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Furamidine dihydrochloride

Chemical Structure : Furamidine dihydrochloride

CAS No.: 55368-40-6

Furamidine dihydrochloride (NSC 305831 dihydrochloride;WR 199385)

Catalog No.: PC-35608Not For Human Use, Lab Use Only.

Furamidine dihydrochloride (NSC 305831, WR 199385) is an inhibitor of tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Furamidine dihydrochloride (NSC 305831, WR 199385) is an inhibitor of tyrosyl-DNA phosphodiesterase (Tdp1), also is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with IC50 of 9.4 uM; exhibits selectivity over PRMT5, PRMT6 and CARM1 (>15-fold); binds duplex DNA in the DNA minor groove selectively at AT rich sites [(A/T)4], Furamidine can also intercalate between GC base pairs of duplex DNA, bind CTG-CAG repeat DNA with nanomolar affinity; synergistically suppresses murine lupus nephritis in vivo combined with Irinotecan; effectively inhibits intracellular PRMT1 activity and blocks cell proliferation in leukemia cell lines with different genetic lesions.

Physicochemical Properties

M.Wt 377.269
Formula C18H18Cl2N4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-, dihydrochloride (9CI)

References

1. Antony S, et al. Nucleic Acids Res. 2007;35(13):4474-84.

2. Jenquin JR, et al. ACS Chem Biol. 2018 Aug 27. doi: 10.1021/acschembio.8b00646.

3. Keil A, et al. Arthritis Rheumatol. 2015 Jul;67(7):1858-67.

4. Yan L, et al. J Med Chem. 2014 Mar 27;57(6):2611-22.

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