2387510-87-2

2387510-87-2 structure

Name: BI-9321 trihydrochloride
Chemical Name: BI-9321 trihydrochloride
CAS Number: 2387510-87-2
Molecular Formula: C₂₂H₂₄Cl₃FN₄
Molecular Weight: 469.81
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2020-04-07 23:35:58
Modify Date: 2024-01-09 12:27:56
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].

Name	BI-9321 trihydrochloride

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.

Molecular Formula	C₂₂H₂₄Cl₃FN₄
Molecular Weight	469.81