Halofuginone (RU-19110) |
| Catalog No.GC31650 |
Febrifugin 유도체인 Halofuginone(RU-19110)(RU-19110)은 Ki가 18.3nM인 경쟁적인 prolyl-tRNA 합성효소 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 55837-20-2
Sample solution is provided at 25 µL, 10mM.
Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga[1]. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM[2]. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity[3].
Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase[1]. The IC50 of Halofuginone is 114.6 and 58.9 nM in KYSE70 and A549 cells. The IC50s of Halofuginone for NRF2 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[1]. The amount of NRF2 protein is significantly decreased in the presence of Halofuginone in both the KYSE70 and A549 cell lines. NRF2 mRNA levels are not decreased, but rather are increased after application of Halofuginone to both KYSE70 and A549 cells, indicating that Halofuginone acts to decrease NRF2 protein expression at the post-transcriptional level. Time-course studies show that Halofuginone decreases NRF2 protein expression in KYSE70 and A549 cells within 12 hours of treatment[1].
Halofuginone attenuates progression of OA in anterior cruciate ligament transection (ACLT) mice. The optimal dose (1 mg/kg body weight) is identified using multiple concentrations of HF (0.2, 0.5, 1 or 2.5 mg/kg) injected every other day for 1 month post surgery. 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) 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].
[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.
| Cas No. | 55837-20-2 | SDF | |
| Canonical SMILES | O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3 | ||
| Formula | C16H17BrClN3O3 | M.Wt | 414.68 |
| Solubility | DMSO : 9 mg/mL (21.70 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4115 mL | 12.0575 mL | 24.115 mL |
| 5 mM | 0.4823 mL | 2.4115 mL | 4.823 mL |
| 10 mM | 0.2411 mL | 1.2057 mL | 2.4115 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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