EI1 - 96%, high purity , CAS No.1418308-27-6, Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit

Item Number
E125706
Grouped product items
SKUSizeAvailabilityPrice Qty
E125706-5mg
5mg
In stock
$102.90
E125706-10mg
10mg
In stock
$173.90
E125706-25mg
25mg
In stock
$391.90
E125706-50mg
50mg
In stock
$521.90
E125706-100mg
100mg
In stock
$756.90

Potent and selective EZH2 inhibitor

Basic Description

Synonyms6-cyano-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-1-(pentan-3-yl)-1H-indole-4-carboxamide | NCGC00351776-03 | HY-15573 | AS-55788 | CCG-268533 | EI1; Ezh2 inhibitor | 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-
Specifications & PurityMoligand™, ≥96%
Biochemical and Physiological MechanismsEI1 demonstrated potent, concentration-dependent inhibition of the enzymatic activity against both Ezh2 wild-type and Y641F mutant enzymes with IC50 of 15 ± 2 nM and 13 ± 3 nM, respectively. Although SAM is the common cofactor for all HMTs, EI1 showed rem
Storage TempProtected from light,Store at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
NoteToxic, refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.

Associated Targets(Human)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 6-cyano-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-1-pentan-3-ylindole-4-carboxamide
INCHI InChI=1S/C23H26N4O2/c1-5-17(6-2)27-8-7-18-19(10-16(12-24)11-21(18)27)22(28)25-13-20-14(3)9-15(4)26-23(20)29/h7-11,17H,5-6,13H2,1-4H3,(H,25,28)(H,26,29)
InChi Key PFHDWRIVDDIFRP-UHFFFAOYSA-N
Canonical SMILES CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C
Isomeric SMILES CCC(CC)N1C=CC2=C(C=C(C=C21)C#N)C(=O)NCC3=C(C=C(NC3=O)C)C
PubChem CID 72199293
Molecular Weight 390.48

Certificates

Certificate of Analysis(COA)

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5 results found

Lot NumberCertificate TypeDateItem
J2213710Certificate of AnalysisJul 16, 2024 E125706
J2213711Certificate of AnalysisJul 16, 2024 E125706
J2213712Certificate of AnalysisJul 16, 2024 E125706
J2213730Certificate of AnalysisJul 16, 2024 E125706
J2213767Certificate of AnalysisJul 16, 2024 E125706

Chemical and Physical Properties

Solubilityinsoluble in H2O; insoluble in EtOH; ≥19.5 mg/mL in DMSO
Sensitivitylight sensitive

Related Documents

References

1. Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, Zeng J, Li M, Fan H, Lin Y et al..  (2012)  Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation..  Proc Natl Acad Sci USA,  109  (52): (21360-5).  [PMID:23236167]

Solution Calculators