A potent, cell-permeable inhibitor of MK2
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.

MK2 Inhibitor III

Item No. 15943

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,5,6,7-tetrahydro-2-[2-(3-quinolinyl)-4-pyridinyl]-4H-pyrrolo[3,2-c]pyridin-4-one, monohydrate
CAS Number
1186648-22-5
Molecular Formula
C21H16N4O • H2O
Formula Weight
358.4
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1.4 mg/mlDMSO: 5 mg/mlDMSO:PBS(pH7.2) (1:1): 0.5 mg/ml
λmax
208, 243, 309 nm
SMILES
O=C(NCC1)C2=C1NC(C3=CC(C4=CC(C=CC=C5)=C5N=C4)=NC=C3)=C2.O
InChi Code
InChI=1S/C21H16N4O.H2O/c26-21-16-11-20(25-18(16)6-8-23-21)14-5-7-22-19(10-14)15-9-13-3-1-2-4-17(13)24-12-15;/h1-5,7,9-12,25H,6,8H2,(H,23,26);1H2
InChi Key
NIKCVKMHGQQSRN-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

    500 µg

    $81

    Add

    1 mg

    $121

    Add

    5 mg

    $248

    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

    MAP kinase-activated protein kinase 2 (MAPKAP2, MK2) is a stress-activated serine/threonine protein kinase that is phosphorylated by p38 MAP kinase and is involved in diverse cellular functions with a central role in inflammation.1,2,3 MK2 inhibitor III is a potent, cell-permeable inhibitor of MK2 (IC50 = 8.5 nM).4 It less potently blocks MK3 and MK5 (IC50s = 210 and 81 nM, respectively) and is weak or inactive against several other kinases, including other p38 MAP kinase targets.4 MK2 inhibitor III prevents LPS-induced synthesis of TNF-α in human monocyte-like U937 cells (IC50 = 4.4 µM).4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huang, X., Shipps, G.W., Jr., Cheng, C.C., et al. Discovery and hit-to-lead optimization of non-ATP competitive MK2 (MAPKAPK2) inhibitors. ACS Med. Chem. Lett. 2(8), 632-637 (2011).

    2. Wang, X., Khaleque, M.A., Zhao, M.J., et al. Phosphorylation of HSF1 by MAPK-activated protein kinase 2 on serine 121, inhibits transcriptional activity and promotes HSP90 binding. The Journal of Biological Chemisty 281(2), 782-791 (2006).

    3. Werz, O., Szellas, D., Steinhilber, D., et al. Arachidonic acid promotes phosphorylation of 5-lipoxygenase at Ser-271 by MAPK-activated protein kinase 2 (MK2). The Journal of Biological Chemisty 277(17), 14793-14800 (2002).

    4. Anderson, D.R., Meyers, M.J., Vernier, W.F., et al. Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). J. Med. Chem. 50(11), 2647-2654 (2007).