BI-9321 trihydrochloride

Names

[ Name ]:
BI-9321 trihydrochloride

Biological Activity

[Description]:

BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[Target]

Kd: 166 nM (NSD3-PWWP1)[1]

[In Vitro]

BI-9321 trihydrochloride is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 trihydrochloride downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells[1].

[References]

[1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₄Cl₃FN₄

[ Molecular Weight ]:
469.81

BI-9321 trihydrochloride

Names

Biological Activity

Chemical & Physical Properties

Related Compounds