2387510-86-1

2387510-86-1 structure

Name: BI-9321
Chemical Name: BI-9321
CAS Number: 2387510-86-1
Molecular Formula: C₂₂H₂₁FN₄
Molecular Weight: 360.43
Catalog: Signaling Pathways Epigenetics Histone Methyltransferase
Create Date: 2020-04-25 15:21:50
Modify Date: 2024-01-05 20:14:55
BI-9321 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 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC50 of 1.2 μM in U2OS cells[1].

Name	BI-9321

Description	BI-9321 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 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 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 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 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	C₂₂H₂₁FN₄
Molecular Weight	360.43