2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. NSD2/MMSET/WHSC1 Isoform

NSD2/MMSET/WHSC1

 

NSD2/MMSET/WHSC1 Related Products (12):

Cat. No. Product Name Effect Purity
  • HY-161574
    LLC0424
    		Inhibitor 98.41%
    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)).
  • HY-141877
    MS4322
    		Degrader 99.14%
    MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-114340
    LEM-14
    		Inhibitor 98.02%
    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.
  • HY-168035
    W4275
    		Inhibitor 98.93%
    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.
  • HY-171119
    NSD2-PWWP1-IN-1
    		Inhibitor 98.72%
    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.
  • HY-177499
    NSD2-IN-5
    		Inhibitor
    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.
  • HY-179427
    NSD2/H3K36me2 modulator-1
    		Modulator
    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).
  • HY-141877B
    MS4322 (isomer)
    		99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).
  • HY-171120
    NSD2-PWWP1-IN-2
    		Inhibitor 99.64%
    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.
  • HY-171121
    NSD2-PWWP1-IN-3
    		Inhibitor 99.63%
    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.
  • HY-178322
    UNC10415667
    		Degrader
    UNC10415667 is a NSD2 degrader, with a DC50 values of 460 nM. UNC10415667 can be used for the study of cancers driven by NSD2 overexpression or dysregulation, such as multiple myeloma, acute lymphocytic leukemia, and prostate cancer.
  • HY-172614
    RK-0080552
    		Inhibitor
    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.