PROTAC NSD3 degrader-1 

PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.

971.28

C₅₆H₇₁FN₈O₄S

CC1=C(C(C)=CC(CNCCCCCCCCCCC(N[C@H](C(N2[C@@H](C[C@H](C2)O)C(N[C@H](C3=CC=C(C=C3)C4=C(N=CS4)C)C)=O)=O)C(C)(C)C)=O)=C1)C5=C(N(C=N5)C)C6=CC=NC7=C6C=CC(F)=C7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ma Z, Bolinger AA, Chen H, Zhou J. Drug Discovery Targeting Nuclear Receptor Binding SET Domain Protein 2 (NSD2). J Med Chem. 2023 Aug 24;66(16):10991-11026.  [Content Brief]