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.
TK-129 structure
CAS No.: 3031476-73-7
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 |
Need another size or custom synthesis? Request a quote.
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