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AMI-1 disodium salt

Cat. No. M10495
AMI-1 disodium salt Structure
Synonym:

AMI1

Size Price Availability Quantity
10mg USD 133  USD133 In stock
25mg USD 265  USD265 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

AMI-1 is a potent and selective, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50 values of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 is also a potent scavenger of NADPH-oxidase-derived superoxide. AMI-1 specifically inhibits arginine, but not lysine, methyltransferase activity in vitro and does not compete for the AdoMet binding site. AMI-1 inhibits methylation of GFP-Npl3 and cellular proteins.

In vivo, AMI-1 (5 μg/rat) in chronic AIPI rats ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 548.45
Formula C21H14N2Na2O9S2
CAS Number 20324-87-2
Purity >98.5%
Solubility DMSO 45 mg/mL
Water 10 mg/mL
Storage at -20°C
References

[1] Baolai Zhang, et al. Oncol Lett. Arginine methyltransferase inhibitor-1 inhibits sarcoma viability in vitro and in vivo

[2] Baolai Zhang, et al. Oncotarget. Targeting protein arginine methyltransferase 5 inhibits colorectal cancer growth by decreasing arginine methylation of eIF4E and FGFR3

[3] Qingzhu Sun, et al. J Immunol. PRMT1 Upregulated by Epithelial Proinflammatory Cytokines Participates in COX2 Expression in Fibroblasts and Chronic Antigen-Induced Pulmonary Inflammation

[4] Donghang Cheng, et al. J Biol Chem. Small molecule regulators of protein arginine methyltransferases

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AMI-1 disodium salt, AMI1 supplier, PRMTs, inhibitors

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