IC50: 0.78 and 1.41 μM for Hmt1p and PRMT1, respectively AMI5 is a non-selective protein methyltransferase inhibitor. Post-translational protein methylation at lysine and arginine residues is related to the gene expression regulation. The enzymatic activities of protein methyltransferases serve to do covalent modifications in the control of gene transcription. In vitro: AMI-5 has been identified as a competitive inhibitor of SAM binding and had been shown to inhibit not only PRMTs but also lysine methylation by the Set7 and disruptor of telomeric silencing 1-like (DOT1L) MTases in vitro. Both AMI-5 and its analog AMI-1 have been used as lead compounds for the development of novel MTase-specific inhibitors. Moreover, it was found that AMI-5 could inhibit Set7 in vitro and decrease H3K4m1 in vascular endothelial cells. . In vivo: Currently, there is no animal study reported. Clinical trial: Up to now, AMI-5 is still in the preclinical development stage.

Product information

CAS Number: 17372-87-1

Molecular Weight: 691.85

Formula: C20H6Br4Na2O5

Chemical Name: disodium 2-(2,4,5,7-tetrabromo-6-oxido-3-oxo-3H-xanthen-9-yl)benzoate

Smiles: [Na+].[Na+].[O-]C(=O)C1=CC=CC=C1C1C2=CC(Br)=C([O-])C(Br)=C2OC2C=1C=C(Br)C(=O)C=2Br

InChiKey: SEACYXSIPDVVMV-UHFFFAOYSA-L

InChi: InChI=1S/C20H8Br4O5.2Na/c21-11-5-9-13(7-3-1-2-4-8(7)20(27)28)10-6-12(22)17(26)15(24)19(10)29-18(9)14(23)16(11)25;;/h1-6,25H,(H,27,28);;/q;2*+1/p-2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.