An NSD3-PWWP1 antagonist
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BI-9321 (hydrochloride)

Item No. 27815

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[5-(7-fluoro-4-quinolinyl)-1-methyl-1H-imidazol-4-yl]-3,5-dimethyl-benzenemethanamine, trihydrochloride
CAS Number
2387510-87-2
Molecular Formula
C22H21FN4 • 3HCl
Formula Weight
469.8
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
FC1=CC2=C(C(C3=C(C4=C(C)C=C(CN)C=C4C)N=CN3C)=CC=N2)C=C1.Cl.Cl.Cl
InChi Code
InChI=1S/C22H21FN4.3ClH/c1-13-8-15(11-24)9-14(2)20(13)21-22(27(3)12-26-21)18-6-7-25-19-10-16(23)4-5-17(18)19;;;/h4-10,12H,11,24H2,1-3H3;3*1H
InChi Key
DCDXMBVQCRHZMW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

    $238

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    Cayman Chemical
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    Product Description

    BI-9321 is an antagonist of the histone-lysine N-methyltransferase NSD3 (IC50 = 0.203 µM in a time-resolved FRET (TR-FRET) assay).1 It selectively binds to the NSD3 PWWP1 domain over 14 other PWWP domains, including NSD2-PWWP1 and NSD3-PWWP2, at 100 µM. BI-9321 is also selective for NSD3 over 20 methyllysine-binding proteins in differential static light scattering (DSLS) assays at 500 µM, 35 DNA or RNA methyltransferases in enzyme activity assays at 10 µM, and 31 kinases in enzyme activity assays at 10 µM. It decreases expression of mRNA encoding Myc in MOLM-13 acute myeloid leukemia (AML) cells when used at a concentration of 10 µM for six hours and reduces the viability of MOLM-13 cells after six days (IC50 = 26.8 µM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Böttcher, J., Dilworth, D., Reiser, U., et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat. Chem. Biol. 15(8), 822-829 (2019).