| 货号 | 17079-5mg |
| 描述 | Protein arginine deiminase 4 (PAD4) catalyzes the post-translational modification of arginine residues on histones to form citrulline, which can alter gene expression.1 Dysregulated PAD4 activity has been implicated in cancer and rheumatoid arthritis.1,2 Cl-amidine (Item No.10599) is an inhibitor of PAD4 deimination activity with an IC50 value of 5.9 μM in an in vitro activity assay.3 BB-Cl-Amidine is a Cl-amidine derivative that retains functional components but possesses a C-terminal benzimidazole designed to limit proteolysis of the C-terminal amide.4 The cellular potency of BB-Cl-amidine against PAD4 activity is increased 20-fold over the parent compound (EC50 = 8.8 µM, vs. >200 µM for Cl-amidine).4 BB-Cl-Amidine also has a significantly longer in vivo half-life than Cl-amidine (1.75 h vs. ~15 min, respectively).4 Both compounds inhibit the formation of neutrophil extracellular traps without altering H2O2 production by neutrophils.4 BB-Cl-Amidine is effective in vivo, improving endothelial function while downregulating the expression of type I interferon-regulated genes in MRL/lprmice.4 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Jones, J.E.,Causey, C.P.,Knuckley, B., et al. Protein arginine deiminase 4 (PAD4): Current understanding and future therapeutic potential. Curr. Opin. Drug Discov. Devel. 12(5), 616-627 (2009). 2.Hill, J.A.,Southwood, S.,Sette, A., et al. Cutting edge: The conversion of arginine to citrulline allows for a high-affinity peptide interaction with the rheumatoid arthritis-associated HLA-DRB1*0401 MHC class II molecule. Journal of Immunology 171, 538-541 (2003). 3.Luo, Y.,Arita, K.,Bhatia, M., et al. Inhibitors and inactivators of protein arginine deiminase 4: Functional and structural characterization. Biochemistry 45(39), 11727-11736 (2006). 4.Knight, J.S.,Subramanian, V.,ODell, A.A., et al. Peptidylarginine deiminase inhibition disrupts NET formation and protects against kidney, skin and vascular disease in lupus-prone MRL/lpr mice. Annals of the Rheumatic Diseases 74(12), 2199-2206 (2015). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 460 |
| 分子式 | C26H26ClN5O |
| CAS号 | 1802637-39-3 |
| 稳定性 | ≥ 1 year |
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