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TNKS-IN-1

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-147245

    STP1002

    PARP Cancer
    Basroparib (STP1002) is a selective, orally active inhibitor of tankyrase (TNKS1/TNKS2) with IC50 of 29.94 nM and 3.68 nM for TNKS1 and TNKS2, respectively. Basroparib has an IC50 of >10 μM for PARP1. Basroparib binds to TNKS, stabilizes AXIN1/2 proteins, blocks Wnt/β-catenin signaling pathway, inhibits tumor cell proliferation and induces apoptosis, while reducing cancer stem cell properties. Basroparib can be used in colorectal cancer (CRC) studies with KRAS mutations (such as G12V/G12D) to overcome acquired resistance to MEK inhibitors. STP1002 has synergistic antitumor activity with MEK inhibitors [1] .
    Basroparib
  • HY-13968
    JW 55
    5 Publications Verification

    PARP Cancer
    JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
    JW 55
  • HY-16910
    WIKI4
    4 Publications Verification

    PARP β-catenin Wnt Cancer
    WIKI4 is a potent tankyrase inhibitor with an IC50 of 26 nM for TNKS2. WIKI4 potently inhibits Wnt/β-catenin signaling and that its half-maximal response dose is 75 nM. WIKI4 mediates its effects on Wnt/β-catenin signaling by inhibiting the enzymatic activity of TNKS2 . WIKI4 is cytotoxic to SCLC cells with an IC50 value of 0.02 μM .
    WIKI4
  • HY-145267

    PARP Wnt Cancer
    OM-153 is a potent and orally active tankyrase inhibitor with IC50s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 (TNKS1/2), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM [1] .
    OM-153
  • HY-147886
    PARP1-IN-11
    1 Publications Verification

    PARP Cancer
    PARP1-IN-11 (compound 49) is a potent PARP1 inhibitor with IC50 value of 0.082 µM. PARP1-IN-11 shows complete inhibition of PARP2 and substantially inhibits PARP3, TNKS1 and TNKS2 .
    PARP1-IN-11
  • HY-114943

    PARP Wnt β-catenin Cancer
    TNKS-IN-1 is a selective and potent tankyrase (TNKS1/TNKS2) inhibitor with IC50 values of 7.9 nM and 8.7 nM. TNKS-IN-1 induces axin2 accumulation with an EC50 of 1500 nM. TNKS-IN-1 can antagonize the Wnt signal transduction pathway by stabilizing axin proteins and promoting β-catenin degradation. TNKS-IN-1 can be used for the research of colorectal cancer [1].
    TNKS-IN-1
  • HY-146336

    PARP Apoptosis Wnt β-catenin Cancer
    PARP1/2/TNKS1/2-IN-1 is a potent and selective dual PARP-1/2 and TNKS1/2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM for PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 suppresses Wnt/β-catenin signaling, decreases pADPr and BRCA1 expression, induces DNA damage, promotes apoptosis, and arrests the cell cycle at the G2/M phase. PARP1/2/TNKS1/2-IN-1 can be used for the study of on colorectal cancer and triple-negative breast cancer [1].
    PARP1/2/TNKS1/2-IN-1
  • HY-23338

    PARP Others
    TNKS-2-IN-1 (Compound 13g) is a TNKS-2 inhibitor. TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM [1].
    TNKS-2-IN-1
  • HY-108516

    Wnt PARP Cancer
    TC-E 5001 is an inhibitor of Wnt pathway that inhibits tankyrase 1/2 (TNKS1/2) via novel adenosine pocket binding, with Kds of 79 nM and 28 nM, respectively. TC-E 5001 also inhibits Axin2 and STF, with IC50s of 0.709 μM and 0.215 μM, respectively [1] .
    TC-E 5001
  • HY-180867

    PARP Neurological Disease
    TNKS modulator-1 is a TNKS modulator.
    TNKS modulator-1

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