TK-129 free base · Synonyms: (R)-TK-129 | 1905481-40-4 (racemate)

TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor.

For research use only. Not for human or veterinary use.

Target Wnt Histone Demethylase

Research area Cardiovascular Disease

Purity 99.40% Stock Inquire

Data Sheet SDS COA

TK-129 structure

CAS No.: 3031476-73-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 650.00	BP-02243-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02243-250mg	In stock	Get quote
500 mg	USD 1,350.00	BP-02243-500mg	In stock	Get quote
1 g	USD 1,900.00	BP-02243-1g	In stock	Get quote
2 g	USD 3,580.00	BP-02243-2g	In stock	Get quote

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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.

Biological activity

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, 0.4, 0.5 μM; 48 h) can engage toand inhibit KDM5B activity in NRCFs. In Vivo TK-129 (2 g/kg; p.o.; single) shows good bio-safety in mice. TK-129 (50 mg/kg; p.o.; twice daily for 24 days) effectively reduces isoproterenol-induced pathological myocardial remodeling in vivo. TK-129 (2 or 10 mg/kg; i.v. or p.o.; single) demonstrates favorable PK properties in vivo.

Identifiers

SMILES: O=C(N[C@H]1CN(C(C2=NNC(C(C)C)=C2)=O)CC1)NC3CC3
InChIKey: WNSMPEBHTSITSG-LLVKDONJSA-N

Specifications

MW (average): 305.3754
Formula: C₁₅H₂₃N₅O₂
CAS No.: 3031476-73-7
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro: DMSO 100 mg/mL

Documents

References

[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.

Same target

Search Wnt

Same research area

Search Cardiovascular Disease