A KDM4B/JMJD2B inhibitor (IC50 = ~10 nM); selective for KDM4B/JMJD2B over KDM5A/JARID1 and LSD1 but does inhibit KDM4A/JMJD2A

NCGC00244536 – 5 mg

Brand:
Cayman
CAS:
2003260-55-5
Storage:
-20
UN-No:
Non-Hazardous - /

NCGC00244536 is an inhibitor of KDM4B/JMJD2B histone lysine demethylase (IC50 = ~10 nM).{29614} 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.  

 

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Description

A KDM4B/JMJD2B inhibitor (IC50 = ~10 nM); selective for KDM4B/JMJD2B over KDM5A/JARID1 and LSD1 but does inhibit KDM4A/JMJD2A, KDM4C/JMJD2C, and KDM4D/JMJD2D at 10 μM; inhibits the growth of various prostate cancer cells (IC50s = <1 μM for all); reduces androgen receptor levels and H3K9 trimethylation in isolated human solid prostate tumors; reduces tumor volume in a PC3 mouse xenograft model at 20 mg/kg

Formal name: 3-(8-hydroxy-6-quinolinyl)-N-(3-phenylpropyl)-benzamide

Synonyms: 

Molecular weight: 382.5

CAS: 2003260-55-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Demethylases||Research Area|Epigenetics, Transcription, & Translation|Erasers

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