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Nsd2+Inhibitors

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-161574
    LLC0424

    		PROTACs Histone Methyltransferase Cancer
    LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
    LLC0424
  • HY-114340
    LEM-14

    		Histone Methyltransferase Apoptosis Cancer
    LEM-14 is a potent and selective NSD2 inhibitor with an IC50 of 132 µM. LEM-14 has very weak activitv against NSD1 and has no activity against NSD3. LEM-14 inhibits fibrotic gene expression in ND but not DIO BMDMs. LEM-14 combined with ionizing radiation (IR) enhances the apoptosis rate and reduces the colony-formation ability of CRC cells. LEM-14 exhibits enhanced anti-tumor efficacy in Balb/c nude mice bearing LoVo cell xenografts when combined with ionizing radiation. LEM-14 has the potential for the research of multiple myeloma and colorectal cancer [2] .
    LEM-14
  • HY-168035
    W4275

    		Histone Methyltransferase Cancer
    W4275 (Compound 42) is a selective NSD2 inhibitor with oral activity, showing an IC50 value of 17 nM. W4275 exhibits antiproliferative activity with an IC50 of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .
    W4275
  • HY-172614
    RK-0080552

    RK-552

    		 Histone Methyltransferase Apoptosis Cancer
    RK-0080552 (RK-552) is a NSD2 inhibitor with an IC50 of 0.11 μM, and it exhibits selectivity over histone methyltransferases G9a (IC50: 1.2 μM) and SET7/9 (IC50: >50 μM). RK-0080552 functionally inhibits NSD2 histone methyltransferase activity, reduces the dimethylation level of histone H3 lysine 36, suppresses IRF4 transcription, induces apoptosis and triggers cell death. RK-0080552 inhibits the growth of xenograft tumors and prolongs host survival. RK-0080552 is available for the research of multiple myeloma .
    RK-0080552
  • HY-161796A
    UNC8732 TFA

    		Histone Methyltransferase Molecular Glues Cancer
    UNC8732 (TFA) is a NSD2 inhibitor and degrader .
    UNC8732 TFA
  • HY-161796
    UNC8732

    		Molecular Glues Cancer
    UNC8732, a chemical probe, is an NSD2 inhibitor and degrader.
    UNC8732
  • HY-177499
    NSD2-IN-5

    		Histone Methyltransferase Cancer
    NSD2-IN-5 (Compound 198) is an NSD2 inhibitor with an IC50 value between 0.001 μM and 0.01 μM. NSD2-IN-5 can be used in cancer research .
    NSD2-IN-5
  • HY-182486
    LEM-06

    		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
  • HY-180553
    NSD2-IN-6

    		Histone Methyltransferase Cancer
    NSD2-IN-6 is a selective and orally active NSD2 inhibitor with IC50s of 3.8  and 274 nM for NSD2 and NSD1 respectively. NSD2-IN-6 reduces H3K36me2 levels, reverses cell plasticity by restoring the androgen receptor ( AR) signaling pathway. NSD2-IN-6 reduces a shift from cluster 2 and 3 states towards the cluster 1 state in organoids. NSD2-IN-6 exerts antitumor activity by reversing tumor cell plasticity, suppressing growth, and promoting apoptosis in vivo. NSD2-IN-6 can be used for prostate cancer research .
    NSD2-IN-6

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