Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 2-[[[2-[[2-(dimethylamino)ethyl]ethylamino]-2-oxoethyl]amino]methyl]-4-pyridinecarboxylic acid, 2,4-bis(1-methylethoxy)phenyl ester, trihydrochloride
Purity: ≥98%
Formula Markup: C27H40N4O5 / 3HCl
Formula Weight: 610.0
CAS Number: 2863676-87-1
Notes: JQKD82 is a prodrug form of KDM5-C49, an inhibitor of Jumonji AT-rich interactive domain 1A (JARID1A), also known as lysine-specific demethylase 5A (KDM5A).{72506} It increases the levels of trimethylated lysine 4 on histone 3 (H3K4me3) in MOLP-8 and MM.1S multiple myeloma cells when used at concentrations of 0.3 and 1 µM. JQKD82 reduces the proliferation of MOLP-8 and MM.1S cells in a concentration-dependent manner and decreases the viability of primary CD138+ cells from patients with multiple myeloma when used at a concentration of 3 µM. It induces cell cycle arrest at the G0/G1 phase, as well as induces apoptosis, in MOLP-8 and MM.1S cells when used at a concentration of 1 µM. JQKD82 (50 mg/kg twice per day) decreases tumor growth and increases survival in a MOLP-8 mouse xenograft model.
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