BI-9321

Modify Date: 2024-01-05 20:14:55

BI-9321 Structure
BI-9321 structure
Common Name BI-9321
CAS Number 2387510-86-1 Molecular Weight 360.43
Density N/A Boiling Point N/A
Molecular Formula C22H21FN4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BI-9321


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].

 Names

Name BI-9321

 BI-9321 Biological Activity

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
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.

 Chemical & Physical Properties

Molecular Formula C22H21FN4
Molecular Weight 360.43
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