An inhibitor of the NSD2-H3K36me2 nucleosome interaction
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UNC6934

Item No. 28814

Technical Information
Formal Name
N-cyclopropyl-3,4-dihydro-3-oxo-N-[[4-[(4-pyrimidinylamino)carbonyl]phenyl]methyl]-2H-1,4-benzoxazine-7-carboxamide
CAS Number
2561494-77-5
Molecular Formula
C24H21N5O4
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(N1)COC2=C1C=CC(C(N(C3CC3)CC4=CC=C(C(NC5=NC=NC=C5)=O)C=C4)=O)=C2
InChi Code
InChI=1S/C24H21N5O4/c30-22-13-33-20-11-17(5-8-19(20)27-22)24(32)29(18-6-7-18)12-15-1-3-16(4-2-15)23(31)28-21-9-10-25-14-26-21/h1-5,8-11,14,18H,6-7,12-13H2,(H,27,30)(H,25,26,28,31)
InChi Key
KOZGEDUWAQFVAV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    UNC6934 is an inhibitor of the protein-protein interaction between histone-lysine N-methyltransferase NSD2 and dimethylated lysine 36 histone 3 (H3K36me2) nucleosomes (IC50 = 104 nM).1 It binds to NSD2 (Kd = 92 nM). UNC6934 also inhibits the serotonin transporter (SERT) and μ-opioid receptor (Kis = 1.4 and 8 µM, respectively). It induces NSD2 nucleolus accumulation in U2OS cells when used at a concentration of 5 µM. See the Structural Genomics Consortium (SGC) website for more information.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dilworth, D., Hanley, R.P., Ferreira de Freitas, R., et alA chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. Nat. Chem. Biol. 18(1), 56-63 (2022).