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HIPK2 inhibitor

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100464
    tBID
    Maximum Cited Publications
    6 Publications Verification

    DYRK Cancer
    tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 μM.
    tBID
  • HY-128439

    DYRK Cancer
    BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 and does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway. BT173 can be studied in research for kidney diseases such as renal fibrosis .
    BT173
  • HY-U00439A
    Protein kinase inhibitor 1 hydrochloride
    4 Publications Verification

    DYRK Cancer
    Protein kinase inhibitor 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
    Protein kinase inhibitor 1 hydrochloride
  • HY-135906
    CK2/ERK8-IN-1
    2 Publications Verification

    Casein Kinase ERK Pim DYRK Apoptosis Cancer
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy .
    CK2/ERK8-IN-1
  • HY-U00439

    DYRK Cancer
    Protein kinase inhibitor 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
    Protein kinase inhibitor 1
  • HY-179378

    DYRK TGF-beta/Smad NF-κB Wnt β-catenin MDM-2/p53 Notch Inflammation/Immunology
    XRF-1021 is an orally active HIPK2 inhibitor (IC50 = 0.18 μM). XRF-1021 reduces the expression of fibrotic markers in TGF-β1 stimulated NRK-49F and HK-2 cells, including Fibronectin, Collagen I and α-SMA. XRF-1021 blocks TGF-β, NF-κB, p53, Wnt/β-catenin, and Notch signaling. XRF-1021 reduces renal injury and fibrosis in vivo. XRF-1021 can be used for the research of chronic kidney disease .
    XRF-1021
  • HY-100464R

    DYRK Reference Standards Cancer
    tBID (Standard) is the analytical standard of tBID (HY-100464). This product is intended for research and analytical applications. tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 μM.
    tBID (Standard)
  • HY-122670

    Pim Apoptosis AMPK DYRK STAT MDM-2/p53 Cancer
    VS-II-173 is a pan-Pim kinase inhibitor with IC50 values ​​of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
    VS-II-173

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