An inhibitor of NSD2
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Gintemetostat

Item No. 46672

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αS,3R)-3-amino-1-[4-[(6-amino-9H-purin-9-yl)methyl]-6-(2,5-difluoro-4-methoxyphenyl)-3-pyridinyl]-α-(difluoromethyl)-3-piperidinemethanol
CAS Number
2604513-16-6
Synonyms
  • KTX-1001
Molecular Formula
C25H26F4N8O2
Formula Weight
546.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)[C@@H](O)[C@@](N)(CCC1)CN1C2=CN=C(C3=C(F)C=C(OC)C(F)=C3)C=C2CN4C5=NC=NC(N)=C5N=C4
InChi Code
InChI=1S/C25H26F4N8O2/c1-39-19-7-15(26)14(6-16(19)27)17-5-13(9-37-12-35-20-23(30)33-11-34-24(20)37)18(8-32-17)36-4-2-3-25(31,10-36)21(38)22(28)29/h5-8,11-12,21-22,38H,2-4,9-10,31H2,1H3,(H2,30,33,34)/t21-,25-/m1/s1
InChi Key
PIFXSVGCYBHXHR-PXDATVDWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $99

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    5 mg

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    10 mg

    $495

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    25 mg

    $990

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    Cayman Chemical
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    Product Description

    Gintemetostat is an inhibitor of the histone-lysine N-methyltransferase NSD2 (IC50 = 0.46 nM).1 It reduces the levels of dimethylated lysine 36 on histone H3 (H3K36me2) in MDA-MB-231 and MDA-MB-468 breast cancer cells and decreases the migration of MDA-MB-231 cells at 10 µM.2 Gintemetostat (50 mg/kg) reduces tumor growth in a mouse model of breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lewis, C.A., Schmidt, C., Beebe, L., et al. Characterization of the activity of KTX-1001, a small molecule inhibitor of multiple myeloma SET domain using surface plasmon resonance. The Journal of Biological Chemisty 301(7), 110382 (2025).

    2. Lin, W., Chen, J., Wu, K., et al. NSD2 drives triple-negative breast cancer progression via ATAD3A-dependent senescence. Cell Signal. 149, 112921 (2026).