A KDM4 inhibitor
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QC6352

Item No. 26231

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[[(1R)-1,2,3,4-tetrahydro-6-(methylphenylamino)-1-naphthalenyl]methyl]amino]-4-pyridinecarboxylic acid
CAS Number
1851373-36-8
Molecular Formula
C24H25N3O2
Formula Weight
387.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1mg/mlDMSO: Sparingly soluble: 1-10mg/ml
SMILES
O=C(O)C1=CC=NC=C1NC[C@@H]2CCCC3=C2C=CC(N(C4=CC=CC=C4)C)=C3
InChi Code
InChI=1S/C24H25N3O2/c1-27(19-8-3-2-4-9-19)20-10-11-21-17(14-20)6-5-7-18(21)15-26-23-16-25-13-12-22(23)24(28)29/h2-4,8-14,16,18,26H,5-7,15H2,1H3,(H,28,29)/t18-/m0/s1
InChi Key
XSMABFRQESMONQ-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    QC6352 is an inhibitor of lysine demethylase 4 (KDM4).1 It is selective for the KDM4 isoforms KDM4A, KDM4B, KDM4C, and KDM4D (IC50s = 104, 56, 35, and 104 nM, respectively) over KDM2B, KDM3A, KDM3B, KDM6B, and PHD finger protein 8 (PHF8; IC50s = >4,000 nM for all) but does inhibit KDM5B (IC50 = 750 nM). QC6352 increases trimethylation of lysine 36 on histone H3 (H3K36Me3) in KYSE-150 esophageal carcinoma cells overexpressing KDM4C (EC50 = 1.3 nM). It reduces the proliferation of KYSE-150 cells (EC50 = 3.5 nM) but not IMR-90 fibroblasts (IC50 = >30 µM). QC6352 (10, 25, and 50 mg/kg) reduces tumor volume in a BR0859f patient-derived xenograft (PDX) mouse model of HER2-positive breast cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chen, Y.K., Bonaldi, T., Cuomo, A., et al. Design of KDM4 inhibitors with antiproliferative effects in cancer models. ACS Med. Chem. Lett. 8(8), 869-874 (2017).