A-395 Inhibitor

Name: A-395 Inhibitor; MyBioSource
Brand: MyBioSource
SKU: MBS5752647
Availability: InStock
Rating: 5 (10 reviews)

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5752647

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: 18nM). More details

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Product Documentation

Sample Manual Insert View PDF

Testing Data View PDF

Certificate of Analysis (COA) View PDF

QC Report View PDF

Material Safety Data Sheet View PDF

Technical Datasheet View PDF

Protocol View PDF

Product Overview

Online Datasheet in PDF

Product Name

A-395, Inhibitor

Full Product Name

A-395

Product Gene Name

A-395, inhibitor

Form/Format

Solid. Powder

Purity/Purification

98.00%

Preparation and Storage

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

Molecular Weight

486.65

Solubility

DMSO: 100mg/mL (205.49mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)

Formula

C26H35FN4O2S

SMILES

O=S(N1CCN(C2=CC=C([C@H]3CN(C4C(C(F)=CC=C5)=C5CC4)C[C@@H]3N(C)C)C=C2)CC1)(C)=O

CAS Number

2089148-72-9

Target & IC50

Trimeric PRC2 complex: ic50 18nM

Cell Research

1,000 multiple myeloma cells are seeded in each well of 96-well cell culture plates and treated with A-395 (0.001-100uM) or DMSO control for 10 d before the cell proliferation assay. Cell proliferation assays are conducted with the CellTiter-Glo Luminescent Cell Viability Assay.

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: 7nM). 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: 390nM and 90nM). Furthermore, A-395 treatment,results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors.

Product References and Citations for A-395, inhibitor

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.
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.

Other Notes

Small volumes of A-395, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for A-395 purchase

MBS5752647 is an inhibitor targeting A-395.

Additional Details

NCBI/Uniprot data below describe general gene information for A-395. It may not necessarily be applicable to this product.

Protein Family

Zinc finger protein

Precautions

All of MyBioSource's Products are for scientific laboratory research purposes and are not for diagnostic, therapeutics, prophylactic or in vivo use. Through your purchase, you expressly represent and warrant to MyBioSource that you will properly test and use any Products purchased from MyBioSource in accordance with industry standards. MyBioSource and its authorized distributors reserve the right to refuse to process any order where we reasonably believe that the intended use will fall outside of our acceptable guidelines.

Disclaimer

While every efforts were made to ensure the accuracy of the information provided in this datasheet, MyBioSource will not be liable for any omissions or errors contained herein. MyBioSource reserves the right to make changes to this datasheet at any time without prior notice.

It is the responsibility of the customer to report product performance issues to MyBioSource within 30 days of receipt of the product. Please visit our Terms & Conditions page for more information.

Product Note

Select online data sheet information is drawn from bioinformatics databases, occasionally resulting in ambiguous or non-relevant product information. It is the responsibility of the customer to review, verify, and evaluate the information to make sure it matches their requirements before purchasing the kit. Our ELISA Kit assays are dynamic research tools and sometimes they may be updated and improved. If the format of this assay is important to you then please request the current manual or contact our technical support team with a presales inquiry before placing an order. We will confirm the current details of the assay. We cannot guarantee the sample manual posted online is the most current manual, it is intended to serve as an example only. Please refer to the instructions For Use provided with the assay kit for precise details.