2. Membrane Transporter/Ion Channel Neuronal Signaling Cell Cycle/DNA Damage Anti-infection TGF-beta/Smad Stem Cell/Wnt
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  4. Halofuginone hydrochloride

Halofuginone hydrochloride  (Synonyms: RU-19110 hydrochloride)

目录号: HY-N1584B
产品使用指南

摩尔计算器

Halofuginone (RU-19110) hydrobromid，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，Ki 为 18.3 nM。Halofuginone hydrobromid 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 hydrobromid 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 hydrobromid 具有抗疟疾、抗炎、抗癌、抗纤维化作用。

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Halofuginone hydrochloride Chemical Structure

Halofuginone hydrochloride Chemical Structure

CAS No. : 1217623-74-9

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规格 价格 是否有货 数量
500 μg ￥2610
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1 mg ￥4680
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Halofuginone hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects[1][2][3][4][5].

IC50 & Target

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)[2]
体外研究
(In Vitro)

Halofuginone hydrobromid 通过占据脯氨酰-tRNA 合成酶的脯氨酸和 tRNA 结合袋来竞争性抑制脯氨酰-tRNA 合成酶[1]。
Halofuginone hydrobromid (1、10、100、1000、10000 nM; 48 小时) 在 KYSE70 和 A549 细胞中的 IC 50 分别为 1.6 和 58.9 nM[1]。
在 KYSE70 和 A549 细胞中，Halofuginone hydrobromid (1、10、100、1000 nM; 24 h) 对 NRF2 蛋白的 IC 50 值分别为 22.3 和 37.2 nM。在 KYSE70 和 A549 细胞中，Halofuginone hydrobromid 对整体蛋白质合成的 IC50 分别为 22.6 和 45.7 nM[1]。
Halofuginone hydrobromid 可增加肺动脉平滑肌细胞 (PASMC) 中的电压门控 K+ (Kv) 电流以及转染 KCNA5 基因的 HEK 细胞中通过 KCNA5 通道的 K+ 电流。Halofuginone hydrobromid (0.03-1μM) 抑制转染钙敏感受体基因的 HEK 细胞中受体操纵的 Ca2+ 内流 (ROCE)，并减弱 PASMC 中钙池操纵的 (SOCE) Ca2+ 内流 [5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Halofuginone hydrochloride 相关抗体:

Western Blot Analysis[1]

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: 24 h
Result: The IC50s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.

Cell Viability Assay[1]

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 h
Result: The IC50s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.
体内研究
(In Vivo)

Halofuginone hydrobromid (0.2, 0.5, 1 or 2.5 mg/kg; injected intraperitoneally every other day for 1 month) 可减轻前交叉韧带横断 (ACLT) 小鼠的 OA 进展。较低浓度 (0.2 或 0.5 mg/kg) 对软骨下骨的影响最小，较高浓度 (2.5 mg/kg) 会导致关节软骨中蛋白聚糖损失[3]。
Halofuginone hydrobromid (0.25 mg/kg; intraperitoneally injected; every day; 16 days) 可降低肿瘤中的 NRF2 蛋白水平。虽然在使用载体、Halofuginone hydrobromid (0.25 mg/kg, intraperitoneally injected, every day) 或单独顺铂治疗之间肿瘤体积没有显着变化。与单独使用 Halofuginone hydrobromid 或顺铂治疗相比，Halofuginone hydrobromid 和顺铂联合治疗可显着抑制肿瘤体积[1]。
腹腔内注射Halofuginone (0.3mg/kg, for 2 weeks) 可部分逆转小鼠已形成的肺动脉高压[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3-month-old male C57BL/6J (WT) mice[3]
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)[1]
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.
分子量

451.14

Formula

C16H18BrCl2N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Halofuginone hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Halofuginone1217623-74-9RU-19110RU19110RU 19110Calcium ChannelDNA/RNA SynthesisParasiteSodium ChannelTGF-beta/SmadCa2+ channelsCa channelsNa channelsNa+ channelsTransforming growth factor betatype-Icollagencollagen-1prolyl-tRNAosteoarthritisTGF-βInhibitorinhibitorinhibit

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