Furamidine dihydrochloride

Research use only, not for human use.

Furamidine dihydrochloride (NSC 305831, WR 199385) is an inhibitor of tyrosyl-DNA phosphodiesterase (Tdp1).

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.

Cell Viability Assay Cell Line:Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells Concentration:20 μM Incubation Time:72 hours Result:Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.Western Blot Analysis Cell Line:293T cells Concentration:20 μM Incubation Time:15 hours Result:The expression level of the methylated GFP-ALY protein is significantly reduced.

Animal Model:Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)Dosage:1 mg/kg Administration:Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks Result:Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.

NSC 305831 dihydrochloride | WR 199385

Chromatin/Epigenetic

HMTase

HMTase

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55368-40-6

377.269

C18H18Cl2N4O

>98% (HPLC)

In Vitro:?DMSO : 12.5 mg/mL (33.13 mM)

C1=CC(=CC=C1C2=CC=C(O2)C3=CC=C(C=C3)C(=N)N)C(=N)N

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

(-20℃)

With Ice Pack

≥ 2 years