PAD

In enzymology, a protein-arginine deiminase is an enzyme that catalyzes a form of post translational modification called arginine de-imination or citrullination. his chemical reaction induces citrullinated proteins formation with altered structure and function, leading to numerous pathological diseases, including inflammation and autoimmune diseases. These pathologies established the PADs as therapeutic targets and multiple PAD inhibitors are known. Humans encode five PADs, designated PADs 1-4 and PAD6. Of the five PAD isozymes (PAD1, 2, 3, 4 and 6), only four (PADs1-4) are catalytically active. PAD activity is tightly regulated by Ca2+ and PADs contain 4 (PAD1), 5 (PAD3, 4) or 6 (PAD2) Ca2+-binding sites. Dysregulated PAD activity, most notably PAD2 and PAD4, is associated with multiple inflammatory diseases (e.g., rheumatoid arthritis) as well as cancer, and PAD inhibitors, such as Cl-amidine and BB-Cl-amidine, show efficacy in multiple preclinical animal models of disease.

Cat. No.	Product Name	CAS No.	Purity
T22277	BMS-P5 化合物BMS-P5	1549811-36-0	98%
T22277	BMS-P5 是一种特异性具有口服活性的肽精氨酸二亚胺酶 4抑制剂。它可阻断多发性骨髓瘤诱导的 NET 形成，并延缓肿瘤进程。
T22277L	BMS-P5 free base 化合物BMS-P5 free base	1550371-22-6	99.96%
T22277L	BMS-P5 free base 是一种特异性，可口服的肽精氨酸二亚胺酶抑制剂，可阻断多发性骨髓瘤诱导的 NET 形成，并延缓肿瘤进程。
T2205	Acefylline 茶碱乙酸	652-37-9	99.95%
T2205	Theophylline-7-acetic acid 是黄嘌呤衍生物，是一种腺苷受体拮抗剂。它是蛋白质精氨酸脱亚氨酶 (PAD) 激活剂，也是一种支气管扩张剂，可抑制大鼠肺 cAMP 磷酸二酯酶同工酶。
T24105	GSK121 化合物GSK121	1652591-80-4	99.63%
T24105	GSK121 Trifluoroacetate 是PAD4的选择性抑制剂。
TQ0067	GSK484 hydrochloride GSK484盐酸盐	1652591-81-5	99.62%
TQ0067	GSK484 hydrochloride 是一种可逆的肽酰基精氨酸脱亚氨酶 4 (PAD4) 抑制剂。它高亲和力与 PAD4 结合，在存在 2 mM 钙和不存在钙的情况下，IC50分别为 250 和 50 nM。
T8861	GSK199 化合物GSK199	1549811-53-1	98.09%
T8861	GSK199 是可逆的PAD4选择性抑制剂，当缺少钙离子时，其IC50值为 200 nM。
T10831L	Cl-amidine hydrochloride 化合物Cl-amidine hydrochloride	1373232-26-8	95%
T10831L	Cl-amidine hydrochloride 是一种口服有效的PAD抑制剂，可阻断组蛋白 3 瓜氨酸化和中性粒细胞胞外陷阱的形成，并提高败血症小鼠的存活率。它可诱导癌细胞凋亡，还可诱导 miR-16 引起细胞周期阻滞。
T10482	BB-Cl-Amidine 化合物BB-Cl-Amidine	1802637-39-3
T10482	BB-Cl-Amidine 是一种肽基精氨酸脱胺酶抑制剂。
T9828	N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide 化合物 N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide	1965308-76-2	98%
T9828	N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide 是Cl-amidine (S 构型)的消旋形式。Cl-amidine 口服有效的 PAD 抑制剂。