AMI-1 - CAS 20324-87-2
Catalog number: 20324-87-2
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H14N2Na2O9S2
Molecular Weight:
548.45
COA:
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Targets:
HMTase
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.
Purity:
98%
Appearance:
Solid powder
Synonyms:
AMI 1; AMI1; AMI-1 disodium salt.
Solubility:
DMSO,100mg/mLwarmed(182.33mM);Water,10mg/mL(18.23mM);Ethanol,<1mg/mL(<1mM)
Storage:
3 years -20℃powder;6 months-80℃in solvent
MSDS:
Inquire
Shelf Life:
2 years if stored properly
Canonical 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+]
1.Arginine methyltransferase inhibitor 1 inhibits gastric cancer by downregulating eIF4E and targeting PRMT5.
Zhang B;Zhang S;Zhu L;Chen X;Zhao Y;Chao L;Zhou J;Wang X;Zhang X;Ma N Toxicol Appl Pharmacol. 2017 Dec 1;336:1-7. doi: 10.1016/j.taap.2017.10.002. Epub 2017 Oct 4.
Arginine methylation is carried out by protein arginine methyltransferase (PRMTs) family. Arginine methyltransferase inhibitor 1 (AMI-1) is mainly used to inhibit type I PRMT activity in vitro. However, the effects of AMI-1 on type II PRMT5 activity and gastric cancer (GC) remain unclear. In this study, we provided the first evidence that AMI-1 significantly inhibited GC cell proliferation and migration while induced GC cell apoptosis, and reduced the expression of PRMT5, eukaryotic translation initiation factor 4E (eIF4E), symmetric dimethylation of histone 3 (H3R8me2s) and histone 4 (H4R3me2s). In addition, AMI-1 inhibited tumor growth, downregulated eIF4E, H4R3me2s and H3R8me2s expression in mice xenografts model of GC. Collectively, our results suggest that AMI-1 inhibits GC by downregulating eIF4E and targeting type II PRMT5.
2.Targeting protein arginine methyltransferase 5 inhibits colorectal cancer growth by decreasing arginine methylation of eIF4E and FGFR3.
Zhang B;Dong S;Zhu R;Hu C;Hou J;Li Y;Zhao Q;Shao X;Bu Q;Li H;Wu Y;Cen X;Zhao Y Oncotarget. 2015 Sep 8;6(26):22799-811.
Protein arginine methyltransferases (PRMTs) plays critical roles in cancer. PRMT5 has been implicated in several types of tumors. However, the role of PRMT5 in cancer development remains to be fully elucidated. Here, we provide evidence that PRMT5 is overexpressed in colorectal cancer (CRC) cells and patient-derived primary tumors, correlated with increased cell growth and decreased overall patient survival. Arginine methyltransferase inhibitor 1 (AMI-1)strongly inhibited tumor growth, increased the ratio of Bax/Bcl-2, and induced apoptosis in mouse CRC xenograt model. AMI-1 also induced apoptosis and decreased the migratory activity in several CRC cells. In CRC xenografts AMI-1 significantly decreased symmetric dimethylation of histone 4 (H4R3me2s), a histone mark of type II PRMT5, but not the expression of H4R3me2a, a histone mark of type I PRMTs. These results suggest that the inhibition of PRMT5 contributes to the antitumor efficacy of AMI-1. Chromatin immunoprecipitation (ChIP) identified FGFR3 and eIF4E as two key genes regulated by PRMT5. PRMT5 knockdown reduced the levels of H4R3me2s and H3R8me2s methylation on FGFR3 and eIF4E promoters, leading to decreased expressions of FGFR3 and eIF4E.
3.Lactate induced HIF-1α-PRMT1 cross talk affects MHC I expression in monocytes.
Gupta P;Singh A;Gowda P;Ghosh S;Chatterjee A;Sen E Exp Cell Res. 2016 Oct 1;347(2):293-300. doi: 10.1016/j.yexcr.2016.08.008. Epub 2016 Aug 9.
Tumor infiltrating monocytes play a crucial role in tumor immune surveillance. As lactate is an important component of the tumor milieu, we investigated its role in the transcriptional regulation of MHC I which is crucial for mounting effective immune responses against tumors. Lactate elevated MHC class I expression in monocytes. Increase in HLAB expression was concomitant with increase in HIF-1α and decrease in PRMT1 levels. Interestingly, a reciprocal relationship was observed between PRMT1 and HIF-1α. While HIF-1α inhibition decreased lactate induced MHC I, both pharmacological inhibition and siRNA mediated knockdown of PRMT1 upregulated HLAB levels. PRMT1 over-expression rescued lactate mediated increase in MHC I expression. Lactate mediated changes in nucleosomal occupancy on HLAB promoter facilitated a chromatin landscape that favoured decreased recruitment of CREB and PRMT1 on CRE site of HLAB locus. The effect of lactate on the chromatin landscape of HLAB was completely mimicked by PRMT1 inhibitor AMI-1 in terms of nucleosomal occupancy and CREB recruitment. Besides demonstrating the importance of lactate in the transcriptional regulation of HLAB, this study highlights for the first time the (i) existence of HIF-1α-PRMT1 regulatory loop and (ii) role of PRMT1 in modulating chromatin landscape crucial for facilitating HLAB gene expression.
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CAS 20324-87-2 AMI-1

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