5.06046

PRMT Inhibitor VII, DB867

• Synonym(s): PRMT Inhibitor VII, DB867, 5-[5-(4-Carbamimidoyl-phenyl)-furan-2-yl]-pyridine-2-carboxamidine
• Empirical Formula (Hill Notation): C₁₇H₁₅NO₅
• CAS Number: 619334-60-0
• Molecular Weight: 313.30
• UNSPSC Code: 51111800
• NACRES: NA.77

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 100
• form: solid
• potency: 9 μM IC₅₀
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: 10% acetic acid: 5 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable biscarboxamidine derivative that acts as a selective inhibitor of protein arginine methyltransferase 1 (PRMT1; IC₅₀ = 9.5 µM). Exhibits about 10-fold greater selectivity over PRMT5 (IC₅₀ = 110 µM) and PRMT6 (IC₅₀ = 118 µM). Shown to block BMP4-induced phosphorylation and activation of Smad1/Smad5 and asymmetric dimethylation of Arg3 on histone 4 (H4R3) in HaCaT cells transfected with PRMT1.

A cell-permeable biscarboxamidine derivative that acts as a selective inhibitor of protein arginine methyltransferase 1 (PRMT1; IC₅₀ = 9.5 µM). Exhibits about 10-fold greater selectivity over PRMT5 (IC₅₀ = 110 µM) and PRMT6 (IC₅₀ = 118 µM). Shown to block BMP4-induced phosphorylation and activation of Smad1/Smad5 and asymmetric dimethylation of Arg3 on histone 4 (H4R3) in HaCaT cells transfected with PRMT1.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Primary Target
PRMT1

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Xu, J., et al, 2013. Mol. Cell.51, 1.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable