An inhibitor of JMJD2D
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KDM4D-IN-1

Item No. 37431

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4,5-dihydro-2-methyl-5-oxo-pyrazolo[1,5-a]pyrido[3,2-e]pyrimidine-3-carbonitrile
CAS Number
2098902-68-0
Synonyms
  • KDM4D Inhibitor 1
Molecular Formula
C11H7N5O
Formula Weight
225.2
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 0.2 mg/mlDMSO: 0.2 mg/ml
λmax
222, 259 nm
SMILES
N#CC(C(C)=NN1C2=NC=CC=C23)=C1NC3=O
InChi Code
InChI=1S/C11H7N5O/c1-6-8(5-12)10-14-11(17)7-3-2-4-13-9(7)16(10)15-6/h2-4H,1H3,(H,14,17)
InChi Key
FIRSAIIBSBCBTF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $72

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    5 mg

    $215

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    10 mg

    $358

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    25 mg

    $715

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    Cayman Chemical
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    Product Description

    KDM4D-IN-1 is an inhibitor of the histone demethylase jumonji domain-containing 2D (JMJD2D; IC50 = 0.41 µM).1 It is selective for JMJD2D over JMJD1B, JMJD2B, and jumonji AT rich interactive domain-containing protein 1A (JARID1A; IC50s = >10 µM for all). KDM4D-IN-1 (0.5 µM) decreases the colony formation, migration, and invasion of Caki-1 clear cell renal carcinoma cells and 786-O adenocarcinoma cells.2 It reduces tumor growth and vessel development in a 786-O mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fang, Z., Wang, T.-q., Li, H., et al. Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of histone lysine demethylase 4D (KDM4D) inhibitors. Bioorg. Med. Chem. Lett. 27(14), 3201-3204 (2017).

    2. Yan, H., Zhu, L., Zhang, J., et al. Histone demethylase KDM4D inhibition suppresses renal cancer progression and angiogenesis through JAG1 signaling. Cell Death Discov. 7(1), 284 (2021).