A pan-PDHK 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.

VER-246608

Item No. 19182

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[4-(2-chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxy-benzamide
CAS Number
1684386-71-7
Molecular Formula
C28H23ClF2N4O4
Formula Weight
553.0
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
SMILES
OC1=CC(O)=C(C(N(C2=CC=C(C3=NC(Cl)=NC=C3C)C=C2)CC4=CC=C(CNC(C(F)F)=O)C=C4)=O)C=C1
InChi Code
InChI=1S/C28H23ClF2N4O4/c1-16-13-33-28(29)34-24(16)19-6-8-20(9-7-19)35(27(39)22-11-10-21(36)12-23(22)37)15-18-4-2-17(3-5-18)14-32-26(38)25(30)31/h2-13,25,36-37H,14-15H2,1H3,(H,32,38)
InChi Key
LCGNLQSOSJFLKR-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

    $37

    Add

    5 mg

    $163

    Add

    10 mg

    $252

    Add

    25 mg

    $493

    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

    VER-246608 is a pan-inhibitor of pyruvate dehydrogenase kinase (PDHK; IC50s = 35, 84, 40, and 91 nM for PDHK1, -2, -3, and -4, respectively).1 It is selective for PDHKs over heat shock protein 90 (Hsp90; IC50 = >100 µM), as well as a panel of 97 kinases at 10 µM. VER-246608 (10 and 20 µM) decreases the production of L-lactate, a marker of glycolytic activity, in PC3 cells cultured in D-glucose- and L-glutamine-depleted media. It reduces the growth of, and induces cell cycle arrest at the G1 phase in, serum-starved PC3 cells when used at a concentration of 20 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Moore, J.D., Staniszewska, A., Shaw, T., et al. VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells. Oncotarget 5(24), 12862-12876 (2014).