Halofuginone - CAS:55837-20-2

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Halofuginone (Synonyms:常山酮; RU-19110)

目录号 : KM12250 CAS No. : 55837-20-2 纯度 : 98%

产品说明书产品使用指南

Halofuginone (RU-19110)，Febrifugine 的衍生物，是一种竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂，K_i 为 18.3 nM。Halofuginone 是 I 型胶原 (type-I collagen) 合成的特异性抑制剂，并通过抑制 TGF-β 活性可减轻骨关节炎。Halofuginone 也是一种有效的肺血管扩张剂，可激活 Kv 通道并阻断电压门控、受体操作和存储操作的 Ca²⁺ channels 通道。Halofuginone 具有抗疟疾、抗炎、抗癌、抗纤维化作用。

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生物活性

Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

体外研究

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.
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 Ca entry (ROCE) in HEK cells transfected with calcium-sensing receptor gene and attenuated store-operated (SOCE) Ca entry in PASMC.

Cell Viability Assay

Cell Line:	KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation
Concentration:	1, 10, 100, 1000, 10000 nM
Incubation Time:	48 hours
Result:	The IC₅₀s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.

Western Blot Analysis

Cell Line:	KYSE70 cells from human oesophageal cancer harbouring a mutation in the NRF2 gene and A549 cells harbouring theKEAP1 gene mutation.
Concentration:	1, 10, 100, 1000 nM
Incubation Time:	24 hours
Result:	The IC₅₀s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.

体内研究

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.
Intraperitoneal administration of Halofuginone (0.3mg/kg, for 2 weeks) partially reverses the established pulmonary hypertension in mice.

Animal Model:	3-month-old male C57BL/6J (WT) mice
Dosage:	0.2, 0.5, 1 or 2.5 mg/kg
Administration:	Injected intraperitoneally every other day for 1 month
Result:	Attenuated progression of OA in ACLT mice.

Animal Model:	Male nude mice (BALB/C nu/nu mice) (6-8-week)
Dosage:	0.25 mg/kg
Administration:	Intraperitoneally injected; every day; 16 days
Result:	The combined treatment with Cisplatin significantly suppressed the tumor volume. NRF2 protein levels in tumors were indeed decreased.

分子式

C₁₆H₁₇BrClN₃O₃

分子量

414.68

CAS号

55837-20-2

中文名称

常山酮；卤夫酮；哈洛夫酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4115 mL	12.0575 mL	24.1150 mL
5 mM	0.4823 mL	2.4115 mL	4.8230 mL
10 mM	0.2411 mL	1.2057 mL	2.4115 mL

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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。