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Halofuginone hydrobromide

CAS No. : 64924-67-0

MCE 站：Halofuginone hydrobromide

产品活性：Halofuginone hydrobromide (RU-19110 hydrobromide) 是 Febrifugine 的一种低毒性衍生物，可从 Dichroa febrifuga 中分离出来。Halofuginone 是一种 ATP 竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂，K_i 为 18.3 nM。Halofuginone 通过抑制 TGF-β 活性可减轻骨关节炎。

研究领域：Cell Cycle/DNA Damage  |  TGF-beta/Smad  |  Stem Cell/Wnt  |  Anti-infection

作用靶点：DNA/RNA Synthesis  |  TGF-beta/Smad  |  Parasite

In Vitro: Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase.
The IC₅₀s of Halofuginone (1, 10, 100, 1000, 10000 nM; 48 hours) are 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
The IC₅₀s of Halofuginone (1, 10, 100, 1000 nM; 24 hours) for NRF2 protein are 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively. The IC₅₀ of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively.

In Vivo: Halofuginone (0.2, 0.5, 1 or 2.5?mg/kg; injected intraperitoneally every other day for 1?month) attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. Lower concentration (0.2 or 0.5 mg/kg) has minimal effects on subchondral bone and higher concentration (2.5 mg/kg) induces proteoglycan loss in articular cartilage.
Halofuginone (0.25 mg/kg; intraperitoneally injected; every day; 16 days) decreases NRF2 protein levels in tumors. While the tumor volumes do not change substantially between treatments with the vehicle, Halofuginone (0.25 mg/kg, intraperitoneally injected, every day) or cisplatin alone. Combined treatment with Halofuginone and Cisplatin significantly suppresses the tumor volume compared to treatment with Halofuginone or cisplatin alone.

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