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

NSD2/MMSET/WHSC1 Inhibitor

NSD2/MMSET/WHSC1 Inhibitors (2):

Cat. No. Product Name Effect Purity
  • HY-161574
    LLC0424
    		Inhibitor 98.42%
    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-168035
    W4275
    		Inhibitor
    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.