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Products Details
Product Description
– Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent[1][2][3].
Web ID
– HY-110137A
Shipping
– Room temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C18H16N4O
References
– [1]Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-84.|[2]Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22.|[3]Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67.
CAS Number
– 73819-26-8
Molecular Weight
– 304.35
SMILES
– N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N
Clinical Information
– No Development Reported
Research Area
– Cancer; Infection; Inflammation/Immunology
Solubility
– 10 mM in DMSO
Target
– Histone Methyltransferase;Parasite;Phosphodiesterase (PDE)
Isoform
– PRMT1
Pathway
– Anti-infection;Epigenetics;Metabolic Enzyme/Protease
Product type
– Reference compound
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