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首页-小分子抑制剂&激动剂-NF-κB Pathway-IκB kinase (IKK)-LIB3S0280
LIB3S0280

Chemical Structure : LIB3S0280

CAS No.:

LIB3S0280

货号: PC-23440Not For Human Use, Lab Use Only.

LIB3S0280 is a potent TANK-binding kinase 1 (TBK1) inhibitor with IC50 of 493.9 nM, inhibits TBK1 downstream signaling.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LIB3S0280 is a potent TANK-binding kinase 1 (TBK1) inhibitor with IC50 of 493.9 nM, inhibits TBK1 downstream signaling.
LIB3S0280 suppresses pancreatic cancer growth and exert cytotoxic effects on high TBK1-expressing pancreatic cancer cells (MIA PaCa-2, MTT IC50=7.5 uM, 72h).
LIB3S0280 decreases phosphorylation of IκBα, phosphorylation level of AKT on the ser473 in pancreatic cancer cell lines.
LIB3S0280 treatment (96 h), the KRAS G12D-mutant pancreatic cancer cell line (PANC-1) exhibited a GI50 value of 4.71 μM and an IC50 value of 10.98 μM, while the KRAS G12C-mutant pancreatic cancer cell line (MIA PaCa-2) showed a GI50 value of 2.24 μM and an IC50 value of 6.64 μM.
LIB3S0280 treatment leads to G2/M arrest and induces apoptosis in pancreatic cancer cells, increases the granularity of pancreatic cells.

物理化学性质&存储条件

分子量 460.92
分子式 C22H25ClN4O5
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-(2-((5-chloro-2-((3,4,5-trimethoxyphenyl)amino)pyrimidin-4-yl)amino)ethyl)-2-methoxyphenol

参考文献

1. Wan-Hsi Shih, et al. Int J Biol Macromol. 2024 Nov 6:137296.

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