CARM1 Inhibitor (1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, PRMT Inhibitor V)

Size

£358.00

SKU:: 217249
Molecular Weight:: 555.3
Purity:: ~95% (HPLC)
Storage Conditions:: 4°C
Supplier:: United States Biological
Format:: Supplied as a orange solid.
Extra Details:: 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.