| Identification | Back Directory | [Name]
Benzamide, 3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl)- | [CAS]
2003260-55-5 | [Synonyms]
CS-2874
KDM4B-IN-B3
NCGC00244536
KDM4B Inhibitor B3
KDM4B INHIBITOR COMPOUND B3
Benzamide, 3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl)- | [Molecular Formula]
C25H22N2O2 | [MDL Number]
MFCD31382180 | [MOL File]
2003260-55-5.mol | [Molecular Weight]
382.45 |
| Chemical Properties | Back Directory | [Boiling point ]
646.9±55.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF:30.0(Max Conc. mg/mL);78.44(Max Conc. mM)
DMF:PBS (pH 7.2) (1:2):0.33(Max Conc. mg/mL);0.86(Max Conc. mM)
DMSO:44.22(Max Conc. mg/mL);115.63(Max Conc. mM)
Ethanol:1.5(Max Conc. mg/mL);3.92(Max Conc. mM) | [form ]
A crystalline solid | [pka]
4.81±0.40(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
NCGC00244536 is a potent KDM4B inhibitor with an IC50 of 10 nM. | [Biological Activity]
NCGC00244536 is a potent KDM4B inhibitor with IC50 of 10 nM. | [in vitro]
NCGC00244536 displays high selectivity for the fast-growing AR-negative PC3 cells (IC 50 =40 nM) and over 100-fold selectivity against the immortalized prostate epithelial cell lines PrEC1 and PrEC4 . NCGC00244536 effectively inhibits AR-positive cell lines, including LNCaP and VCaP, with IC 50 s in the sub-micromolar range, and abolishes androgen-stimulated LNCaP cell growth. NCGC00244536 is also potent in inhibiting the growth of other cancer cell lines, including the breast cancer cell lines MDA-MB2 and MCF-7, with micromolar IC 50 s. | [in vivo]
Treatment with NCGC00244536 results in significant inhibition of tumor growth and animals do not exhibit any major toxicity and appear to be normal. Histological data clearly indicate that NCGC00244536-treated tumors have significant amount of cell apoptosis, necrosis, and fibrosis . | [IC 50]
KDM4 | [storage]
Store at -20°C | [References]
[1] Duan L, et al. KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes. Chem Biol. 2015 Sep 17;22(9):1185-96. DOI:10.1016/j.chembiol.2015.08.007 |
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