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TK-129

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].

Product Specifications

CAS Number

[3031476-73-7]

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

Available Sizes

Curated Selection

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