pwwp1

NSD2-PWWP1-IN-3 (compound 36) is an effective inhibitor of NSD2-PWWP1, with an IC50 value of 8.05 µM. It has potential applications in cancer research.

NSD2-PWWP1-IN-2 (compound 33) is a potent NSD2-PWWP1 inhibitor, exhibiting an IC50 value of 1.49 µM, indicating its potential utility in cancer research.

NSD2-PWWP1-IN-1 (compound 31) is a potent inhibitor of NSD2-PWWP1 with an IC50 value of 0.64 µM, demonstrating potential applications in cancer research.

BI-9321 trihydrochloride (BI9321 trihydrochloride) is a selective and potent NSD3-PWWP1 antagonist that downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells.

LEM-14 is a potent NSD2-specific inhibitor (IC50:132 μM).LEM-14 may be used in the study of multiple myeloma.

BI-9321 is a selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist (Kd: 166 nM). BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2.

NSD2-IN-1 (compound 38) is a potent and highly selective inhibitor of NSD2-PWWP1 (nuclear receptor-binding SET domain 2-PWWP1), with an IC50 value of 0.11 μM. By binding to NSD2-PWWP1, NSD2-IN-1 influences gene expression regulated by NSD2, resulting in apoptosis and cell cycle arrest [1].

MS9715 is a potent and selective NSD3-targeting PROTAC, designed by leveraging BI-9321, which targets the PWWP1 domain of NSD3, in conjunction with an E3 ligase VHL ligand. This compound holds potential for research in NSD3-dependent cancer treatments [1].

UNC7096 is a potent, selective degrader of NSD2-PWWP1, exhibiting a dissociation constant (Kd) of 46 nM, and shows promise for treating NSD2-related diseases [1].

UNC6934 Negative Control (Axon 3591) is a chemically related compound that serves as a negative control for UNC6934, a potent and selective chemical probe that specifically targets the N-terminal PWWP (PWWP1) domain of NSD2.

MR837 (NSD2-PWWP1 antagonist 3f) is a NSD2-PWWP1 antagonist.

UNC6934 is a chemical probe targeting the N-terminal PWWP (PWWP1) domain of NSD2.