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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O=C(O)[C@@H]1[C@H](C1)C(C2=CC=C(C(Cl)=C2)Cl)=O
InChI
1S/C11H8Cl2O3/c12-8-2-1-5(3-9(8)13)10(14)6-4-7(6)11(15)16/h1-3,6-7H,4H2,(H,15,16)/t6-,7-/m0/s1
InChI 密鑰
ZBRKMOHDGFGXLN-BQBZGAKWSA-N
生化／生理作用
UPF-648 is a potent, active site-targeting kynurenine 3-monooxygenase (KMO; kynurenine 3-hydroxylase) inhibitor (IC50 = 20 nM) that prevents productive binding of the substrate L-kynurenine by perturbing the local active-site structure. UPF-648 protects against neurodegeneration in a murine (30 mg/kg, i.p.) and a Drosophila (100 μM in maize media) model of Huntington′s disease by shifting kynurenine pathway metabolism towards enhanced neuroprotective kynurenic acid (KYNA) formation and away from the free radicals generator 3-hydroxykynurenine (3-HK) and the excitotoxic quinolinic acid (QUIN).
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Endogenous kynurenate controls the vulnerability of striatal neurons to quinolinate: Implications for Huntington's disease
Sapko MT, Guidetti P, Yu P, Tagle DA, Pellicciari R, Schwarcz R
Experimental Neurology, 197, 31-40 (2006)
Biochemistry and structural studies of kynurenine 3-monooxygenase reveal allosteric inhibition by Ro 61-8048
Faseb Journal, 32, 2036-2045 (2018)
Susanna Campesan et al.
Current biology : CB, 21(11), 961-966 (2011-06-04)
Neuroactive metabolites of the kynurenine pathway (KP) of tryptophan degradation have been implicated in the pathophysiology of neurodegenerative disorders, including Huntington's disease (HD) [1]. A central hallmark of HD is neurodegeneration caused by a polyglutamine expansion in the huntingtin (htt)
Marta Amaral et al.
Nature, 496(7445), 382-385 (2013-04-12)
Inhibition of kynurenine 3-monooxygenase (KMO), an enzyme in the eukaryotic tryptophan catabolic pathway (that is, kynurenine pathway), leads to amelioration of Huntington's-disease-relevant phenotypes in yeast, fruitfly and mouse models, as well as in a mouse model of Alzheimer's disease. KMO
Tzu-Ting Huang et al.
EBioMedicine, 54, 102717-102717 (2020-04-09)
Triple-negative breast cancer (TNBC) is aggressive and has a poor prognosis. Kynurenine 3-monooxygenase (KMO), a crucial kynurenine metabolic enzyme, is involved in inflammation, immune response and tumorigenesis. We aimed to study the role of KMO in TNBC. KMO alteration and
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