TK-129 is a highly potent, selective, and orally efficacious KDM5B ((lysine demethylase 5B, JARID1B) inhibitor with IC50 of 44 nM in homogeneous time-resolved fluorescence assay (HTRF).
TK-129 also potently inhibits KDM5A with an IC50 value of 0.079 μM but is less effective toward KDM5C (IC50 = 0.353 μM).
TK-129 increases the expression level of KDM5B substrate H3K4me3 protein in neonatal rat cardiac fibroblasts (NRCFs), with low cytotoxicity.
TK-129 alleviates Ang II-induced activation, migration, and proliferation of myocardial fibroblasts in NRCFs.
TK-129 alleviates myocardial remodeling induced by isoproterenol (ISO) in pathological myocardial remodeling in vivo.
Physicochemical Properties
M.Wt
305.38
10 mM in DMSO (R)-1-Cyclopropyl-3-(1-(3-isopropyl-1H-pyrazole-5-carbonyl)pyrrolidin-3-yl)urea
Formula
C15H23N5O2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
Chemical Name/SMILES
