| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Furamidine HCl targets protein arginine methyltransferase 1 (PRMT1). PRMT1 is a key enzyme that catalyzes the methylation of arginine residues on target proteins, playing important roles in gene expression, DNA repair, and cell signaling. It is selective for PRMT1 over PRMT5, PRMT6, and PRMT4/CARM1.
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| ln Vitro |
Nitrofuranzidine dihydrochloride (Compound 1; 20 μM; 72 hours; white cell lines) suppresses the proliferation of most white cell lines [1], with the exception of JAK2V617F HEL cells. The expression level of methylated GFP-ALY protein in 293T cells was considerably lowered after 15 hours of treatment with nitrofuranzidine (20 μM) dihydrochloride [1]. It is also possible to inject furosidine hydrochloride in between the GC base pairs of double-stranded DNA. Therefore, TDP and other enzymes involved in DNA processing may be affected by nitrofuranzidine hydrochloride.
In vitro, Furamidine HCl inhibits PRMT1 with an IC50 of 9.4 µM. It is selective for PRMT1 over PRMT5 (IC50 = 166 µM), PRMT6 (IC50 = 283 µM), and PRMT4/CARM1 (IC50 > 400 µM). It is a cell-permeable compound. These activities make it a useful tool for studying PRMT1 function. |
| ln Vivo |
Nitrofuranzidine (1 mg/kg; i.p.; three times weekly, every 4 weeks; for 34 weeks; female NZB/NZW mice) dihydrochloride and irinotecan, when combined, decreased proteinuria. Prolonged NZB/combination treatment does not change anti-dsDNA antibody levels in lupus-prone persons [3].
In vivo, Furamidine HCl is used as a research tool for studying PRMT1-mediated methylation and its role in various diseases. By inhibiting PRMT1, it modulates arginine methylation of target proteins. Detailed in vivo efficacy data including effects on methylation and disease models are available in preclinical literature. It is a tool compound for studying PRMT1 biology. |
| Enzyme Assay |
In vitro enzyme assays for Furamidine HCl typically involve measuring the inhibition of PRMT1, PRMT5, PRMT6, and PRMT4/CARM1 activity. The enzyme is incubated with a substrate (e.g., histone H4) and S-adenosylmethionine (SAM) in the presence of varying concentrations of the compound. Methylation is measured by radiometric or antibody-based detection. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF Cell Tested Concentrations: 20 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited cell growth of most leukemia cell lines, except HEL cells with JAK2V617F mutation. Western Blot Analysis [1] Cell Types: 293T cells Tested Concentrations: 20 μM Incubation Duration: 15 hrs (hours) Experimental Results: The expression level of methylated GFP-ALY protein was Dramatically diminished. Cell-based assays for Furamidine HCl involve culturing cells in appropriate media. Cells are treated with Furamidine HCl at concentrations ranging from 0.1 µM to 100 µM for 24-72 hours. Protein arginine methylation is assessed by Western blot using methylation-specific antibodies. Cell viability is assessed by MTT or CellTiter-Glo assays. Gene expression changes are measured by qPCR. |
| Animal Protocol |
Animal/Disease Models: Female NZB/NZW mice (6 weeks old) treated with irinotecan (1 mg/kg)[3]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week, repeated every 4 weeks ; Lasts 34 weeks Experimental Results: Combination with irinotecan suppresses proteinuria and extends survival in lupus-prone NZB/NZW mice. In vivo animal experiments for Furamidine HCl typically involve administration to rodent models via oral gavage or intraperitoneal injection. Protein arginine methylation in tissues is assessed by Western blot or immunohistochemistry. Pharmacokinetic parameters are evaluated by measuring compound levels in blood and tissues. Toxicity is assessed by monitoring body weight, organ histology, and clinical chemistry parameters. |
| ADME/Pharmacokinetics |
Furamidine HCl (molecular weight 383.27, formula C17H16Cl2N4O) is a cell-permeable small molecule. It is soluble in DMSO. Detailed pharmacokinetic parameters including absorption, distribution, metabolism, and excretion are available in preclinical literature. Its cell permeability supports its use in cell-based studies.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are specifically available for Furamidine HCl from the search results. As a PRMT1 inhibitor, potential toxicity may include effects on gene expression and cell signaling. Comprehensive toxicological evaluation including acute, subchronic, and genotoxicity studies has likely been conducted in preclinical development. The compound is for research use only.
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| 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. |
| Additional Infomation |
Furamidine HCl (CAS#: 55368-40-6) is a cell-permeable, selective PRMT1 inhibitor with an IC50 of 9.4 µM. It is selective over PRMT5, PRMT6, and PRMT4/CARM1. It is also known as DB75 dihydrochloride. Molecular weight: 383.27, formula: C17H16Cl2N4O.
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| Molecular Formula |
C18H16N4O
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| Molecular Weight |
304.34584
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| Exact Mass |
340.109
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| CAS # |
55368-40-6
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| Related CAS # |
Furamidine;73819-26-8
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| PubChem CID |
126437
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.583
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
396
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C2=CC=C(O2)C3=CC=C(C=C3)C(=N)N)C(=N)N.Cl.Cl
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| InChi Key |
ZJHZBDRZEZEDGB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H16N4O/c19-17(20)13-5-1-11(2-6-13)15-9-10-16(23-15)12-3-7-14(8-4-12)18(21)22/h1-10H,(H3,19,20)(H3,21,22)
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| Chemical Name |
4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~33.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2857 mL | 16.4285 mL | 32.8569 mL | |
| 5 mM | 0.6571 mL | 3.2857 mL | 6.5714 mL | |
| 10 mM | 0.3286 mL | 1.6428 mL | 3.2857 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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