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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-WS-384
WS-384

Chemical Structure : WS-384

CAS No.: 2247544-03-0

WS-384 (WS384)

货号: PC-21875Not For Human Use, Lab Use Only.

WS-384 is a specific, small-molecule inhibitor dually targeting LSD1 (IC50=338.8 nM) and the DCN1-UBC12 interaction (IC50=14.8 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

WS-384 is a specific, small-molecule inhibitor dually targeting LSD1 (IC50=338.8 nM) and the DCN1-UBC12 interaction (IC50=14.8 uM).
WS-384 blocks the neddylation of cullin1 and cullin3 but had no effect on the neddylation of other cullin members in NSCLC cell, increases the levels of p21 and total level of all three isoforms of Bim (substrates of cullin 1) and NRF-2 (substrate of cullin 3).
WS-384 inhibits histone demethylation of NSCLC cells.
WS-384 inhibits cell proliferation and induced cell apoptosis in a concentration-dependent manner in A549 and H1975 cells with IC50 of 6.67 uM and 2.23 uM (24h), respectively.
WS-384 induced cell cycle arrest in A549 and H1975 cells.
WS-384 25 mg/kg and 50 mg/kg by oral administration suppresses tumor growth in A549 xenografts.

物理化学性质&存储条件

分子量 542.90
分子式 C18H21BrClN9S2
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

2-(5-((2-((4-bromobenzyl)thio)-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)thio)-1H-tetrazol-1-yl)-N,N-dimethylethan-1-amine hydrochloride

参考文献

1. Anqi Li, et al. Biomed Pharmacother. 2024 Feb 23:173:116240.

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