Furamidine dihydrochloride

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Cat.No. 5202 - Furamidine dihydrochloride | C18H16N4O.2HCl | CAS No. 55368-40-6
Description: Selective PRMT1 inhibitor
Chemical Name: 4,4'-(2,5-Furandiyl)bis-benzenecarboximidamide dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (3)

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.

Select a batch to recalculate based on the batch molecular weight:
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.

View Related Products by Product Action

View all Protein Arginine Methyltransferase Inhibitors

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

3 Citations for Furamidine dihydrochloride

Citations are publications that use Tocris products. Selected citations for Furamidine dihydrochloride include:

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

Marsden et al (2021) Inhibition of Arginine Methylation Impairs Platelet Function. ACS Pharmacol.Transl.Sci 4 1567 PMID: 34661075

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


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Reviews for Furamidine dihydrochloride

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Literature in this Area

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