BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K d 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 IC 50 of 1.2 μM in U2OS cells
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:Kd: 166 nM (NSD3-PWWP1)
规格
别名
BI-9321 三盐酸盐
规格或纯度
≥98%
英文名称
BI-9321 trihydrochloride
生化机理
BI-9321 三盐酸盐是一种强效、选择性和细胞活性的核受体结合 SET 结构域 3 (NSD3)-PWWP1 结构域拮抗剂,其 K d 值为 166 nM。BI-9321 三盐酸盐对 NSD2-PWWP1 和 NSD3-PWWP2 无活性。BI-9321 三盐酸盐