A cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50=7.1uM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100uM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50>100uM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100uM 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 6uM inhibitor).
Formula:C26H21Br2NO3
Primary Target:PRMT4
Primary Target IC50:CARM1-mediated methylation over PRMT1 and SET7 (IC50 = 7.1, 63 and 943uM
Secondary target:SET7
Molecular Weight:555.3
Solubility:DMSO
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
