PRMT INHIBITOR VII DB867 (C15-1304-373)

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

Molecular Weight: 313.30. Empirical Formula: C₁₇H₁₅NO₅. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. potency: 9 . μ. M 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.