D-Cl-amidine

Names

[ CAS No. ]:
1404060-15-6

[ Name ]:
D-Cl-amidine

Biological Activity

[Description]:

D-Cl-amidine is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Protein Arginine Deiminase

[In Vitro]

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].

[In Vivo]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C14H19ClN4O2

[ Molecular Weight ]:
310.78

Related Compounds