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  4. Halofuginone hydrochloride

Halofuginone hydrochloride  (Synonyms: RU-19110 hydrochloride)

目錄號(hào): HY-N1584B
產(chǎn)品使用指南

Halofuginone (RU-19110) hydrobromid，F(xiàn)ebrifugine 的衍生物，是一種競(jìng)爭(zhēng)性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制劑，Ki 為 18.3 nM。Halofuginone hydrobromid 是 I 型膠原 (type-I collagen) 合成的特異性抑制劑，并通過(guò)抑制 TGF-β 活性可減輕骨關(guān)節(jié)炎。Halofuginone hydrobromid 也是一種有效的肺血管擴(kuò)張劑，可激活 Kv 通道并阻斷電壓門控、受體操作和存儲(chǔ)操作的 Ca2+ channels 通道。Halofuginone hydrobromid 具有抗瘧疾、抗炎、抗癌、抗纖維化作用。

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Halofuginone hydrochloride Chemical Structure

Halofuginone hydrochloride Chemical Structure

CAS No. : 1217623-74-9

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Halofuginone hydrochloride 的其他形式現(xiàn)貨產(chǎn)品:

Customer Review

Other Forms of Halofuginone hydrochloride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
體外研究
(In Vitro)

Halofuginone hydrobromid 通過(guò)占據(jù)脯氨酰-tRNA 合成酶的脯氨酸和 tRNA 結(jié)合袋來(lái)競(jìng)爭(zhēng)性抑制脯氨酰-tRNA 合成酶[1]。
Halofuginone hydrobromid (1、10、100、1000、10000 nM; 48 小時(shí)) 在 KYSE70 和 A549 細(xì)胞中的 IC 50 分別為 1.6 和 58.9 nM[1]。
在 KYSE70 和 A549 細(xì)胞中，Halofuginone hydrobromid (1、10、100、1000 nM; 24 h) 對(duì) NRF2 蛋白的 IC 50 值分別為 22.3 和 37.2 nM。在 KYSE70 和 A549 細(xì)胞中，Halofuginone hydrobromid 對(duì)整體蛋白質(zhì)合成的 IC50 分別為 22.6 和 45.7 nM[1]。
Halofuginone hydrobromid 可增加肺動(dòng)脈平滑肌細(xì)胞 (PASMC) 中的電壓門控 K+ (Kv) 電流以及轉(zhuǎn)染 KCNA5 基因的 HEK 細(xì)胞中通過(guò) KCNA5 通道的 K+ 電流。Halofuginone hydrobromid (0.03-1μM) 抑制轉(zhuǎn)染鈣敏感受體基因的 HEK 細(xì)胞中受體操縱的 Ca2+ 內(nèi)流 (ROCE)，并減弱 PASMC 中鈣池操縱的 (SOCE) Ca2+ 內(nèi)流 [5]。

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

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.
體內(nèi)研究
(In Vivo)

Halofuginone hydrobromid 通過(guò)占據(jù)脯氨酰-tRNA 合成酶的脯氨酸和 tRNA 結(jié)合袋來(lái)競(jìng)爭(zhēng)性抑制脯氨酰-tRNA 合成酶[1]。
Halofuginone hydrobromid (1、10、100、1000、10000 nM; 48 小時(shí)) 在 KYSE70 和 A549 細(xì)胞中的 IC 50 分別為 1.6 和 58.9 nM[1]。
在 KYSE70 和 A549 細(xì)胞中，Halofuginone hydrobromid (1、10、100、1000 nM; 24 h) 對(duì) NRF2 蛋白的 IC 50 值分別為 22.3 和 37.2 nM。在 KYSE70 和 A549 細(xì)胞中，Halofuginone hydrobromid 對(duì)整體蛋白質(zhì)合成的 IC50 分別為 22.6 和 45.7 nM[1]。
Halofuginone hydrobromid 可增加肺動(dòng)脈平滑肌細(xì)胞 (PASMC) 中的電壓門控 K+ (Kv) 電流以及轉(zhuǎn)染 KCNA5 基因的 HEK 細(xì)胞中通過(guò) KCNA5 通道的 K+ 電流。Halofuginone hydrobromid (0.03-1μM) 抑制轉(zhuǎn)染鈣敏感受體基因的 HEK 細(xì)胞中受體操縱的 Ca2+ 內(nèi)流 (ROCE)，并減弱 PASMC 中鈣池操縱的 (SOCE) Ca2+ 內(nèi)流 [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 號(hào)
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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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.

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Halofuginone hydrochloride
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HY-N1584B
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