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H3K36me2

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

    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 .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .
    Gintemetostat
  • HY-145103
    UNC6934

    		Histone Methyltransferase Cancer
    UNC6934 is a selective NSD2-PWWP1 antagonist with IC50 values of 78 nM and 104 nM, and a Ka of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma.
    UNC6934
  • HY-157251
    UNC8153 TFA

    		Histone Methyltransferase Cancer
    UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
    UNC8153 TFA
  • HY-179427
    NSD2/H3K36me2 modulator-1

    		Histone Methyltransferase Apoptosis Reactive Oxygen Species (ROS) Cancer
    NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC) .
    NSD2/H3K36me2 modulator-1
  • 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-157251A
    UNC8153

    		Histone Methyltransferase Cancer
    UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
    UNC8153
  • HY-155817
    UNC7096

    		Histone Methyltransferase Others
    UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions .
    UNC7096
  • 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
  • HY-179651
    NSD2-PWWP1-IN-6

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-6 (Compound 16) is an effective NSD2-PWWP1 inhibitor with a Kd value of 30 nM. NSD2-PWWP1-IN-6 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-6 can be used for cancer research .
    NSD2-PWWP1-IN-6
  • HY-179650
    NSD2-PWWP1-IN-5

    		Histone Methyltransferase Apoptosis Cancer
    NSD2-PWWP1-IN-5 (Compound 13) is an effective NSD2-PWWP1 inhibitor with a Kd value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma .
    NSD2-PWWP1-IN-5
  • HY-161576
    Thalidomide-Pip-N-boc

    		E3 Ligase Ligand-Linker Conjugates Cancer
    Thalidomide-Pip-N-boc is a conjugate of E3 ligase ligand and linker. Thalidomide-Pip-N-boc is utilized for synthesis of PROTAC Degrader LLC0424 (HY-161574) .
    Thalidomide-Pip-N-boc
  • HY-185557
    LLC0424N

    		Histone Methyltransferase Cancer
    LLC0424N is a negative control compound designed by methylating the thalidomide moiety of LLC0424 (HY-161574). LLC0424N shows does not induce NSD2 degradation and inhibit growth of acute lymphoblastic leukemia cells with NSD2 mutation. LLC0424N can be used for the research of acute lymphoblastic leukemia .
    LLC0424N

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