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品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]/D +175 to +195°, c = 1 in methylene chloride
儲存條件
protect from light
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
ClC1=CC=C(NC2=C3CCC[C@H]2NC(C4=NC=CC=C4)=O)C3=C1
InChI
1S/C18H16ClN3O/c19-11-7-8-14-13(10-11)12-4-3-6-15(17(12)21-14)22-18(23)16-5-1-2-9-20-16/h1-2,5,7-10,15,21H,3-4,6H2,(H,22,23)
InChI 密鑰
WJQBOBGVBBZLJU-UHFFFAOYSA-N
生化/生理作用
GSK983 blocks RNA virus replication with EC50 values of 10–40 nM, and also blocks cell proliferation. GSK983 acts by inhibition of dihydroorotate dehydrogenase (DHODH), necesssary for pyrimidine biosynthesis. Exogenous deoxycytidine was able to reduce GSK983 cytotoxicity, allowing cells to synthesize DNA, but still preventing RNA virus replication. GSK983 was active against dengue fever and Venezuelan equine encephalitis viruses.
GSK983 is a tetrahydrocarbazole or a broad spectrum antiviral lead compound. GSK983 acts by stimulating a subset of interferon-stimulated genes.
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2
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
GSK983: a novel compound with broad-spectrum antiviral activity.
Antiviral Research, 82(1), 1-11 (2009)
Nature chemical biology, 12(5), 361-366 (2016-03-29)
Broad-spectrum antiviral drugs targeting host processes could potentially treat a wide range of viruses while reducing the likelihood of emergent resistance. Despite great promise as therapeutics, such drugs remain largely elusive. Here we used parallel genome-wide high-coverage short hairpin RNA
Antiviral research, 82(1), 1-11 (2009-02-04)
GSK983, a novel tetrahydrocarbazole, inhibits the replication of a variety of unrelated viruses in vitro with EC(50) values of 5-20 nM. Both replication of the adenovirus Ad-5 and the polyoma virus SV-40, and episomal maintenance of human papillomaviruses (HPV) and
Parallel shRNA and CRISPR-Cas9 screens enable antiviral drug target identification.
Nature Chemical Biology, 12(5), 361-366 (2016)
Bioorganic & medicinal chemistry letters, 19(15), 4110-4114 (2009-06-27)
Synthesis of a series of tetrahydrocarbazole amides with potent activity against human papillomaviruses is described. Synthetic approaches allowing for variation of the substitution pattern of the tetrahydrocarbazole and the amide are outlined and resulting changes in antiviral activity and certain
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