Furamidine dihydrochloride
Based on 4 publication(s) in Google Scholar
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.
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- Purity : 99.0%
- CAS No.: 55368-40-6
- 화학식: C18H18Cl2N4O
- 분자량:377.27
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Furamidine dihydrochloride
MoreAll Histone Methyltransferase Isoforms
MoreAll Parasite Isoforms
More
Biological Activity
제품 설명
IC50 & Target
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PRMT1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| B16 | IC50 |
9.2 μM
Compound: DB75
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Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation
Drug concentration required to inhibit B16 cell growth by 50% after 72 hours of incubation
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[PMID: 11985467] |
| HEK293 | IC50 |
178.04 μM
Compound: 7e; DB75
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Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay
Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 24 hrs by Alamar blue assay
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[PMID: 28038325] |
| HEK-293T | IC50 |
166 μM
Compound: 1, DB75, furamidine
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Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay
Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 mins by P81 filter binding assay
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[PMID: 24564570] |
| L6 | IC50 |
23.3 μM
Compound: FMD, DB75, Furamidine
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Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs
Antiprotozoal activity against intracellular amastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ infected in rat L6 cells after 48 hrs
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[PMID: 23795673] |
| L6 | IC50 |
6.4 mM
Compound: FMD
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Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay
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[PMID: 23871911] |
| L6 | IC50 |
6.4 nM
Compound: Furamidine
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Cytotoxicity against rat L6 cells by alamar blue assay
Cytotoxicity against rat L6 cells by alamar blue assay
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[PMID: 17178177] |
| L6 | IC50 |
6.4 μM
Compound: FMD
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Cytotoxicity against rat L6 cells by Alamar blue assay
Cytotoxicity against rat L6 cells by Alamar blue assay
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[PMID: 34146914] |
| L6 | IC50 |
6.4 μM
Compound: FMD, DB75, Furamidine
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Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay
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[PMID: 23795673] |
| L6 | IC50 |
6.4 μM
Compound: FMD, Furamidine
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Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
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[PMID: 24268543] |
| L6 | IC50 |
6.4 μM
Compound: Furamidine
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Cytotoxicity against rat L6 cells by alamar blue assay
Cytotoxicity against rat L6 cells by alamar blue assay
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[PMID: 21194955] |
| L6 | IC50 |
6400 nM
Compound: 2a
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Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay
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[PMID: 24012380] |
In Vitro
Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) dihydrochloride inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations[1].
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Furamidine (compound 1; 20 μM; 15 hours; 293T cells) dihydrochloride significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells[1].
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Furamidine dihydrochloride can also intercalate between GC base pairs of duplex DNA. Furamidine dihydrochloride could therefore interfere with DNA processing enzymes such as TDP-1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
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Concentration:20 μM
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Incubation Time:72 hours
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Result:Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.
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Cell Line:293T cells
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Concentration:20 μM
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Incubation Time:15 hours
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Result:The expression level of the methylated GFP-ALY protein is significantly reduced.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)[3]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
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Result:Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.
Chemical Information
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CAS No. 55368-40-6
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Appearance Solid
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분자량 377.27
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화학식 C18H18Cl2N4O
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Color Light yellow to yellow
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SMILES
N=C(C1=CC=C(C2=CC=C(C3=CC=C(C(N)=N)C=C3)O2)C=C1)N.[H]Cl.[H]Cl
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Synonyms
DB75 dihydrochloride; NSC 305831 dihydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Antioxidants (Basel)
A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]2026 May 12;15(5):612. PMID: 42193234 -
Cell Rep
CRISPR screening identifies PRMT1 as a key pro-ferroptotic gene via a two-layer regulatory mechanism. [Abstract]2024 Aug 22;43(9):114662. PMID: 39178116 -
Int Immunopharmacol
DB75 targets PRMT1 to suppress liver metastasis and synergizes with PD-L1 blockade for enhanced therapeutic efficacy. [Abstract]2025 Oct 30:164:115327. PMID: 40782428 -
용액&용해도
In Vitro:
DMSO : 12.5 mg/mL (33.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.31 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
순도&문서
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6506 mL | 13.2531 mL | 26.5062 mL | 66.2655 mL |
| 5 mM | 0.5301 mL | 2.6506 mL | 5.3012 mL | 13.2531 mL | |
| 10 mM | 0.2651 mL | 1.3253 mL | 2.6506 mL | 6.6266 mL | |
| 15 mM | 0.1767 mL | 0.8835 mL | 1.7671 mL | 4.4177 mL | |
| 20 mM | 0.1325 mL | 0.6627 mL | 1.3253 mL | 3.3133 mL | |
| 25 mM | 0.1060 mL | 0.5301 mL | 1.0602 mL | 2.6506 mL | |
| 30 mM | 0.0884 mL | 0.4418 mL | 0.8835 mL | 2.2089 mL |
Furamidine dihydrochloride Related Classifications
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