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Nsd2 Inhibitors

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. 상품명 Target 연구분야 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-100034
    NSC 663284
    Maximum Cited Publications
    6 Publications Verification

    DA-3003-1

    		 Phosphatase Histone Methyltransferase Cancer
    NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
    NSC 663284
  • HY-15647
    BRD9539
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
    BRD9539
  • HY-138993A
    NNMT-IN-6 hydrochloride

    		Amine N-methyltransferase Cancer
    NNMT-IN-6 hydrochloride is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 hydrochloride inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 hydrochloride can be used for the research of oral cancer .
    NNMT-IN-6 hydrochloride
  • HY-147914
    NSD2-IN-1

    		Apoptosis Cancer
    NSD2-IN-1 (compound 38) is a potent and high selective NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC50 of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest .
    NSD2-IN-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-138283
    MR837
    1 Publications Verification

    		 Histone Methyltransferase Cancer
    MR837 is an inhibitor of NSD2-PWWP1. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain) .
    MR837
  • HY-151101
    MS159
    1 Publications Verification

    		 PROTACs Cancer
    MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease .
    MS159
  • 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 .
    LEM-14
  • HY-138993
    NNMT-IN-6

    		Amine N-methyltransferase Cancer
    NNMT-IN-6 is a selective nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 of 1.41 μM and a Kd of 5.55 μM. NNMT-IN-6 hydrochloride exhibits selectivity over PRMT1 and NSD2. NNMT-IN-6 inhibits cancer cell proliferation and reduces cellular N-methylnicotinamide (MNA) production. NNMT-IN-6 can be used for the research of oral cancer .
    NNMT-IN-6
  • HY-162308
    NSD-IN-3

    		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-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-125244
    LEM-14-1189

    		Histone Methyltransferase Cancer
    LEM-14-1189, a LEM-14 (HY-114340) derivative, is a NSDs inhibitor with IC50s of 418 μM (NSD1), 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research .
    LEM-14-1189
  • HY-171120
    NSD2-PWWP1-IN-2

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 1.49 µM. NSD2-PWWP1-IN-2 has the potential for the research of cancer .
    NSD2-PWWP1-IN-2
  • HY-171119
    NSD2-PWWP1-IN-1

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-1 (compound 31) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 0.64 µM. NSD2-PWWP1-IN-1 has the potential for the research of cancer .
    NSD2-PWWP1-IN-1
  • 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-161796A
    UNC8732 TFA

    		Histone Methyltransferase Molecular Glues Cancer
    UNC8732 (TFA) is a NSD2 inhibitor and degrader .
    UNC8732 TFA
  • HY-155818
    NSD2-IN-4

    		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-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-161796
    UNC8732

    		Molecular Glues Cancer
    UNC8732, a chemical probe, is an NSD2 inhibitor and degrader.
    UNC8732
  • HY-175871
    (Rac)-NSD2-PWWP1-IN-4

    		Histone Methyltransferase Cancer
    (Rac)-NSD2-PWWP1-IN-4 (compound 7) is an effective NSD2-PWWP1 inhibitor IC50 and Kd values are 0.21 and 0.15 μM. (Rac)-NSD2-PWWP1-IN-4 can be used in tumor research .
    (Rac)-NSD2-PWWP1-IN-4
  • HY-124699
    MMSET-IN-1

    		Histone Methyltransferase Cancer
    MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC50s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a Kd of 1.6 μM for MMSET .
    MMSET-IN-1
  • HY-161670
    NSD2-PWWP1 ligand 1

    		Histone Methyltransferase Cancer
    NSD2-PWWP1 ligand 1 (compound 34) is a small molecule ligand targeting the NSD2-PWWP1 domain (pIC50: 8.2). NSD2 is a large multidomain protein with histone writer and histone reader functions. Dysregulation of the levels of histone methyltransferase nuclear receptor binding SET domain 2 (NSD2) may lead to a variety of hematological and solid malignancies. NSD2-PWWP1 ligand 1 binds to NSD2, reducing its enzymatic activity and inhibiting tumorigenesis .
    NSD2-PWWP1 ligand 1
  • HY-171121
    NSD2-PWWP1-IN-3

    		Histone Methyltransferase Cancer
    NSD2-PWWP1-IN-3 (compound 36) is a potent NSD2-PWWP1 inhibitor with an IC50 value of 8.05 µM. NSD2-PWWP1-IN-3 has the potential for the research of cancer .
    NSD2-PWWP1-IN-3
  • 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-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-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-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-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
  • HY-177400
    NSD-IN-5

    		Histone Methyltransferase Cancer
    NSD-IN-5 (Example 47) is a nuclear receptor-binding SET domain (NSD) inhibitor with IC5050 values ​​of 6 and < 1 nM for NSD1 and NSD2, respectively. NSD-IN-5 also exhibits inhibitory activity against Avg KMS11 cells with an IC5050 of 6 nM. NSD-IN-5 may be used in research on multiple myeloma .
    NSD-IN-5
  • HY-100034R
    NSC 663284 (Standard)

    DA-3003-1 (Standard)

    		 Phosphatase Reference Standards Histone Methyltransferase Cancer
    NSC 663284 (Standard) is the analytical standard of NSC 663284 (HY-100034). This product is intended for research and analytical applications. NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM) .
    NSC 663284 (Standard)

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