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AMI-1

Catalog No. T2352 CAS 20324-87-2

AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).

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AMI-1, CAS 20324-87-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 128.00
50 mg	In stock	$ 189.00
100 mg	In stock	$ 297.00
500 mg	In stock	$ 718.00
1 mL * 10 mM (in DMSO)	In stock	$ 52.00

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Purity: 99.9%

Purity: 98%

Purity: 97.53%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AMI-1 is an effective and selective Histone Methyltransferase (HMT) inhibitor (IC50: 3.0/8.8 μM, for yeast Hmt1p, and human PRMT1).
Targets&IC50	Hmt1p (yeast):3.0 μM, PRMT1 (human):8.8 μM
In vitro	In HeLa cells, AMI-1 inhibits methylation levels of GFP-Npl3 fusion and endogenous PRMT1-like activity. AMI-1 also inhibits nuclear receptor-mediated transactivation of a luciferase reporter in MCF7 cells. [1] In addition, AMI-1 inhibits HIV-1 RT polymerase activity with IC50 of 5 μM and inhibits DNA binding to HIV-1 RT with Kd of 2 μM. [2] In INS-1 cells, AMI-1 improves INS-1 cell function and mediates translocations of FOXO1 and PDX-1 intracellularly by regulating FOXO1 phosphorylation and methylation. [4]
In vivo	In chronic AIPI rats, AMI-1 (5 μg/rat) ameliorates COX2 expression and asthmatic indexes, and decreases the airway and alveoli lesions, mucus secretion, and collagen deposition in lungs. [3]
Kinase Assay	INS-1 832/13 cells are suspended in RPMI medium containing 11 mM glucose and the supplements described above. These cells are seeded at a density of 2×104?cells/well in a 96-well black plate coated with poly-D-lysine, and 1% BSA and 0.1% DMSO alone (control), palmitic acid (62.5, 125, 250, 500, and 1000 μM), oleic acid (62.5, 125, 250, 500, and 1000 μM), or TAK-875 (6.25, 12.5, 25, 50, and 100 μM) is added to the plate with 1% BSA and 0.1% DMSO, followed by culture for 72 h. After the culture, caspase 3/7 activity is measured with the Apo-one homogeneous caspase 3/7 assay according to the manufacturer's instructions. Fluorescence intensity is measured at an excitation of 485 nm and an emission at 535 nm.

Molecular Weight	548.45
Formula	C21H14N2Na2O9S2
CAS No.	20324-87-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: 10 mg/mL (18.23 mM)

DMSO: 93 mg/mL (159.1 mM)

References and Literature

1. Cheng D, et al. J Biol Chem. 2004, 279(23), 23892-23899. 2. Skillman AG, et al. Bioorg Chem. 2002, 30(6), 443-458. 3. Sun Q, et al. J Immunol. 2015, 195(1), 298-306. 4. Lv L, et al. Endocrine. 2015,49(3), 669-682.

Citations

1. Li X, Wang Y, Zhang Y, et al. Overexpression of MCAM induced by SMYD2-H3K36me2 in breast cancer stem cell properties. Breast Cancer. 2022: 1-15 2. Feng G, Chen C, Luo Y.PRMT1 accelerates cell proliferation, migration, and tumor growth by upregulating ZEB1/H4R3me2as in thyroid carcinoma.Oncology Reports.2023, 50(6): 1-11.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library Target-Focused Phenotypic Screening Library Stem Cell Differentiation Compound Library Anti-Aging Compound Library Chromatin Modification Compound Library Bioactive Compounds Library Max Methylation Compound Library Reprogramming Compound Library Covalent Inhibitor Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AMI-1 20324-87-2 Chromatin/Epigenetic Histone Methyltransferase protein arginine N-methyltransferases Hmt1p Inhibitor inhibit AMI1 AMI 1 PRMT1 yeast-Hmt1p PRMTs inhibitor

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