A cell-permeable inhibitor with selectivity for PRMT1 (IC50 = 9.4 μM) over PRMT5

Furamidine (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
55368-40-6
Storage:
-20
UN-No:
Non-Hazardous - /

Furamidine is a cell-permeable inhibitor of protein arginine methyltransferase 1 (PRMT1) that is selective for PRMT1 over PRMT5, PRMT6, and PRMT4/coactivator-associated arginine methyltransferase 1 (CARM1) (IC50s = 9.4, 166, 283, and >400 μM, respectively).{38288} In vitro, furamidine (20 μM) inhibits Aly protein methylation in HEK293T cells and growth of several leukemia cell lines. It inhibits tyrosyl-DNA phosphodiesterase (Tdp1) activity on both single- and double-stranded DNA substrates with concentrations in the low micromolar range, but it is more potent against a duplex DNA substrate.{38289} Furamidine inhibits growth of T. brucei, the parasite that causes sleeping sickness, with IC50 values of 1.5 to 37 nM across various strains.{38290} It inhibits the T. brucei P2 aminopurine transporter (Ki = 1.2 μM).{38290} It also binds to AT-rich DNA sequences in trypanosome kinetoplast DNA.{38292,38293,38291}  

 

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Description

A cell-permeable inhibitor with selectivity for PRMT1 (IC50 = 9.4 μM) over PRMT5, PRMT6, and PRMT4/CARM1 (IC50s = 166, 283, and >400 μM, respectively); inhibits Aly protein methylation in HEK293T cells and growth of several leukemia cell lines when used at a concentration of 20 μM; inhibits Tdp1 activity on single- and double-stranded DNA with concentrations in the low micromolar range; inhibits T. brucei (IC50 values of 1.5 to 37 nM across various strains); inhibits the T. brucei P2 aminopurine transporter (Ki = 1.2 μM); binds to AT-rich DNA sequences,

Formal name: 4,4′-(2,5-furandiyl)bis-benzenecarboximidamide, dihydrochloride

Synonyms: 

Molecular weight: 377.3

CAS: 55368-40-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Antiparasitics|Antiprotozoals||Product Type|Biochemicals|Small Molecule Inhibitors|Methyltransferases||Research Area|Epigenetics, Transcription, & Translation|Writers||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Parasitic Diseases|African Sleeping Sickness

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