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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-E3 Ubiquitin Ligase-GS143
GS143

Chemical Structure : GS143

CAS No.: 916232-21-8

GS143 (GS-143)

货号: PC-24524Not For Human Use, Lab Use Only.

GS143 is a specific small molecule inhibitor of E3 ligase β-TrCP, exhibits potent latency reversing agent (LRA) activity, also is a NF-kappaB signaling inhibitor, inhibits IκBα ubiquitylation (IC50=5.2 uM).

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25 mg ¥1180 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

GS143 is a specific small molecule inhibitor of E3 ligase β-TrCP, exhibits potent latency reversing agent (LRA) activity, also is a NF-kappaB signaling inhibitor, inhibits IκBα ubiquitylation (IC50=5.2 uM).
GS143 selectively inhibits IκBα ubiquitination inhibitor withIC50 of 5.2 uM for SCF βTrCP1-mediated IκBα ubiquitylation.
GS143 displays potent LRA activity in a primary cell model of HIV-1 latency.
GS143 triggers a novel signaling pathway to reactivate latent HIV-1 that leads to the unconventional activation of NFκB p65, by initiating the noncanonical signaling via NIK, followed by activation of IKK leading to phosphorylation of p65 on S536 and its nuclear translocation.

物理化学性质&存储条件

分子量 466.47
分子式 C28H19FN2O4
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

4-(3-Benzyl-4-{[5-(2-fluorophenyl)furan-2-yl]methylidene}-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid

参考文献

1. Sarkar S, et al. PLoS Pathog. 2025 Apr 1;21(4):e1013018.

2. Nakajima H, et al. Biochem Biophys Res Commun. 2008;368(4):1007–13.

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