AMI-1

SKU: orb1225739

Description

A specific inhibitor of PRMTs (protein arginine methyltransferases), but not lysine methyltransferases; inhibits PRMT1 and Hmt1p with IC50s of 8.81 uM and 3.03 uM respectively; increases the ratio of Bax/Bcl-2, and leads to apoptosis and loss of migratory activity in several HCC cells,decreases the expression levels of H4R3me2s; strongly inhibits HCC growth in vivo.

Key Properties

• CAS Number: 20324-87-2
• MW: 548.4534
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₄N₂Na₂O₉S₂
• SMILES: O=C(NC1=CC2=CC(S(=O)([O-])=O)=CC(O)=C2C=C1)NC3=CC4=CC(S(=O)([O-])=O)=CC(O)=C4C=C3.[Na+].[Na+]
• Target: HMTase
• Solubility: DMSO: ≥ 46 mg/mL

Bioactivity

• In Vivo:
  AMI-1 (0.5 mg; intratumorally; daily; for 7 days) inhibits S180 viability In vivo. AMI-1 (0.5 mg; intratumorally; daily; for 7 days) downregulates PRMT5 but does not regulate the expression of PRMT7 in a tumor xenograft model. AMI-1 (0.5 mg; intratumorally; daily; for 7 days) decreases the levels of H4R3me2s and H3R8me2s in a tumor xenograft model. Animal model: 6-7 weeks old male Kunming mice (18-22 g), with S180 cells xenograft. Dosage: 0.5 mg. Administration: Intratumorally, daily, for 7 days. Result: Decreased tumor weight.
• In Vitro:
  AMI-1 can inhibit the in vitro methylation reactions performed by all five recombinantly active PRMTs (PRMT1, -3, -4, and -6 and Hmt1p). AMI-1 not only inhibits type I PRMTs (PRMT1, 3, 4 and 6) but also type II PRMT5. 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. AMI-1 (0.6-2.4 mM; 48-96 hours) inhibits the cell viability of sarcoma in S180 and U2OS cells in a time-dependent and dose-dependent manner in vitro. AMI-1 (1.2-2.4 mM; 48-72 hours) reduces S180 cell viability through the induction of cell apoptosis. Cell Viability Assay Cell line: S180 cells, U2OS cells. Concentration: 0.6 mM, 1.2 mM, 2.4 mM Incubation time: 48 hours, 72 hours, 96 hours. Result: Inhibited the cell viability. Apoptosis Analysis Cell line: S180 cells. Concentration: 1.2 mM, 2.4 mM Incubation time: 48 hours, 72 hours. Result: Increased the percentages of cells undergoing apoptosis.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AMI-1 | AMI 1 | AMI1 | AMI-1 disodium salt.

Quick Database Links

Gene Symbol

HMTase