CARM1-IN-1 (Synonyms: Protein Arginine Methyltransferase 4/CoactivatorAssociated Arginine Methyltransferase 1 Inhibitor) |
| رقم الكتالوجGC34108 |
CARM1-IN-1 عبارة عن مثبط CARM1 قوي ومحدد (مرتبط بمنشطات arginine methyltransferase 1) مع IC50 يبلغ 8.6 ميكرومتر ؛ يُظهر نشاطًا منخفضًا جدًا مقابل PRMT1 و SET7 (IC50> 600 uM)
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Cas No.: 1020399-49-8
Sample solution is provided at 25 µL, 10mM.
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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.
[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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