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A-395

Catalog No. T10205 CAS 2089148-72-9

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).

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A-395, CAS 2089148-72-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 40.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 132.00
25 mg	In stock	$ 218.00
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 95.00

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Purity: 97.82%

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Description	A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).
Targets&IC50	PRC2:18 nM
In vitro	The embryonic ectoderm development (EED) protein is an essential subunit of PRC2. A-395 antagonizes the H3K27me3 binding functions of EED. A-395 binds to EED in the H3K27me3-binding pocket, thereby preventing allosteric activation of the catalytic activity of PRC2. A-395 is capable of competing for H3K27me3 peptide binding to EED (IC50: 7 nM). A-395, but not the close chemical analog A-395N, modulates the activity of PRC2 in cells by potently reducing the H3K27 methyl mark in a highly selective manner. A-395 treatment inhibits both H3K27me2 and H3K27me3 (IC50s: 390 nM and 90 nM). Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.
Cell Research	1,000 multiple myeloma cells are seeded in each well of 96-well cell culture plates and treated with A-395 (0.001-100 μM) or DMSO control for 10 d before the cell proliferation assay. Cell proliferation assays are conducted with the CellTiter-Glo Luminescent Cell Viability Assay.

Molecular Weight	486.65
Formula	C26H35FN4O2S
CAS No.	2089148-72-9

Storage

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

Solubility Information

DMSO: 100 mg/mL (205.49 mM), Sonication is recommended.

References and Literature

1. He Y, et al. The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat Chem Biol. 2017 Apr;13(4):389-395.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library PPI Inhibitor Library Methylation Compound Library Epigenetics Compound Library Bioactive Compound Library Bioactive Compounds Library Max Histone Modification Compound Library Reprogramming Compound Library

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Keywords

A-395 2089148-72-9 Chromatin/Epigenetic Histone Methyltransferase A395 Inhibitor A 395 inhibit inhibitor

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