D-Cl-amidine hydrochloride是有效的、高度选择性的 PAD1 抑制剂。D-Cl-amidine 耐受性好、无明显毒性。
D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity[1].
D-Cl-amidine (200-400 μM) is effective in significantly decreasing cell viability in MDA-MB-231 cells[1].D-Cl-amidine increase caspase 3 activity, indicating that inhibition of PAD1 leads to an increase in apoptosis[1].
D-Cl-amidine, administered by iv at a dose of 2.5 mg/kg, is still detected after 2 h in serum at a concentration of ~21 nM and at 4 h at ~10 nM. D-Cl-amidine is still observed in the blood serum at a concentration of ～10 nM at 4 h when administered by ip at a dose of 10 mg/kg[1].
[1]. Bicker KL, et al. D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. ACS Med Chem Lett. 2012 Oct 26;3(12):1081-1085.
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