CARM1-IN-1

• CAT Number: I000146
• CAS Number: 1020399-49-8
• Molecular Formula: C26H21Br2NO3
• Molecular Weight: 555.26
• Purity: ≥95%
• Synonyms: (3E,5E)-1-benzyl-3,5-bis[(3-bromo-4-hydroxyphenyl)methylidene]piperidin-4-one
• InChI: InChI=1S/C26H21Br2NO3/c27-22-12-18(6-8-24(22)30)10-20-15-29(14-17-4-2-1-3-5-17)16-21(26(20)32)11-19-7-9-25(31)23(28)13-19/h1-13,30-31H,14-16H2/b20-10+,21-11+
• InChIKey: KNMFTTWVELIVCC-CLVAPQHMSA-N
• SMILES: C1C(=CC2=CC(=C(C=C2)O)Br)C(=O)C(=CC3=CC(=C(C=C3)O)Br)CN1CC4=CC=CC=C4

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 inhibitor
in 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.

Reference

[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.
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