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Valemetostat (DS-3201) - 98%, high purity , CAS No.1809336-39-7, Inhibitor of enhancer of zeste 1 polycomb repressive complex 2 subunit;Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit

  • Moligand™
  • ≥98%
Item Number
V414273
Grouped product items
SKUSizeAvailabilityPrice Qty
V414273-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$246.90
V414273-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,111.90
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EZH1/2 Inhibitors

View related series
enhancer of zeste 1 polycomb repressive complex 2 subunit Inhibitor enhancer of zeste 2 polycomb repressive complex 2 subunit Inhibitor

Basic Description

SynonymsValemetostat|1809336-39-7|Valemetostat [INN]|EZH1/2 inhibitor DS-3201|60RD0234VE|DS-3201|UNII-60RD0234VE|DS-3201b|DS3201|(2R)-7-chloro-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxami
Specifications & Purity98%
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of enhancer of zeste 1 polycomb repressive complex 2 subunit;Inhibitor of enhancer of zeste 2 polycomb repressive complex 2 subunit
Product Description

Information

Valemetostat (DS-3201) Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.


Targets

EZH1 ; EZH2


In vitro

Valemetostat significantly reducs ATL cell viability compared with the others. Valemetostat significantly reactivates the expression of the highly H3K27me3-accumulated EZH1/2 target genes in an ex vivo culture of primary ATL cells. Valemetostat shows superior anti-growth effects compared with EZH2-selective inhibitor in malignant lymphoma cell lines..


Cell Research(from reference)

Cell lines：23 cell lines derived from hematological malignancies 

Incubation Time：1, 7, 14 days 

Associated Targets

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name (2R)-7-chloro-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
INCHI InChI=1S/C26H34ClN3O4/c1-14-11-15(2)29-25(32)20(14)13-28-24(31)19-12-21(27)23-22(16(19)3)33-26(4,34-23)17-7-9-18(10-8-17)30(5)6/h11-12,17-18H,7-10,13H2,1-6H3,(H,28,31)(H,29,32)/t17?,18?,26-/m1/s1
InChi Key SSDRNUPMYCFXGM-ZZHSESOFSA-N
Canonical SMILES CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)OC(O3)(C)C4CCC(CC4)N(C)C)Cl)C
Isomeric SMILES CC1=CC(=C(C(=O)N1)CNC(=O)C2=CC(=C3C(=C2C)O[C@@](O3)(C)C4CCC(CC4)N(C)C)Cl)C
PubChem CID 126481870
Molecular Weight 488.02

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 100 mg/mL (204.9 mM);    

Related Documents

 SDS

 Specification Sheet

References

1. Kim KH, Roberts CW.  (2016)  Targeting EZH2 in cancer..  Nat Med,  22  (2): (128-34).  [PMID:26845405]
2. Honma D, Kanno O, Watanabe J, Kinoshita J, Hirasawa M, Nosaka E, Shiroishi M, Takizawa T, Yasumatsu I, Horiuchi T et al..  (2017)  Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor..  Cancer Sci,  108  (10): (2069-2078).  [PMID:28741798]
3. Yamagishi M, Hori M, Fujikawa D, Ohsugi T, Honma D, Adachi N, Katano H, Hishima T, Kobayashi S, Nakano K et al..  (2019)  Targeting Excessive EZH1 and EZH2 Activities for Abnormal Histone Methylation and Transcription Network in Malignant Lymphomas..  Cell Rep,  29  (8): (2321-2337.e7).  [PMID:31747604]
4. Dou F, Tian Z, Yang X, Li J, Wang R, Gao J.  (2022)  Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma..  Drug Discov Ther,  129  (3): (589-97).  [PMID:36310058]

Solution Calculators

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