Chemical Structure : TK-129
CAS No.:
3031476-73-7
TK-129
(TK129)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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
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M.Wt
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305.38
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Formula
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C15H23N5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-1-Cyclopropyl-3-(1-(3-isopropyl-1H-pyrazole-5-carbonyl)pyrrolidin-3-yl)urea
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References
1. Kai Tang, et al. J Med Chem. 2022 Oct 13;65(19):12979-13000.
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