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NSD2-SET

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-154812

    KTX-1001

    Histone Methyltransferase CD44 Cancer
    Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM .Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents [2] .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma [2] .
    Gintemetostat
  • HY-162308

    Histone Methyltransferase Apoptosis Cancer
    NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC50 values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .
    NSD-IN-3
  • HY-155818

    Histone Methyltransferase Cancer
    NSD2-IN-4 is a potent and selective NSD2-SET inhibitor. NSD2-IN-4 has the potential for NSD2-related diseases .
    NSD2-IN-4
  • HY-182486

    Histone Methyltransferase Cancer
    LEM-06 is an NSD2 inhibitor with a human IC50 of 890 μM and 0.8 mM. LEM-06 binds to the histone-tail binding groove of NSD2-SET, inhibiting NSD2-mediated H3K36 histone methyltransferase activity and H3K36 mono-methylation. LEM-06 serves as a hit molecule for further optimization or derivation to explore NSD2 biology. LEM-06 can be used for the research of multiple myeloma .
    LEM-06

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