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Furamidine

CAT: 0804-HY-110137ASize: 1 EachDry Ice: NoHazardous: No
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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].
CAS Number
73819-26-8
Product Name Alternative
DB75; NSC 305831
UNSPSC
12352005
Target
Histone Methyltransferase; Parasite; Phosphodiesterase (PDE)
Type
Reference compound
Related Pathways
Anti-infection; Epigenetics; Metabolic Enzyme/Protease
Applications
COVID-19-immunoregulation
Field of Research
Cancer; Infection; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/furamidine.html
Solubility
10 mM in DMSO
Smiles
N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N
Molecular Formula
C18H16N4O
Molecular Weight
304.35
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PRMT1
Citation 01
Research Square Print. September 20th, 2022.|Cell Rep. 2024 Aug 22;43 (9) :114662.|Int Immunopharmacol. 2025 Aug 8:164:115327.

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