| Bioactivity | 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]. |
| Target | Ki: 18.3±0.5 nM (prolyl-tRNA synthetase) |
| Invitro | 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. 0 --> Halofuginone hydrochloride 相关抗体: Western Blot Analysis[1] Cell Line: |
| 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: |
| CAS | 1217623-74-9 |
| Formula | C16H18BrCl2N3O3 |
| Molar Mass | 451.14 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Tsuchida K, et al. Halofuginone enhances the chemo-sensitivity of cancer cells by suppressing NRF2 accumulation. Free Radic Biol Med. 2017 Feb;103:236-247. [2]. Keller TL, et al. Halofuginone and other Febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7. [3]. Cui Z, et al. Halofuginone attenuates osteoarthritis by inhibition of TGF-β activity and H-type vessel formation in subchondral bone. Ann Rheum Dis. 2016 Sep;75(9):1714-21. [4]. Tracy L McGaha, et al. Halofuginone, an inhibitor of type-I collagen synthesis and skin sclerosis, blocks transforming-growth-factor-beta-mediated Smad3 activation in fibroblasts. J Invest Dermatol. 2002 Mar;118(3):461-70. [5]. Pritesh P Jain, et al. Halofuginone, a Promising Drug for Treatment of Pulmonary Hypertension. Br J Pharmacol. 2021 Mar 10. |
Halofuginone hydrochloride
CAS: 1217623-74-9 F: C16H18BrCl2N3O3 W: 451.14
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a
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