Cas No.: | 1020399-49-8 |
Chemical Name: | CARM1-IN-1 |
Synonyms: | CARM1-IN-1;PRMT4/CARM1 Inhibitor |
SMILES: | O=C1/C(CN(CC2=CC=CC=C2)C/C1=C\C3=CC=C(O)C(Br)=C3)=C/C4=CC=C(O)C(Br)=C4 |
Formula: | C26H21Br2NO3 |
M.Wt: | 555.257845640183 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | CARM1-IN-1 is a potent, selective coactivator-associated arginine methyltransferase 1 (CARM1) with IC50 of 8.6 uM, exhibits lower or no activity against a panel of different PRMTs or HKMTs (>80-fold over PRMT1 and SET7); inhibits CARM1-mediated methylation of different substrates (PABP1, CA150, SmB, and H3) up to single-digit micromolar level, significantly and dose-dependently reduces the prostate-specific antigen (PSA) promoter activity in human prostate cancer LNCaP cells, does not affect cell viability. |
References: | [1]. Cheng D, et al. Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity. J Med Chem. 2011 Jul 14;54(13):4928-32. |