A-395 - 95%, high purity , CAS No.2089148-72-9, Inhibitor of embryonic ectoderm development

Item Number
A607294
Grouped product items
SKUSizeAvailabilityPrice Qty
A607294-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$39.90
A607294-5mg
5mg
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Production requires sourcing of materials. We appreciate your patience and understanding.
$81.90
A607294-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$129.90
A607294-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$259.90

Basic Description

Specifications & PurityMoligand™, ≥95%
Biochemical and Physiological MechanismsIn Vitro: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 al
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of embryonic ectoderm development
Product Description

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).


Associated Targets(Human)

EED Tchem Polycomb protein EED (7 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EED Tchem Polycomb protein EED (645 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KARPAS-422 (454 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EZH2 Tclin EZH2/SUZ12/EED complex (20 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name (3R,4S)-1-(7-fluoro-2,3-dihydro-1H-inden-1-yl)-N,N-dimethyl-4-[4-(4-methylsulfonylpiperazin-1-yl)phenyl]pyrrolidin-3-amine
INCHI InChI=1S/C26H35FN4O2S/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/t22-,24?,25+/m1/s1
InChi Key REVJNSVNICWODC-KIDMSAQOSA-N
Canonical SMILES CN(C)C1CN(CC1C2=CC=C(C=C2)N3CCN(CC3)S(=O)(=O)C)C4CCC5=C4C(=CC=C5)F
Isomeric SMILES CN(C)[C@H]1CN(C[C@@H]1C2=CC=C(C=C2)N3CCN(CC3)S(=O)(=O)C)C4CCC5=C4C(=CC=C5)F
PubChem CID 123132213
Molecular Weight 486.65

Certificates

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8 results found

Lot NumberCertificate TypeDateItem
E2420503Certificate of AnalysisFeb 04, 2024 A607294
E2420506Certificate of AnalysisFeb 04, 2024 A607294
E2420507Certificate of AnalysisFeb 04, 2024 A607294
E2420508Certificate of AnalysisFeb 04, 2024 A607294
E2420511Certificate of AnalysisFeb 04, 2024 A607294
E2420512Certificate of AnalysisFeb 04, 2024 A607294
E2420513Certificate of AnalysisFeb 04, 2024 A607294
E2420515Certificate of AnalysisFeb 04, 2024 A607294

Related Documents

References

1. He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM et al..  (2017)  The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex..  Nat Chem Biol,  13  (4): (389-395).  [PMID:28135237] [10.1021/op500134e]

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