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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-CMV-HCMV NEC inhibitor GK1
HCMV NEC inhibitor GK1

Chemical Structure : HCMV NEC inhibitor GK1

CAS No.: 1186662-25-8

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HCMV NEC inhibitor GK1 (WZ4140)

货号: PC-21357Not For Human Use, Lab Use Only.

HCMV NEC inhibitor GK1 is a small molecule inhibitor of HCMV nuclear egress complex (NEC) subunit interactions, interferes with the interaction of UL50 and UL53 with IC50 of 5.3 uM in HTRF assays, exerts selective antiviral activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HCMV NEC inhibitor GK1 is a small molecule inhibitor of HCMV nuclear egress complex (NEC) subunit interactions, interferes with the interaction of UL50 and UL53 with IC50 of 5.3 uM in HTRF assays, exerts selective antiviral activity.
GK1 does not show inhibition in an HTRF assay for interactions of mouse cytomegalovirus NEC subunits, and not show meaningful inhibition in the HSV-1 P30-UL42.
GK1 inhibits HCMV plaque formation with ED50 of 0.83 uM in human foreskin fibroblasts (HFFs), exhibits less potent anti-HSV-1 activity (ED50=11 uM).
GK1 inhibits late events in the viral replication cycle and modestly affect co-localization of UL50 and UL53.
The covalent interaction of GK1 with UL53 cysteine 214 (C214) is crucial for inhibition of NEC interactions in vitro, and UL53 cysteine 214 confers resistance to GK1.
The HCMV NEC is a virally encoded, two-subunit protein heterodimer, comprised of an INM-anchored subunit (UL50) and a nucleoplasmic subunit (UL53), which, based on work from other herpesviruses, forms higher order hexagonal arrays to promote budding.
HCMV NEC is crucial for viral replication and differs markedly from host proteins, important properties for an antiviral drug target.

物理化学性质&存储条件

分子量 313.74
分子式 C16H12ClN3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-((6-chloro-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)acrylamide

参考文献

1. Chen H, et al. PLoS Pathog. 2023 Nov 17;19(11):e1011781.

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