A KDM4B/JMJD2B inhibitor
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NCGC00244536

Item No. 18478

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl)-benzamide
CAS Number
2003260-55-5
Molecular Formula
C25H22N2O2
Formula Weight
382.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mLDMSO: Soluble: ≥10 mg/mL
λmax
278 nm
SMILES
OC1=C(N=CC=C2)C2=CC(C3=CC=CC(C(NCCCC4=CC=CC=C4)=O)=C3)=C1
InChi Code
InChI=1S/C25H22N2O2/c28-23-17-22(16-20-12-6-13-26-24(20)23)19-10-4-11-21(15-19)25(29)27-14-5-9-18-7-2-1-3-8-18/h1-4,6-8,10-13,15-17,28H,5,9,14H2,(H,27,29)
InChi Key
NYKBXXGHEMXSBB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $158

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    10 mg

    $290

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    25 mg

    $653

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    Product Description

    NCGC00244536 is an inhibitor of KDM4B/JMJD2B histone lysine demethylase (IC50 = ~10 nM).1 It is selective for KDM4B/JMJD2B over KDM5A/JARID1 and lysine-specific demethylase 1 (LSD1) but does inhibit KDM4A/JMJD2A, KDM4C/JMJD2C, and KDM4D/JMJD2D at 10 μM. NCGC00244536 inhibits the growth of PC3, DU145, LNCaP, VCaP, and C4-2 prostate cancer cells (IC50s = <1 μM for all). It reduces androgen receptor levels and trimethylation of histone 3 lysine 9 (H3K9) in isolated human solid prostate tumors. NCGC00244536 (20 mg/kg, s.c.) reduces tumor volume in a PC3 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duan, L., Rai, G., Roggero, C., et al. KDM4/JMJD2 histone demethylase inhibitors block prostate tumor growth by suppressing the expression of AR and BMYB-regulated genes. Chem. Biol. 22(9), 1185-1196 (2015).