TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC 50 =44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B -associated Wnt pathway. TK-129 reduces ang II-induced activation of car Appearance:Solid IC50& Target:KDM5 44 nM (IC 50 ) In Vitro:TK-129 mediates inhibition of KDM5B activity significantly reduces the activation, migration, and proliferation of myofibroblasts induced by Ang II in vitro. TK-129 (10 μM; 48 h) shows low cytotoxicity in NRCFs and NRCMs. TK-129 (0.1, 0.2, 0.3, In Vivo:TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice. TK-129 (50mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo. TK-129 (2 or 10mg/kg; i.v. or p.o.; single) demo Biological Activity:TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC 50 =44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B -associated Wnt pathway. TK-129 reduces ang II-induced activation of car
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TK-129
CAS number:unknown molecular formula:C15H23N5O2
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C15H23N5O2 |
| molecular weight | 305.38 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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