A KDM2A and KDM7A inhibitor
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KDM2A/7A-IN-1

Item No. 43730

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,3S)-1-acetyl-2,3-dihydro-3-phenyl-2-[5-[7-(1-pyrrolidinyl)heptyl]-3-pyridinyl]-1H-indole-3-carbonitrile
CAS Number
2169272-46-0
Synonyms
  • KDM2A/7A Inhibitor 1
  • Lysine demethylase 2A/7A-IN-1
  • Lysine demethylase 2A/7A Inhibitor 1
Molecular Formula
C33H38N4O
Formula Weight
506.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/mlPBS (pH 7.2): Slightly soluble: 0.1-1 mg/ml
SMILES
N#C[C@]1(C2=CC=CC=C2N(C(C)=O)[C@H]1C3=CN=CC(CCCCCCCN4CCCC4)=C3)C5=CC=CC=C5
InChi Code
InChI=1S/C33H38N4O/c1-26(38)37-31-18-10-9-17-30(31)33(25-34,29-15-7-5-8-16-29)32(37)28-22-27(23-35-24-28)14-6-3-2-4-11-19-36-20-12-13-21-36/h5,7-10,15-18,22-24,32H,2-4,6,11-14,19-21H2,1H3/t32-,33+/m0/s1
InChi Key
VJAWJBZGYNKPQV-JHOUSYSJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $182

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    5 mg

    $863

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    10 mg

    $1,362

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    25 mg

    $2,723

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    Product Description

    KDM2A/7A-IN-1 is an inhibitor of lysine demethylase 2A (KDM2A) and KDM7A (IC50s = 0.16 and 0.19 µM, respectively).1 It is selective for KDM2A and -7A over KDM3A (IC50 = 39 µM), KDM4A, -4C, and -4D (IC50s = 639, 430, and 321 µM, respectively), KDM5B and -C (IC50s = 17 and 16 µM, respectively), KDM6B (IC50 = 20 µM), and KDM7B (IC50 = 34 µM). KDM2A/7A-IN-1 (1 and 10 µM) inhibits KDM2A-mediated demethylation of dimethylated histone H3 lysine 36 (H3K36me2) in HeLa cells.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gerken, P.A., Wolstenhulme, J.R., Tumber, A., et al. Discovery of a highly selective cell-active inhibitor of the histone lysine demethylases KDM2/7. Angew Chem. Int. Ed. Engl. 56(49), 15555-15559 (2017).