AMI-1,HistoneMethyltransferaseInhibitor

Biological Activity:

AMI-1 is a potent and specific small molecule inhibitor of histone methyltransferase with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. It also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. In chronic AIPI rats, AMI-1 (5 μg/rat) ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs.

How to Use:

In vitro: AMI-1 was used at 10-30 µM final concentration in vitro and in cellular assays.
In vivo: AMI-1 was dosed by intranasal injection to Chronic AIPI rats at 50 μL (concentration of 0.1 mg/mL).

Reference:

• 1. Cheng D, et al. Small molecule regulators of protein arginine methyltransferases. (2004) J Biol Chem. 279(23):23892-9. 
• 2. Sun Q, et al. PRMT1 Upregulated by Epithelial Proinflammatory Cytokines Participates in COX2 Expression in Fibroblasts and Chronic Antigen-Induced Pulmonary Inflammation. (2015) J Immunol. 195(1):298-306. 

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