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抑制剂描述:

产品名称:Cl-amidine TFA

产品别名:见爱必信官网

英文别名:Cl-amidine TFA

靶点:PAD

CAS:1043444-18-3

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Cl-amidine is a cell-permeable compound that acts as a pan PAD inhibitor (IC50 = 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively) in enzymatic assays.

溶解性:DMSO :84 mg/mL warmed (197.74 mM)
Ethanol :84 mg/mL warmed (197.74 mM)
Water :70 mg/mL warmed (164.78 mM)

体外研究:

Cl-amidine antagonizes the PAD4-mediated enhancement of the the p300GBD-GRIP1 interaction in a dose-dependent manner. The inhibitory effect of this compound is not a nonspecific one but is targeted at the active PAD4 enzyme. Cl-amidine increases p53 expression in CD45 positive immune cells. It triggers the differentiation and apoptosis of multiple cancer cell lines that are p53+/+ and p53?/? (e.g., HL60, HT29, TK6, and U2-OS cells). Cl-amidine induces the expression of p53 and several downstream target genes including the cyclin dependent kinase inhibitor p21, GADD45, and the proapoptotic protein PUMA in U2-OS osteosarcoma cells.

体内研究:Cl-amidine treatment inhibits NZM(New Zealand mixed 2328) NET(neutrophil extracellular trap) formation in vivo and significantly alters circulating autoantibody profiles and complement levels while reducing glomerular IgG deposition. Further, Cl-amidine increases the differentiation capacity of bone marrow endothelial progenitor cells, improves endothelium-dependent vasorelaxation, and markedly delays time to arterial thrombosis induced by photochemical injury. Cl-amidine delays thrombosis development in NZM mice. It inhibits PADs in mice without significant toxicity and improves disease phenotypes in animal models of inflammatory arthritis and inflammatory bowel disease. And It is shown to reduce disease severity in mouse models of ulcerative colitis and RA.

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