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Chemical Structure : A-395
CAS No.: 2089148-72-9
Catalog No.: PC-62309Not For Human Use, Lab Use Only.
A-395 (A395) is a potent, selective, and cellularly active PRC2 subunit EED inhibitor with Kd of 1.5 nM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $588 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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A-395 (A395) is a potent, selective, and cellularly active PRC2 subunit EED inhibitor with Kd of 1.5 nM.
A-395 potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with IC50 of 18 nM, and inhibits PRC2 at 1 and 50 uM.
A-395 shows no activity against any of the other protein lysine methyltransferases, arginine methyltransferases, or DNA methyltransferases.
A-395inhibits both H3K27me2 and H3K27me3 with IC50 of 390 nM and 90 nM, respectively; exhibits potent antitumor efficacy in vivo.
| M.Wt | 486.650 | |
| Formula | C26H35FN4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
200 mM in DMSO (97.3 mg/mL) |
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| Chemical Name/SMILES |
(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 |
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1. He Y, et al. Nat Chem Biol. 2017 Apr;13(4):389-395.
2. Cancer Discov. 2017 Apr;7(4):OF8. doi: 10.1158/2159-8290.CD-RW2017-030.
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