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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%

CAS#: 1809336-39-7
Formula: C₂₆H₃₄ClN₃O₄
Molecular Weight: 488.02
PubChem CID: 126481870

Item Number

V414273

Grouped product items
SKU	Size	Availability	Price	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

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

Synonyms	SCHEMBL18393626 \| (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide \| SCHEMBL18639210 \| HY-109108 \| NSC813381 \| NSC-813381 \| Valemetostat \| 60RD0234VE \| M
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	Valemetostat (DS-3201, DS-3201b) is a selective EZH1/2 dual inhibitor.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor 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(Human)

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 (0 Activities)

Discover Target: EZH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (0 Activities)

Discover Target: EZH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EZH2 Tclin Histone-lysine N-methyltransferase EZH2 (2012 Activities)

Discover Target: EZH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EZH1 Tchem Histone-lysine N-methyltransferase EZH1 (112 Activities)

Discover Target: EZH1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

KARPAS-422 (454 Activities)

Discover Target:

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

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

PubChem CID

126481870

CAS Registry No.

1809336-39-7

ChEMBL Ligand

CHEMBL4597193

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]

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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

Basic Description

Associated Targets(Human)

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

Related Documents

References

Solution Calculators

Molarity Calculator

Dilution Calculator

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