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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) Select Batch:

    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.
    Furamidine dihydrochloride 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.
    Furamidine dihydrochloride synergistically suppresses murine lupus nephritis in vivo combined with Irinotecan.
    Furamidine dihydrochloride 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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