A dual EZH1 and EZH2 inhibitor
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

Valemetostat

Item No. 31674

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R)-7-chloro-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-2-[trans-4-(dimethylamino)cyclohexyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
CAS Number
1809336-39-7
Synonyms
  • DS-3201b
  • (R)-OR-S2
Molecular Formula
C26H34ClN3O4
Formula Weight
488.0
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
216 nm
SMILES
CC1=C2C(O[C@@](O2)([C@]3([H])CC[C@H](CC3)N(C)C)C)=C(C=C1C(NCC4=C(C=C(NC4=O)C)C)=O)Cl
InChi Code
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-UYPAYLBCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    500 µg

    $59

    Add

    1 mg

    $105

    Add

    5 mg

    $292

    Add

    10 mg

    $525

    Add
    Cayman Chemical
    Visit Our Cancer Resource Center
    Find Tools & Resources to Study the Hallmarks of Cancer
    • Cancer cell signaling & regulation
    • Cancer metabolism
    • Tumor microenvironment
    EXPLORE NOW
    Product Description

    Valemetostat is a dual inhibitor of enhancer of zeste homolog 1 (EZH1) and EZH2.1 It inhibits polycomb repressive complex 2 (PRC2) containing EZH1 or EZH2 as the catalytic subunit in cell-free assays (IC50s = 8.4 and 2.5 nM, respectively). Valemetostat inhibits trimethylation of histone H3 lysine 27 in HCT116 cells (IC50 = 0.44 nM). It inhibits the growth of Karpas-422 diffuse large B cell lymphoma (DLBCL) cells (GI50 = 4.8 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Honma, D., Kanno, O., Watanabe, J., et al. Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor. Cancer Sci. 108(10), 2069-2078 (2017).