AMI-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PRMT（蛋白质精氨酸甲基转移酶）的特异性抑制剂，但不是赖氨酸甲基转移酶。

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.

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 AnalysisCell Line:S180 cellsConcentration:1.2 mM, 2.4 mM Incubation Time:48 hours, 72 hours Result:Increased the percentages of cells undergoing apoptosis.

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.

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

Chromatin/Epigenetic

HMTase

PRMT1|yeastHmt1p

Inflammation/Immunology

——

20324-87-2

548.4534

C21H14N2Na2O9S2

>98% (HPLC)

DMSO: ≥ 46 mg/mL

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+]

2-Naphthalenesulfonic acid, 7,7'-(carbonyldiimino)bis[4-hydroxy-, sodium salt (1:2)

(-20℃)

With Ice Pack

≥ 2 years