|
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
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).
产品信息
Form Orange solid
Primary Target PRMT4
Primary Target IC50 CARM1-mediated methylation over PRMT1 and SET7 (IC50 = 7.1, 63 and 943 µM,
Secondary target SET7
Molar mass 555.3
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Reversible 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C26H21Br2NO3
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |