domain, an IgG1 domain that contains calcium...

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme. It is selective for PAD4 over PAD1-3. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human...

Protein arginine deiminases (PADs) catalyze the posttranslational modification of arginine residues on proteins to form citrulline, which plays a large role in regulating gene expression. Abnormally high PAD activity has been observed in a host of human diseases. Citrulline-specific probe-rhodamine is a highly...

GSK 199 is an inhibitor of peptidyl arginine deiminase 4 (PAD4, IC50 = 200 nM in the absence of calcium). It selectively inhibits the production of citrulline by PAD4 over PAD1, PAD2, and PAD3 in kinetic assays. GSK 199 (10 µM) prevents histone H3 citrullination and neutrophil extracellular trap (NET) formation...

Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases. GSK106 is an inactive control for the selective PAD4 inhibitors, GSK484 (Cay-17488)...

Protein arginine deiminase 3 (PAD3) catalyzes the conversion of arginine residues to citrulline within its cellular protein substrates, which include S100A3, trichohyalin, and filaggrin, resulting in the loss of a positive charge, which can alter protein structure and/or function. It exists as a homodimer and is...

Peptidyl arginine deiminase 1 (PAD1) is a calcium-dependent enzyme that catalyzes the conversion of arginine residues to citrulline within its cellular protein substrates, resulting in the loss of a positive charge, which can alter protein structure and/or function. It exists as a monomer and is composed of a...

Protein arginine deiminase 6 (PAD6) is a homodimeric guanidine-modifying enzyme belonging to the amidinotransferase superfamily. It is a calcium-dependent enzyme that catalyzes the post-translational modification of target proteins by converting arginine to citrulline. PAD6 is expressed in mammalian oocytes, sperm...

Peptidyl arginine deiminase 2 (PAD2) catalyzes the conversion of arginine residues to citrulline within cellular protein substrates, resulting in the loss of a positive charge, which can alter protein structure and/or function. It is composed of an alpha/beta propeller domain, an IgG1 domain that contains calcium...

F-amidine is an inhibitor of protein arginine deiminases (PADs) that is selective for PAD1 and PAD4 (IC50s = 29.5, 350, and 21.6 µM for PAD1, PAD3, and PAD4 in vitro, respectively). It irreversibly inactivates all four PAD subtypes (kinact/KI = 2,800, 380, 170, and 3,000 M-1min-1 by covalently modifying an active...

BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine (Cay-17079) that contains an alkyne moiety for use in click chemistry reactions. BB-Cl-Yne inhibits PAD1-4 with kinact/KI values of 6,400, 3,600, 10,800, and 4,900 M-1min-1, respectively. It has been used for...