CAS:55837-20-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
Array ( [133] => Array ( [id] => 133 [name] => Inhibitors & Antagonists & Agonists [children] => Array ( [352] => Array ( [id] => 352 [name] => Protein Tyrosine Kinase/PTK ) [350] => Array ( [id] => 350 [name] => PI3K/Akt/mTOR ) [351] => Array ( [id] => 351 [name] => Endocrinology & Hormones ) [357] => Array ( [id] => 357 [name] => Angiogenesis ) [358] => Array ( [id] => 358 [name] => HIF ) [363] => Array ( [id] => 363 [name] => Immunology & Inflammation ) [364] => Array ( [id] => 364 [name] => Stem Cells ) [365] => Array ( [id] => 365 [name] => Apoptosis ) [377] => Array ( [id] => 377 [name] => Metabolic Enzyme & Protease ) [379] => Array ( [id] => 379 [name] => Autophagy ) [380] => Array ( [id] => 380 [name] => ER Stress ) [384] => Array ( [id] => 384 [name] => Cell Cycle ) [385] => Array ( [id] => 385 [name] => Cytoskeleton ) [386] => Array ( [id] => 386 [name] => DNA Damage & DNA Repai ) [387] => Array ( [id] => 387 [name] => Epigenetics ) [388] => Array ( [id] => 388 [name] => Ubiquitin ) [389] => Array ( [id] => 389 [name] => JAK/STAT ) [390] => Array ( [id] => 390 [name] => GPCR & G Protein ) [391] => Array ( [id] => 391 [name] => Neuronal Signal Pathway ) [392] => Array ( [id] => 392 [name] => MAPK ) [393] => Array ( [id] => 393 [name] => NF-κB ) [394] => Array ( [id] => 394 [name] => Membrane Transporter & Ion Channel ) [395] => Array ( [id] => 395 [name] => TGF-β/Smad ) [396] => Array ( [id] => 396 [name] => Hippo ) [775] => Array ( [id] => 775 [name] => Antibody-drug Conjugate/ADC Related ) [122] => Array ( [id] => 122 [name] => Others ) ) [num] => 2140 ) )
>
Small Molecule Compounds >
Inhibitors & Antagonists & Agonists >
Cell Cycle >
HalofuginoneCAS:55837-20-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:White to off-white Solid
CAS | 55837-20-2 |
Chinese Name | 常山酮 |
English Name | Halofuginone |
Synonyms | 卤夫酮;RU-19110;Tempostatin;empostatin |
Molecular Formula | C16H17BrClN3O3 |
Molecular Weight | 414.68 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
Delivery Time | 1-2 Days |
EC | EINECS 1806241-263-5 |
MDL | MFCD09834143 |
SMILES | O=C1N(CC(C[C@@H]2NCCC[C@H]2O)=O)C=NC3=C1C=C(Cl)C(Br)=C3 |
InChIKey | LVASCWIMLIKXLA-LSDHHAIUSA-N |
InChI | InChI=1S/C16H17BrClN3O3/c17-11-6-13-10(5-12(11)18)16(24)21(8-20-13)7-9(22)4-14-15(23)2-1-3-19-14/h5-6,8,14-15,19,23H,1-4,7H2/t14-,15+/m0/s1 |
PubChem CID | 400772 |
Target Point | prolyl-tRNA synthetase |
Passage | Cell Cycle;DNA Damage/DNA Repair |
Background | Halofuginone is a competitive prolyl-tRNA synthetase inhibitor. Halofuginone has anti-malarial, anti-inflammatory, anti-cancer and anti-fibrosis activities. |
Biological Activity | Halofuginone 是 Febrifugine 的一种低毒性衍生物,可从 Dichroa febrifuga 中分离出来[1]。Halofuginone 是一种 ATP 竞争性的脯氨酰-tRNA 合成酶 (prolyl-tRNA synthetase) 抑制剂,Ki 为 18.3 nM[2]。Halofuginone 通过抑制 TGF-β 活性可减轻骨关节炎[3]。 |
In Vitro | Halofuginone通过占据脯氨酰-tRNA合成酶的脯氨酸和tRNA结合口袋竞争性地抑制脯氨酰-tRNA合成酶[1]。在KYSE70和A549细胞中,Halofuginone的IC50为114.6和58.9nM。在KYSE70和A549细胞中,Halofuginone对NRF2的IC50分别为22.3和37.2nM。在KYSE70和A549细胞中,Halofuginone对全球蛋白质合成的IC50分别为22.6和45.7 nM [1]。在KYSE70和A549细胞系中,在Halofuginone存在下NRF2蛋白的量显著降低。在将Halofuginone应用于KYSE70和A549细胞后,NRF2 mRNA水平没有降低,而是增加,表明Halofuginone在转录后水平起降低NRF2蛋白表达的作用。时程研究表明,Halofuginone在治疗12小时内降低了KYSE70和A549细胞中NRF2蛋白的表达[1]。 |
In Vivo | Halofuginone减弱前交叉韧带横断(ACLT)小鼠的OA进展。使用多次浓度的HF(0.2,0.5,1或2.5mg/kg)在手术后每隔一天注射1个月来确定最佳剂量(1mg/kg体重)。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)可诱导关节软骨中蛋白多糖的丢失[3]。 Halofuginone(0.25mg/kg,腹膜内)降低肿瘤中的NRF2蛋白水平。虽然与载体治疗之间肿瘤体积没有显著变化,但是单独使用卤夫酮(0.25 mg/kg,腹膜内注射,每天)或单独使用顺铂,与单独使用Halofuginone或顺铂治疗相比,Halofuginone和顺铂联合治疗显著抑制了肿瘤体积[1]。 |
Data Literature Source | [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. |
Unit | Bottle |
Specification | 5mg |