217531

CARM1 Inhibitor

The CARM1 Inhibitor controls the biological activity of CARM1. This small molecule/inhibitor is primarily used for Cell Structure applications.

• Sinonimo/i: CARM1 Inhibitor, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5- bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5- bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one, PRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one, PRMT Inhibitor V
• Formula empirica (notazione di Hill): C₂₆H₂₁Br₂NO₃
• Numero CAS: 1020399-49-8
• Peso molecolare: 555.26
• Numero MDL: MFCD23115307
• Codice UNSPSC: 12352200
• NACRES: NA.28

Proprietà

• Livello qualitativo: 100
• Saggio: ≥95% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: orange
• Solubilità: DMSO: 50 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: O=C(/C(CN(CC1=CC=CC=C1)C/2)=C/C3=CC=C(O)C(Br)=C3)C2=C\C4=CC(Br)=C(O)C=C4

Descrizione

Descrizione generale

A cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC₅₀ = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC₅₀ >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PRMT4

Reversible: yes

Secondary Target
SET7

Target IC₅₀: CARM1-mediated methylation over PRMT1 and SET7 (IC₅₀ = 7.1, 63 and 943 µM,

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Altre note

Cheng, D., et al. 2011. J. Med. Chem.54, 4928.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable