A-395
- Product Name
- A-395
- CAS No.
- 2089148-72-9
- Chemical Name
- A-395
- Synonyms
- A-395;A-395, 10 mM in DMSO;A-395,Histone Methyltransferase,A395,A 395,Inhibitor,inhibit;(3R,4S)-1-(7-Fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-4-(4-(4-(methylsulfonyl)piperazin-1-yl)phenyl)pyrrolidin-3-amine;3-Pyrrolidinamine, 1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-4-[4-[4-(methylsulfonyl)-1-piperazinyl]phenyl]-, (3R,4S)-
- CBNumber
- CB04667470
- Molecular Formula
- C26H35FN4O2S
- Formula Weight
- 486.65
- MOL File
- 2089148-72-9.mol
A-395 Property
- Boiling point:
- 612.2±65.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (205.49 mM)
- form
- Solid
- pka
- 8.49±0.40(Predicted)
- color
- White to yellow
- Water Solubility
- H2O: 10mg/mL, clear
- InChIKey
- REVJNSVNICWODC-KIDMSAQOSA-N
- SMILES
- FC1=CC=CC2=C1C(N3C[C@H](C(C=C4)=CC=C4N5CCN(S(C)(=O)=O)CC5)[C@@H](N(C)C)C3)CC2
Safety
- WGK Germany
- WGK 3
- Storage Class
- 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects - Hazard Classifications
- Acute Tox. 3 Oral
Eye Irrit. 2
Skin Irrit. 2
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0021615
- Product name
- A-395
- Purity
- 99.31%
- Packaging
- 5mg
- Price
- $110
- Updated
- 2021/12/16
- Product number
- CS-0021615
- Product name
- A-395
- Purity
- 99.31%
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0021615
- Product name
- A-395
- Purity
- 99.31%
- Packaging
- 25mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- DC10129
- Product name
- A395
- Purity
- >98%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
- Product number
- DC10129
- Product name
- A395
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1750
- Updated
- 2021/12/16
A-395 Chemical Properties,Usage,Production
Uses
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM[1].
Biological Activity
A-395 is a potent and selective chemical probe for the polycomb protein EED (embryonic ectoderm development), an essential component of Polycomb repressive complex 2 (PRC2), involved in transcriptional repression through methylation of histone H3K27. A-395 has been found to bind to EED in vitro with a Ki value of 0.4 nM, inhibit the PRC2 complex with an IC50 value 34 nM for methylation of H3K27, and have >100-fold selectivity over other histone methyltransferases and non-epigenetic targets. In RD rhabdoid tumor cell line A-395 inhibited the PRC2 complex with an IC50 value of 90 nM, inhibiting the formation of H3K27me3. For characterization details of A-395, please visit the A-395 probe summary on the Structural Genomics Consortium (SGC) website.
A-395N is the negative control for the active enantiomer, A-395. A-395N is available from Sigma. To learn more about and purchase A-395N, click here.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
in vivo
The embryonic ectoderm development (EED) protein is an essential subunit of Polycomb repressive complex 2 (PRC2). A-395 antagonizes of 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, with an IC50 of 7 nM. A-395, but not the close chemical analog A-395N, modulates 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, with IC50 values of 390 nM and 90 nM, respectively. Furthermore, A-395 treatment results in growth inhibition of human tumor cell lines sensitive to SAM-competitive EZH2 inhibitors[1].
IC 50
EZH2
References
[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. DOI:10.1038/nchembio.2306
A-395 Preparation Products And Raw materials
Raw materials
Preparation Products
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