Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TK-129 is an orally active, potent inhibitor of KDM5B with IC 50 of 44 nM that is low-toxicity. TK-129 shows cardioprotective effects by inhibiting KDM5B and blocking the KDM5B -associated Wnt pathway. TK-129 can be used in cardiovascular disease studies which reduce isoprenaline-induced myocardial remodelling and fibrosis in vivo as well as reduce ang II-induced activation of cardiac fibroblasts in vitro [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
50 mg | 10-14 weeks | $ 789.00 | |
100 mg | 10-14 weeks | $ 1,280.00 |
Description | TK-129 is an orally active, potent inhibitor of KDM5B with IC 50 of 44 nM that is low-toxicity. TK-129 shows cardioprotective effects by inhibiting KDM5B and blocking the KDM5B -associated Wnt pathway. TK-129 can be used in cardiovascular disease studies which reduce isoprenaline-induced myocardial remodelling and fibrosis in vivo as well as reduce ang II-induced activation of cardiac fibroblasts in vitro [1]. |
In vitro | TK-129 significantly inhibits KDM5B activity, thereby substantially reducing the activation, migration, and proliferation of myofibroblasts that Ang II induces in vitro [1]. At a concentration of 10 μM over 48 hours, TK-129 demonstrates low cytotoxicity in NRCFs and NRCMs, maintaining cell survival rates above 90% [1]. Furthermore, when applied to NRCFs at concentrations ranging from 0.1 to 0.5 μM for 48 hours, TK-129 effectively targets and inhibits KDM5B activity. This engagement is evidenced by a dose-dependent increase in the expression of the KDM5B substrate, the H3K4me3 protein, indicating TK-129's precision in modulating specific histone modifications [1]. |
In vivo | TK-129 demonstrates good bio-safety and efficacy in various mouse models. At a dosage of 2 g/kg administered orally in a single dose, TK-129 was proven safe in mice, with all subjects surviving and exhibiting normal weight gain over two weeks. The compound, at 50 mg/kg given orally twice daily for 24 days, significantly mitigated isoproterenol-induced myocardial remodeling in C57BL/6 mice. Pharmacokinetic (PK) properties were favorable, evidenced by administration at 2 mg/kg intravenously or 10 mg/kg orally in male SD rats, yielding promising pharmacokinetic parameters such as clearance (CL), volume of distribution at steady-state (Vss), half-life (T1/2), time to reach maximum concentration (Tmax), maximum concentration (Cmax), area under the curve from 0 to 24 hours (AUC0-24), and bioavailability (F%). |
Molecular Weight | 305.38 |
Formula | C15H23N5O2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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