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BI-9321 trihydrochloride

Chemical Structure : BI-9321 trihydrochloride

CAS No.: 387510-87-2

BI-9321 trihydrochloride (BI 9321 trihydrochloride)

Catalog No.: PC-72294Not For Human Use, Lab Use Only.

BI-9321 trihydrochloride (BI 9321) is a potent, selective and cellular active inhibitor of the NSD3-PWWP1 domain with SPR Kd of 166 nM.

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Biological Activity

BI-9321 trihydrochloride (BI 9321) is a potent, selective and cellular active inhibitor of the NSD3-PWWP1 domain with SPR Kd of 166 nM.
BI-9321 displays no significant inhibition against a selection of 31 diverse kinases, closest family members NSD2-PWWP1, BRD4 and KDM1B.
BI-9321 targets the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 uM.
BI-9321 downregulated Myc messenger RNA expression and reduces proliferation in MOLM-13 cells, BI-9321 inhibited proliferation of both MOLM-13 (IC50=26.8 uM) and RN2 cells (IC50=13 uM).
BI-9321 enhanced the JQ1-dependent proliferation phenotype in the MOLM-13 cell line.

Physicochemical Properties

M.Wt 469.81
Formula C22H24Cl3FN4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

100 mM in DMSO (46.9 mg/mL)

Chemical Name/SMILES

(4-(5-(7-Fluoroquinolin-4-yl)-1-methyl-1H-imidazol-4-yl)-3,5-dimethylphenyl)methanamine trihydrochloride

References

1. Böttcher J, et al. Nat Chem Biol. 2019 Aug;15(8):822-829.

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