CARM1-IN-1

CARM1-IN-1 is a potent and specific CARM1(Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7(IC50 > 600 uM). IC50 value: 8.6 uM [1]Target: CRAM1 inhibitorin vitro: CARM1-IN-1(Cmp 7g) displayed high and selective CARM1 inhibition, with lower or no activity against a panel of different PRMTs or HKMTs. In human LNCaP cells, 7g showed a significant dose-dependent reduction of the PSA promoter activity.

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

Research Areas >> Cancer

[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.

GSK126 | Tazemetostat (EPZ-6438) | UNC 0642 | GSK343 | Pinometostat (EPZ5676) | 3-Deazaneplanocin A (hydrochloride) | Pemrametostat (GSK3326595) | UNC1999 | BIX-01294 | EPZ031686 | AZ505 (ditrifluoroacetate) | MS023 | EPZ 004777 | EPZ015666 | EPZ015866(GSK591)