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Results for "

ENL YEATS domain

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-162350
    TDI-11055

    		Epigenetic Reader Domain Apoptosis Cancer
    TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia .
    TDI-11055
  • HY-145409
    SR-0813

    		Epigenetic Reader Domain Cancer
    SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia .
    SR-0813
  • HY-152469
    Eleven-Nineteen-Leukemia Protein IN-1

    		Epigenetic Reader Domain Cancer
    Eleven-Nineteen-Leukemia Protein IN-1 is an inhibitor of ENL YEATS domain with an IC50 value of 14.5 nM. Eleven-Nineteen-Leukemia Protein IN-1 interacts with ENL protein and enhances the thermal stability of ENL protein in vitro .
    Eleven-Nineteen-Leukemia Protein IN-1
  • HY-152471
    Eleven-Nineteen-Leukemia Protein IN-3

    		Epigenetic Reader Domain Cancer
    Eleven-Nineteen-Leukemia Protein IN-3 is an orally active inhibitor of ENL YEATS domain with an IC50 value of 15.4 nM. Eleven-Nineteen-Leukemia Protein IN-3 down-regulates MYC expression through ENL in cells and can enhances the thermal stability of ENL protein in vitro .
    Eleven-Nineteen-Leukemia Protein IN-3
  • HY-183555
    MS108

    		PROTACs Epigenetic Reader Domain Cancer
    MS108 is a selective VHL-based eleven-nineteen leukemia protein (ENL) PROTAC degrader with DC50 of 0.6 nM. MS108 recruits VHL E3 ligase to induce ENL degradation in a VHL- and ubiquitin-proteasome system (UPS)-dependent manner. MS108 degrades the ENL paralog AF9, which shares a highly conserved YEATS domain with ENL. MS108 suppresses proliferation of cancer cells .
    MS108
  • HY-183825
    Eleven-Nineteen-Leukemia Protein IN-4

    		Epigenetic Reader Domain c-Myc Cancer
    Eleven-Nineteen-Leukemia Protein IN-4 is a ENL YEATS domain inhibitor with an IC50 of 62.0 nM and a Kd of 100.4 nM. Eleven-Nineteen-Leukemia Protein IN-4 downregulates MYC expression and inhibits cancer cell growth; it exerts a synergistic effect with the bromodomain inhibitor JQ-1 (HY-13030). Eleven-Nineteen-Leukemia Protein IN-4 can be used in the research of acute myeloid leukemia .
    Eleven-Nineteen-Leukemia Protein IN-4
  • HY-129224
    XS018661

    		Epigenetic Reader Domain Cancer
    XS018661 is a dual inhibitor of the YEATS domains of ENL and its paralog AF9 with IC50 values of 1.6 and 3 μM as well as Kd values of 754 nM and 523 nM, respectively .
    XS018661

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