5.06046

PRMT Inhibitor VII, DB867

• Synonym(e): PRMT Inhibitor VII, DB867, 5-[5-(4-Carbamimidoyl-phenyl)-furan-2-yl]-pyridine-2-carboxamidine
• Empirische Formel (Hill-System): C₁₇H₁₅NO₅
• CAS-Nummer: 619334-60-0
• Molekulargewicht: 313.30
• UNSPSC-Code: 51111800
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Wirksamkeit: 9 μM IC₅₀
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: yellow
• Löslichkeit: 10% acetic acid: 5 mg/mL
• Lagertemp.: 2-8°C

Beschreibung

Allgemeine Beschreibung

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. Wirkung

Primary Target
PRMT1

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Sonstige Hinweise

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

Rechtliche Hinweise

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

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable