A SETD2 inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

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.

EZM0414

Item No. 43914

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1R,3S)-3-(4-acetyl-1-piperazinyl)cyclohexyl]-4-fluoro-7-methyl-1H-indole-2-carboxamide
CAS Number
2411748-50-8
Molecular Formula
C22H29FN4O2
Formula Weight
400.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
FC1=C2C(NC(C(N[C@@H]3CCC[C@@H](C3)N4CCN(CC4)C(C)=O)=O)=C2)=C(C=C1)C
InChi Code
InChI=1S/C22H29FN4O2/c1-14-6-7-19(23)18-13-20(25-21(14)18)22(29)24-16-4-3-5-17(12-16)27-10-8-26(9-11-27)15(2)28/h6-7,13,16-17,25H,3-5,8-12H2,1-2H3,(H,24,29)/t16-,17+/m1/s1
InChi Key
PGNLXEBQMQHFNK-SJORKVTESA-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

    1 mg

    $219

    Add

    5 mg

    $657

    Add

    10 mg

    $1,095

    Add

    25 mg

    $1,916

    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

    EZM0414 is an inhibitor of SET domain-containing protein 2 (SETD2; IC50 = 18 nM).1 It inhibits the proliferation of A549 non-small cell lung cancer (NSCLC) cells (EC50 = 57 nM). EZM0414 (15 and 30 mg/kg) decreases tumor volume in a KMS-11 multiple myeloma mouse xenograft model. It decreases cardiomyocyte levels of trimethylated lysine 36 on histone H3 (H3K36Me3) in a mouse model of heart failure with preserved ejection fraction (HFpEF) induced by a high-fat diet and L-NAME (Item No. 80210).2 EZM0414 also reduces lung congestion and cardiac hypertrophy in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alford, J.S., Lampe, J.W., Brach, D., et al. Conformational-design-driven discovery of EZM0414: A selective, potent SETD2 inhibitor for clinical studies. ACS Med. Chem. Lett. 13(7), 1137-1143 (2022).

    2. Costantino, S., Mohammed, S.A., Ambrosini, S., et al. Chromatin rewiring by SETD2 drives lipotoxic injury in cardiometabolic HFpEF. Circ. Res. 136(10), 1079-1095 (2025).