| Identification | Back Directory | [Name]
A-395 | [CAS]
2089148-72-9 | [Synonyms]
A-395
A-395,Histone Methyltransferase,A395,A 395,Inhibitor,inhibit
3-Pyrrolidinamine, 1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-4-[4-[4-(methylsulfonyl)-1-piperazinyl]phenyl]-, (3R,4S)- | [Molecular Formula]
C26H35FN4O2S | [MOL File]
2089148-72-9.mol | [Molecular Weight]
486.65 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 nMinhibit the PRC2 complex with an IC50 value 34 nM for methylation of H3K27and 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 nMinhibiting the formation of H3K27me3. For characterization details of A-395please visit the A-395 probe summary on the Structural Genomics Consortium (SGC) website.
A-395N is the negative control for the active enantiomerA-395. A-395N is available from Sigma. To learn more about and purchase A-395N | [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 | [storage]
Store at -20°C | [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 |
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1-631-485-4226; 16314854226 |
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ChemeGen
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https://www.chemegen.com |
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