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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-STAT-WZ-2-033
WZ-2-033

Chemical Structure : WZ-2-033

CAS No.: 2416196-47-7

WZ-2-033

货号: PC-21874Not For Human Use, Lab Use Only.

WZ-2-033 is a potent, selective STAT3 inhibitor, binds to the SH2 domain of the STAT3 protein with KD of 7.4 uM, disrupts STAT3 dimerization and significantly inhibits STAT3 signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

WZ-2-033 is a potent, selective STAT3 inhibitor, binds to the SH2 domain of the STAT3 protein with KD of 7.4 uM, disrupts STAT3 dimerization and significantly inhibits STAT3 signaling.
WZ-2-033 preferentially suppresses STAT3-DNA binding, with no obvious effect on STAT5-DNA-binding activity.
WZ-2-033 suppresses STAT3-dependent transcriptional activation, reduces tyrosine (Y705) phosphorylation level of STAT3 in HEK-293T cells, inhibits the expression of STAT3 downstream genes, including Bcl-2, Bcl-xL, and c-Myc, in TNBC and GC cells.
WZ-2-033 strongly suppresses the proliferation, colony survival, migration, and invasion of TNBC and GC cells with aberrantly active STAT3.
WZ-2-033 (5 or 15 mg/kg, i.p. per day) inhibits tumor growth in MGC-803 xenograft mice, significantly suppresses the level of pY705-STAT3 and subsequently downregulated the expression of STAT3-targeted genes in human TNBC cell xenografts.

物理化学性质&存储条件

分子量 513.49
分子式 C25H18F3N3O4S
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-(1,1-dioxidobenzo[b]thiophen-6-yl)-2-(7-methoxy-2-(4-(trifluoromethyl)phenyl)imidazo[1,2-a]pyridin-3-yl)acetamide

参考文献

1. Yan Zhong, et al. Acta Pharmacol Sin. 2022 Apr;43(4):1013-1023.

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