product name AMI-1
Description: AMI-1 is a potent and specific Histone Methyltransferase (HMT) inhibitor with IC50 of 3.0 μM and 8.8 μM for yeast Hmt1p and human PRMT1, respectively. It is cell permeable and does not compete for the AdoMet (S-adenosyl-L-methionine, SAM) binding site, Blocks peptide substrate binding, HIV-1 RT polymerase inhibitor (IC50 = 5, 0 µM).
References: J Biol Chem. 2004 Jun 4;279(23):23892-9; J Immunol. 2015 Jul 1;195(1):298-306.
548.45
Formula
C21H14N2Na2O9S2
CAS No.
20324-87-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (182.3 mM)
Water: 10 mg/mL (18.2 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
PBS: 22mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. AMI-1 also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. In addition, AMI-1 inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. In INS-1 cells, AMI-1 improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | 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. |
| Animal model | Chronic AIPI rats |
| Formulation & Dosage | Dissolved in PBS; 50 μL at a concentration of 0.1 mg/mL; Intranasal injection |
| References | J Biol Chem. 2004 Jun 4;279(23):23892-9; J Immunol. 2015 Jul 1;195(1):298-306. |
