Protein Arginine Deiminase Peptidylarginine Deiminase

Protein arginine deiminases (PADs) is a unique family of enzymes that catalyzes the hydrolysis of peptidyl-arginine to form peptidyl-citrulline on histones, fibrinogen, and other biologically relevant proteins. In humans, the PAD family is composed of five, calcium dependent isozymes (PADs 1-4 and 6), which share roughly 50% sequence similarity. PADs are found in a myriad of cell and tissue types, including the epidermis and uterus (PAD1), skeletal muscle, brain, inflammatory cells, several cancer cell lines, and secretory glands (PAD2), hair follicles and keratinocytes (PAD3), granulocytes and several types of cancer (PAD4), and oocytes and embryos (PAD6). PAD4, the best characterized isozyme, has also been shown to citrullinate a number of other proteins, including p300, ING4, RPS2, lamin C, and nucleophosmin.

www.MedChemExpress.com 1 Protein Arginine Deiminase Inhibitors & Activators

Acefylline BB-Cl-Amidine (Theophyllineacetic acid; Theophylline-7-acetic acid) Cat. No.: HY-B1505 Cat. No.: HY-111347

Acefylline (Theophyllineacetic acid), a xanthine BB-Cl-Amidine is a peptidylarginine deminase derivative, is an adenosine receptor antagonist. (PAD) inhibitor. Acefylline is a peptidylarginine deiminase (PAD) activator. Acefylline is also a bronchodilator, which inhibits rat lung cAMP phosphodiesterase isoenzymes. Purity: 99.89% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg Size: 1 mg, 5 mg

BB-Cl-Amidine hydrochloride BMS-P5 Cat. No.: HY-111347A Cat. No.: HY-137655

BB-Cl-Amidine hydrochloride is a peptidylarginine BMS-P5 is a specific and orally active deminase (PAD) inhibitor. peptidylarginine deiminase 4 (PAD4) inhibitor. BMS-P5 blocks MM-induced NET formation and delays progression of MM in a syngeneic mouse model.

Purity: 99.98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg

BMS-P5 free base Cl-amidine Cat. No.: HY-137655A Cat. No.: HY-100574

BMS-P5 free base is a specific and orally active Cl-amidine is an orally active peptidylarginine

peptidylarginine deiminase 4 (PAD4) inhibitor. deminase (PAD) inhibitor, with IC50 values of 0.8 BMS-P5 free base blocks MM-induced NET formation μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, and delays progression of MM in a syngeneic mouse respectively. Cl-amidine induces apoptosis in model. cancer cells.

Purity: 99.94% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 1 mg, 5 mg

Cl-amidine hydrochloride Cl-amidine TFA Cat. No.: HY-100574A Cat. No.: HY-100574B

Cl-amidine hydrochloride is an orally active Cl-amidine TFA is an orally active peptidylarginine

peptidylarginine deminase (PAD) inhibitor, with deminase (PAD) inhibitor, with IC50 values of 0.8

IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, PAD3, and PAD4, respectively. Cl-amidine respectively. Cl-amidine TFA induces apoptosis in hydrochloride induces apoptosis in cancer cells. cancer cells.

Purity: ≥95.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 1 mg, 5 mg

D-Cl-amidine GSK484 hydrochloride Cat. No.: HY-100574C Cat. No.: HY-100514

D-Cl-amidine is a potent and highly selective GSK484 hydrochloride is a selective and reversible PAD1 inhibitor. D-Cl-amidine is well-torelated peptidylarginine deiminase 4 (PAD4) inhibitor. with no significant toxicity. GSK484 hydrochloride demonstrates high affinity

binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed. Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

PAD2-IN-1 Cat. No.: HY-136557

PAD2-IN-1, a benzimidazole-based derivative, is a potent and selective protein arginine deiminase 2 (PAD2) inhibitor. PAD2-IN-1 shows superior selectivity for PAD2 over PAD4 (95-fold) and PAD3 (79-fold).

Purity: >98% Clinical Data: No Development Reported Size: 1 mg, 5 mg