NCGC00244536

NCGC00244536 is an inhibitor of KDM4B/JMJD2B histone lysine demethylase (IC50 = ~10 nM). 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.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: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 20 mg/ml. lambdamax: 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.