1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
    Anti-infection
  2. DNA/RNA Synthesis
    Parasite
    TGF-beta/Smad
  3. Halofuginone

Halofuginone (Synonyms: RU-19110)

製品番号: HY-N1584 純度: 98.32%
取扱説明書

Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone attenuates osteoarthritis (OA) by inhibition of TGF-β activity.

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Halofuginone 構造式

Halofuginone 構造式

CAS 番号 : 55837-20-2

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 99 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 140 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 280 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 450 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 750 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

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].

IC50 & Target

Ki: 18.3±0.5 nM (prolyl-tRNA synthetase)[2]

体外実験

Halofuginone competitively inhibits prolyl-tRNA synthetase by occupying both the prolineand tRNA-binding pockets of prolyl-tRNA synthetase[1].
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[1].

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 hours
Result: The IC50s were 114.6 and 58.9 nM in KYSE70 and A549 cells, respectively.

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 nM
Incubation Time: 24 hours
Result: The IC50s for NRF2 protein were 22.3 and 37.2 nM in KYSE70 and A549 cells, respectively.
体内実験

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[3].
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[1].

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.
臨床実験
分子量

414.68

分子式

C₁₆H₁₇BrClN₃O₃

CAS 番号

55837-20-2

SMILES

O=C1N(CC(C[[email protected]@H]2NCCC[[email protected]]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 9 mg/mL (21.70 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
参考文献
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Keywords:

HalofuginoneRU-19110RU19110RU 19110DNA/RNA SynthesisParasiteTGF-beta/SmadTransforming growth factor betaInhibitorinhibitorinhibit

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製品名:
Halofuginone
製品番号:
HY-N1584
数量:
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