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Submit ReviewFuramidine dihydrochloride
Description: Selective PRMT1 inhibitor
Chemical Name: 4,4'-(2,5-Furandiyl)bis-benzenecarboximidamide dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Furamidine dihydrochloride
Furamidine dihydrochloride is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor (IC50 = 9.4 μM). Exhibits selectivity over PRMT5, PRMT6 and CARM1 (IC50 values are 166, 283 and >400 μM respectively). Inhibits tyrosyl-DNA phosphodiesterase 1 (TDP-1) (IC50 = 1.2 μM). Inhibits cell proliferation in leukemia cell lines, suppresses neuroblastoma tumor growth, and reduces mis-splicing in in vitro and in vivo models of myotonic dystrophy type 1. Also shows dose-dependent inhibition of platelet aggregation (IC50 = 14.8 uM). Cell-permeable.
Compound Libraries for Furamidine dihydrochloride
Furamidine dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
Technical Data for Furamidine dihydrochloride
| M. Wt | 377.27 |
| Formula | C18H16N4O.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 55368-40-6 |
| PubChem ID | 462428 |
| InChI Key | VXNYQUQHOUERTR-UHFFFAOYSA-N |
| Smiles | NC(C(C=C3)=CC=C3C1=CC=C(C2=CC=C(C(N)=N)C=C2)O1)=N.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Furamidine dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 18.86 | 50 | |
| DMSO | 18.86 | 50 |
Preparing Stock Solutions for Furamidine dihydrochloride
The following data is based on the product molecular weight 377.27. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.3 mL | 26.51 mL | 53.01 mL |
| 2.5 mM | 1.06 mL | 5.3 mL | 10.6 mL |
| 5 mM | 0.53 mL | 2.65 mL | 5.3 mL |
| 25 mM | 0.11 mL | 0.53 mL | 1.06 mL |
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Product Datasheets for Furamidine dihydrochloride
References for Furamidine dihydrochloride
References are publications that support the biological activity of the product.
Yan et al (2014) Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J.Med.Chem. 57 2611 PMID: 24564570
Jenquin et al (2018) Furamidine rescues myotonic dystrophy type I associated mis-splicing through multiple mechanisms. ACS Chem.Biol. 13 2708 PMID: 30118588
Hua et al (2020) PRMT1 promotes neuroblastoma cell survival through ATF5. Oncogenesis 9 50 PMID: 32415090
Marsden et al (2021) Inhibition of arginine methylation impairs platelet function. ACS Pharmacol.Transl.Sci. 4 1567 PMID: 34661075
If you know of a relevant reference for Furamidine dihydrochloride, please let us know.
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Keywords: Furamidine dihydrochloride, Furamidine dihydrochloride supplier, Selective, protein, arginine, methyltransferase, 1, PRMT1, inhibitors, inhibits, leukemia, coactivator-associated, tdp1, tyrosyl, DNA, topoisomerase, Protein, Arginine, Methyltransferases, Phosphodiesterases, 5202, Tocris Bioscience
5 Citations for Furamidine dihydrochloride
Citations are publications that use Tocris products. Selected citations for Furamidine dihydrochloride include:
Marsden et al (2021) Inhibition of Arginine Methylation Impairs Platelet Function. ACS Pharmacol.Transl.Sci 4 1567 PMID: 34661075
Jer-Yen et al (2022) PRMT1 is an important factor for medulloblastoma cell proliferation and survival. Biochem Biophys Rep 32 101364 PMID: 36237442
Samuel et al (2018) Inhibiting Arginine Methylation as a Tool to Investigate Cross-Talk with Methylation and Acetylation Post-Translational Modifications in a Glioblastoma Cell Line. Proteomes 6 44 PMID: 30347783
Tang et al (2022) A genome-scale CRISPR screen reveals PRMT1 as a critical regulator of androgen receptor signaling in prostate cancer. Cell Rep. 38 110417 PMID: 35196489
Min-Jung et al (2020) TC-E 5003, a protein methyltransferase 1 inhibitor, activates the PKA-dependent thermogenic pathway in primary murine and human subcutaneous adipocytes. FEBS Lett 594 2923-2930 PMID: 32767856
Do you know of a great paper that uses Furamidine dihydrochloride from Tocris? Please let us know.
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Literature in this Area
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.