TK-129

• Description :

  TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with high affinity; IC50=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 cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease[1].

• UNSPSC :

  12352005

• Target :

  Histone Demethylase; Wnt

• Type :

  Reference compound

• Related Pathways :

  Epigenetics; Stem Cell/Wnt

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Cardiovascular Disease

• Assay Protocol :

  https://www.medchemexpress.com/tk-129.html

• Purity :

  98.0

• Solubility :

  DMSO : 100 mg/mL (ultrasonic)

• Smiles :

  O=C(N[C@H]1CN(C(C2=NNC(C(C)C)=C2)=O)CC1)NC3CC3

• Molecular Formula :

  C15H23N5O2

• Molecular Weight :

  305.38

• References & Citations :

  [1]Tang K, et al. Discovery of Novel Pyrazole-Based KDM5B Inhibitor TK-129 and Its Protective Effects on Myocardial Remodeling and Fibrosis. J Med Chem. 2022 Sep 16.

• Shipping Conditions :

  Blue Ice

• Storage Conditions :

  -20°C, 3 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  KDM5

• CAS Number :

  [3031476-73-7]