TK-129 | KDM5B inhibitor | Probechem Biochemicals

Chemical Structure : TK-129

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TK-129 (TK129)

货号: PC-22358Not For Human Use, Lab Use Only.

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).

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生物&药学活性

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.

物理化学性质&存储条件

分子量	305.38
分子式	C15H23N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-1-Cyclopropyl-3-(1-(3-isopropyl-1H-pyrazole-5-carbonyl)pyrrolidin-3-yl)urea

参考文献

1. Kai Tang, et al. J Med Chem. 2022 Oct 13;65(19):12979-13000.

TK-129 (TK129)

生物&药学活性

物理化学性质&存储条件

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TK-129 (TK129)

生物&药学活性

物理化学性质&存储条件

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