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BI-9321

BI-9321, a chemical probe, 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].

Product Specifications

CAS Number

[2387510-86-1]

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-9321.html

Solubility

10 mM in DMSO

Smiles

NCC1=CC(C)=C(C2=C(C3=CC=NC4=CC(F)=CC=C34)N(C)C=N2)C(C)=C1

Molecular Formula

C22H21FN4

Molecular Weight

360.43

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Curated Selection

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