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Search Results for " protein arginine deiminase "

13

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8861	GSK199	PAD	Chromatin/Epigenetic
	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。
T22277	BMS-P5	PAD	Chromatin/Epigenetic
	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。
T24105	GSK121 GSK-121,GSK 121	PAD	Chromatin/Epigenetic
	GSK121 Trifluoroacetate 是PAD4的选择性抑制剂。
T10831L	Cl-amidine hydrochloride	Apoptosis; PAD	Apoptosis; Chromatin/Epigenetic
	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。
T22277L	BMS-P5 free base	PAD	Chromatin/Epigenetic
	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。
TQ0067	GSK484 hydrochloride GTPL8577,AOB6992,GSK484盐酸盐	PAD	Chromatin/Epigenetic
	GSK484 hydrochloride (GTPL8577) 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。
T36393	CAY10727
	CAY10727 is an inhibitor of protein arginine deiminase 3 (PAD3; kinact/KI= 15,600 M-1min-1).1It is selective for PAD3 over PAD1, -2, and -4 (kinact/KIs = 360, 1,110, and 1,460 M-1min-1, respectively). 1.Jamali, H., Khan, H.A., Stringer, J.R., et al.Identification of multiple structurally distinct, nonpeptidic small molecule inhibitors of protein arginine deiminase 3 using a substrate-based fragment methodJ. Am. Chem. Soc.137(10)3616-3621(2015)
T39515	PAD2-IN-1 PAD2-IN-1
	PAD2-IN-1, a benzimidazole-based derivative, is an efficacious and specific inhibitor of protein arginine deiminase 2 (PAD2). Demonstrating remarkable selectivity, PAD2-IN-1 exhibits a 95-fold higher affinity for PAD2 in comparison to PAD4 and a 79-fold higher affinity than PAD3.
T63601	PAD2-IN-1 hydrochloride
	PAD2-IN-1 hydrochloride 是有效的、选择性的蛋白精氨酸脱亚氨酶 2 (PAD2) 抑制剂，且对 PAD2 的选择性优于 PAD4 (95 倍) 和 PAD3 (79 倍)，是一种基于苯并咪唑的衍生物。
T36632	BB-Cl-Yne
	BB-Cl-Yne is a cell-permeable derivative of the protein arginine deiminase (PAD) inhibitor BB-Cl-amidine 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 labeling PADs in cell-free and cell-based assays, followed by click reactions with azide-modified TAMRA or biotin reporters.
T36108	YW3-56 (hydrochloride) (technical grade) YW3-56 (hydrochloride) (technical grade)
	YW3-56 is an inhibitor of protein arginine deiminase 2 (PAD2) and PAD4 (IC50s = 0.5-1 and 1-5 μM, respectively).1It inhibits the growth of U2OS osteosarcoma cells (IC50= ~2.5 μM) in a p53-dependent mannerviainduction of SESN2 and subsequent inhibition of mTORC1. YW3-56 (10 mg/kg) reduces tumor growth in an S-180 murine sarcoma tumor model. It also inhibits tumor growth in the 1883 MDA-MB-231 breast cancer bone metastasis mouse xenograft model.2 1.Wang, Y., Li, P., Wang, S., et al.Anticancer pept...
T35817	Photoswitchable PAD Inhibitor (technical grade)
	Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK29...
T63423	AFM-30a hydrochloride
	AFM-30a hydrochloride 是一种有效的、高度选择性的蛋白质精氨酸脱亚胺酶 2(PAD2) 抑制剂。AFM-30a hydrochloride 能够与 PAD2 结合 (EC50: 9.5 μM)，也能够抑制 H3 瓜氨酸化 (EC50: 0.4 μM)。AFM-30a hydrochloride 能够用于研究某些癌症和多种自身免疫性疾病如类风湿性关节炎 (RA)、多发性硬化症、狼疮和溃疡性结肠炎。

化合物

Cat.No: T8861

Target: PAD

Cat.No: T22277

Target: PAD

Cat.No: T24105

Synonym: GSK-121,GSK 121

Target: PAD

Cl-amidine hydrochloride

Cat.No: T10831L

Target: Apoptosis, PAD

BMS-P5 free base

Cat.No: T22277L

Target: PAD

GSK484 hydrochloride

Cat.No: TQ0067

Synonym: GTPL8577,AOB6992,GSK484盐酸盐

Target: PAD

Cat.No: T36393

Cat.No: T39515

Synonym: PAD2-IN-1

PAD2-IN-1 hydrochloride

Cat.No: T63601

Cat.No: T36632

YW3-56 (hydrochloride) (technical grade)

Cat.No: T36108

Synonym: YW3-56 (hydrochloride) (technical grade)

Photoswitchable PAD Inhibitor (technical grade)

Cat.No: T35817

AFM-30a hydrochloride

Cat.No: T63423

Cat. No.	Product Name	Target	Signaling Pathways
T2205	Acefylline Theophylline-7-acetic acid,茶碱乙酸,Carboxymethyltheophylline,acetyloxytheophylline,Theophyllineacetic acid	TNF; PAD; PKA; HDAC; PDE; Adenosine Receptor	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience; Tyrosine Kinase/Adaptors
	Acefylline (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。

天然产物

Cat.No: T2205

Synonym: Theophylline-7-acetic acid,茶碱乙酸,Carboxymethyltheophylline,acetyloxytheophylline,Theophyllineacetic acid

Target: TNF, PAD, PKA, HDAC, PDE, Adenosine Receptor

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