A-395 ( A395 )

Catalog No. M13262 CAS No. 2089148-72-9

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Product Name

A-395
Note

Research use only, not for human use.
Brief Description

A-395 (A395) is a potent, selective, and cellularly active PRC2 subunit EED inhibitor with Kd of 1.5 nM.
Description

A-395 (A395) is a potent, selective, and cellularly active PRC2 subunit EED inhibitor with Kd of 1.5 nM; potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with IC50 of 18 nM, and inhibits PRC2 at 1 and 50 uM, shows no activity against any of the other protein lysine methyltransferases, arginine methyltransferases, or DNA methyltransferases; inhibits both H3K27me2 and H3K27me3 with IC50 of 390 nM and 90 nM, respectively; exhibits potent antitumor efficacy in vivo.
Synonyms

A395
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

Cancer
Indication

——

CAS Number

2089148-72-9
Formula Weight

442.62
Molecular Formula

C24H34N4O2S
Purity

>98% (HPLC)
Solubility

DMSO : 100 mg/mL 205.49 mM
SMILES

CN(C)C1CN(CC1C2=CC=C(C=C2)N3CCN(CC3)S(=O)(=O)C)C4CCC5=C4C(=CC=C5)F
Chemical Name

(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

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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