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| Cas No.: | 55368-40-6 |
| Chemical Name: | Benzenecarboximidamide,4,4'-(2,5-furandiyl)bis-, dihydrochloride (9CI) |
| Synonyms: | Benzenecarboximidamide,4,4'-(2,5-furandiyl)bis-, dihydrochloride (9CI);Furamidine Dihydrochloride;4-[5-(4-carbamimidoylphenyl)-2-furyl]benzenecarboximidamide;Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-, dihydrochloride;2,5-Furandiylbis(1,4-phenylene)bisformamidine;DB75;DB-75;Furamidine;WR-199385;2,5-Bis(4-amidinophenyl)furan dihydrochloride;4,4′-(2,5-Furandiyl)bis-benzenecarboximidamide dihydrochloride;DB 75;NSC 305831;WR199385 |
| SMILES: | NC(C1C=CC(C2=CC=C(C3C=CC(C(=N)N)=CC=3)O2)=CC=1)=N |
| Formula: | C18H16N4O |
| M.Wt: | 304.345843315125 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent[1][2][3]. |
| Target: | IC50: 9.4 μM (Protein arginine methyltransferase 1 (PRMT1)); 166 µM (PRMT5), 283 µM (PRMT6) and >400 µM (PRMT4)[1] Parasite[1] Tyrosyl-DNA phosphodiesterase 1 (TDP-1)[2] |
| In Vivo: | Furamidine (1 mg/kg; intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks; female NZB/NZW mice) and Irinotecan combined treatment suppresses proteinuria and prolongs survival of lupus-prone NZB/NZW mice. The combination treatment does not change the levels of anti-dsDNA antibodies[3]. Animal Model: Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)[3] 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. |
| In Vitro: | Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations[1]. Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells[1]. Furamidine 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. Furamidine could therefore interfere with DNA processing enzymes such as TDP-1[2]. Cell Viability Assay[1] 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[1] Cell Line: 293T cells Concentration: 20 μM Incubation Time: 15 hours Result: The expression level of the methylated GFP-ALY protein is significantly reduced. |
| References: | [1]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22. [2]. 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. [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. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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