An inhibitor of TOPK, Chk1, and MEK1 kinases
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.

HI TOPK 032

Item No. 19815

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide
CAS Number
487020-03-1
Molecular Formula
C20H11N5OS
Formula Weight
369.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 3mg/mL (warmed)
λmax
219, 272, 302, 369, 496 nm
SMILES
O=C(C1=CC=CS1)NC2=CC3=C(C#N)C4=NC5=CC=CC=C5N=C4N3C=C2
InChi Code
InChI=1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26)
InChi Key
BCSBXWKRZUPFHW-UHFFFAOYSA-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

    $38

    Add

    5 mg

    $102

    Add

    10 mg

    $165

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    HI TOPK 032 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK), blocking phosphorylation of the substrate histone H2AX with an IC50 value of ~2 µM and providing complete inhibition at 5 µM.1 It also inhibits checkpoint kinase 1 (Chk1; IC50 = 9.6 µM).2 In addition, HI TOPK 032 inhibits MEK1, achieving 40% inhibition at 5 µM, but it does not alter the activities of ERK1, JNK1, or p38 MAPK at 2 µM.1 HI TOPK 032 decreases the growth of colon cancer and glioma initiating cells in vitro and suppresses tumor growth in vivo.1,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, D.J., Li, Y., Reddy, K., et al. Novel TOPK inhibitor HI-TOPK-032 effectively suppresses colon cancer growth. Cancer Res. 72(12), 3060-3068 (2012).

    2. Li, Y., Kim, D.J., Ma, W., et al. Discovery of novel checkpoint kinase 1 inhibitors by virtual screening based on multiple crystal structures. J. Chem. Inf. Model 51(11), 2904-2914 (2011).

    3. Joel, M., Mughal, A.A., Grieg, Z., et al. Targeting PBK/TOPK decreases growth and survival of glioma initiating cells in vitro and attenuates tumor growth in vivo. Mol. Cancer 14, 121 (2015).