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Merck

SML1824

Sigma-Aldrich

GSK983

≥98% (HPLC)

别名:

GSK260983, N-[(1R)-6-Chloro-2,3,4,9-tetrahydro-1H-carbazol-1-yl]-2-pyridinecarboxamide

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About This Item

经验公式(希尔记法):
C18H16ClN3O
分子量:
325.79
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.77

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.

象形圖

Exclamation mark

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


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GSK983: a novel compound with broad-spectrum antiviral activity.
Harvey R, et al.
Antiviral Research, 82(1), 1-11 (2009)
Richard M Deans et al.
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
Robert Harvey et al.
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.
Deans RM, et al.
Nature Chemical Biology, 12(5), 361-366 (2016)
Kristjan S Gudmundsson et al.
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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