An NSD2 inhibitor
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MR837

Item No. 43711

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-cyano-N-cyclopropyl-N-(2-thienylmethyl)-benzamide
CAS Number
1210906-48-1
Molecular Formula
C16H14N2OS
Formula Weight
282.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
N#CC1=CC=C(C(N(CC2=CC=CS2)C3CC3)=O)C=C1
InChi Code
InChI=1S/C16H14N2OS/c17-10-12-3-5-13(6-4-12)16(19)18(14-7-8-14)11-15-2-1-9-20-15/h1-6,9,14H,7-8,11H2
InChi Key
WYAGGMZTARRIDX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $60

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    10 mg

    $114

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    50 mg

    $476

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    100 mg

    $713

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    Product Description

    MR837 is an inhibitor of the histone-lysine N-methyltransferase NSD2 (IC50 = 24.67 µM).1 It binds to the NSD2 PWWP1 domain (Kd = 7 µM), which binds methylated histones, and inhibits the protein-protein interaction between NSD2 and histone H3.3 in U2OS cells (IC50 = 17.3 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, N., Yang, H., Liu, K., et al. Structure-based discovery of a series of NSD2-PWWP1 inhibitors. J. Med. Chem. 65(13), 9459-9477 (2022).

    2. Ferreira de Freitas, R., Liu, Y., Szewczyk, M.M., et al. Discovery of small-molecule antagonists of the PWWP domain of NSD2. J. Med. Chem. 64(3), 1584-1592 (2021).