Halofuginone (RU-19110), a Febrifugine derivative, is a competitiveprolyl-tRNA synthetaseinhibitor with aK_iof 18.3 nM^[1][2]. Halofuginone is a specific inhibitor oftype-I collagensynthesis and attenuates osteoarthritis (OA) by inhibition ofTGF-βactivity^[3][4]. Halofuginone is also a potent pulmonary vasodilator by activatingKv channelsand blocking voltage-gated, receptor-operated and store-operatedCa²⁺channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects^[5].

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)^[2]

Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase^[1].
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 IC₅₀of Halofuginone for global protein synthesis is 22.6 and 45.7 nM in KYSE70 and A549 cells, respectively^[1].
Halofuginone increases voltage-gated K⁺(Kv) currents in pulmonary artery smooth muscle cells (PASMC) and K⁺currents through KCNA5 channels in HEK cells transfected with KCNA5 gene. Halofuginone (0.03-1μM) inhibits receptor-operated Ca²⁺entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuated store-operated (SOCE) Ca²⁺entry in PASMC^[5].

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^[3].
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^[1].
Intraperitoneal administration of Halofuginone (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice^[5].

414.68

Solid

C₁₆H₁₇BrClN₃O₃

55837-20-2

常山酮；卤夫酮；哈洛夫酮

• Alkaloids
• Piperidine Alkaloids

• Plants
• Saxifragaceae
• Dichroa febrifugaLour

Room temperature in continental US; may vary elsewhere.

DMSO : 20 mg/mL(48.23 mM;ultrasonic and adjust pH to 5 with HCl)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2 mg/mL (4.82 mM); Clear solution

  此方案可获得 ≥ 2 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2 mg/mL (4.82 mM); Clear solution

  此方案可获得 ≥ 2 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 0.67 mg/mL (1.62 mM); Clear solution

  此方案可获得 ≥ 0.67 mg/mL (1.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。