An EED protein-protein interaction inhibitor
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A-395 (hydrochloride)

Item No. 20257

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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, hydrochloride
Molecular Formula
C26H35FN4O2S • XHCl
Formula Weight
486.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Water: soluble
λmax
254 nm
SMILES
CS(N1CCN(C2=CC=C([C@H]3CN(C4CCC5=C4C(F)=CC=C5)C[C@@H]3N(C)C)C=C2)CC1)(=O)=O.Cl
InChi Code
InChI=1S/C26H35FN4O2S.ClH/c1-28(2)25-18-30(24-12-9-20-5-4-6-23(27)26(20)24)17-22(25)19-7-10-21(11-8-19)29-13-15-31(16-14-29)34(3,32)33;/h4-8,10-11,22,24-25H,9,12-18H2,1-3H3;1H/t22-,24?,25+;/m1./s1
InChi Key
JUZXQLNCGDDSMJ-NNEMXYTISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $186

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    10 mg

    $351

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    Product Description

    A-395 is an inhibitor of the interaction between embryonic ectoderm development (EED) and histone H3 lysine 27 (H3K27) that binds to the EED subunit of polycomb repressor complex 2 (PRC2) and inhibits H3K27 methylation (Ki = 0.4 nM).1 It inhibits H3K27 di- and trimethylation in RD rhabdoid tumor cells (IC50s = 390 and 90 nM, respectively). In vivo, A-395 (200 mg/kg) reduces tumor volume and intratumor H3K27 trimethylation in a Pfeiffer diffuse large B cell lymphoma (DLBCL) mouse xenograft model. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hey, Y., Selvaraju, S., Curtin, M.L., et al. The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex. Nat. Chem. Biol. 13(4), 389-395 (2017).