A family of calcium-dependent enzymes known as Protein Arginine Deiminase (PAD) is able to catalyze the conversion of arginine residues into citrulline. Numerous pathological diseases, including inflammation and autoimmune disorders, are caused by this chemical reaction, which also causes the formation of citrullinated proteins with altered structure and function. These pathologies made the PADs viable therapeutic targets, and several PAD inhibitors are currently available.
Five PADs, known as PADs 1-4 and PAD6, are encoded by humans. Only four (PADs1-4) of the five PAD isozymes (PADs1, 2, 3, 4, and 6) are catalytically active. Ca2+ is a key regulator of PAD activity, and PADs have 4 (PAD1), 5 (PAD3), or 6 (PAD2) Ca2+-binding sites. Multiple inflammatory diseases (like rheumatoid arthritis) and cancer are linked to dysregulated PAD activity, and PAD inhibitors like Cl-amidine and BB-Cl-amidine are effective in a variety of preclinical animal disease models.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V52435 | AFM-30a | 2095107-57-4 | AFM-30a is a potent protein arginine deiminase 2 (PAD2) inhibitor (antagonist) with excellent PAD2 selectivity. |
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V77281 | AFM-30a hydrochloride | AFM-30a HCl is a potent protein arginine deiminase 2 (PAD2) inhibitor (antagonist) with excellent PAD2 selectivity. | |
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V22824 | AFM32a (PAD2-IN-1) | 2095109-82-1 | AFM32a (PAD2-IN-1), a benzimidazole-based analogue, is a potent and specific inhibitor of protein arginine deiminase 2 (PAD2). |
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V77280 | AFM32a hydrochloride (PAD2-IN-1 hydrochloride) | AFM32a (PAD2-IN-1) HCl, a benzimidazole-based analogue, is a potent and specific inhibitor of protein arginine deiminase 2 (PAD2). | |
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V32207 | BB-Cl-Amidine | 1802637-39-3 | BB-Cl-Amidine is a peptidylarginine deminase (PAD) inhibitor with potentialfor Canine and Feline Mammary Cancer via Activation of the Endoplasmic Reticulum Stress Pathway. |
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V53041 | BB-Cl-Amidine hydrochloride | 2436747-41-8 | BB-Cl-Amidine HCl is an inhibitor (blocker/antagonist) of peptidyl arginine deaminase (PAD). |
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V60078 | BMS-P5 HCL | 1549811-36-0 | BMS-P5 is a specific, orally bioactive inhibitor of peptide arginine diiminase 4 (PAD4). |
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V28803 | Cl-amidine | 913723-61-2 | Cl-amidine is an orally bioavailable PAD inhibitor (antagonist) with IC50s of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3 and PAD4 respectively. |
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V77100 | D-Cl-amidine hydrochloride | D-Cl-amidine HCl is a potent and selective PAD1 inhibitor. | |
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V3606 | GSK484 | 1652591-81-5 | GSK484 is a novel and potent inhibitor of peptidylarginine deiminase 4 (PAD4). |
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V51674 | JBI-589 | 2308504-22-3 | JBI-589 is a non-covalent, selective PAD4 inhibitor. |
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V56116 | PAD4-IN-2 | 2642327-52-2 | PAD4-IN-2 (Compound 5i) is a PAD4 inhibitor (IC50=1.94 μM). |
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V75474 | PAD4-IN-3 | 2642327-44-2 | PAD4-IN-3 (compound 4B) is a PAD4 inhibitor (antagonist) with anti-tumor activity in vitro and in vivo. |
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