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CAS No.: 292168-79-7

KY1220 Catalog No. CSN20582

KY1220 inhibits Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 cells and it can destabilize both β-catenin and Ras.

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靶点选择性

生物活性

靶点 Wnt/β-catenin

IC50:2.1μM
描述Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Axin is a cytoplasmic protein which contains a regulation of G-protein signaling (RGS) domain and a dishevelled and axin (DIX) domain. Axin is a component of the β-catenin destruction complex required for regulating CTNNB1 levels through phosphorylation and ubiquitination, and modulating Wnt-signaling. In Wnt signaling, axin probably facilitates the phosphorylation of CTNNB1 and APC by GSK3B^[3]. KY1220 specifically binds to the RGS domain of Axin, activates GSK3β via a conformational change enhancing β-catenin complex assembly, and subsequently degrade both β-catenin and Ras via proteasomal degradation^[4]. The inhibitory IC₅₀ of KY1220 on the Wnt/β-catenin pathway was 2.1 μM, and in HEK293 cells, both β-catenin and pan-Ras protein levels were reduced in a dose-dependent manner after treatment with KY1220 at the concentration of 5~50 μM^[5]. The proliferation and transformation of HCT15, SW480, D-WT and D-MT colon cancer cells were efficiently inhibited after treatment with KY1220^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.1815 mL
- 15.9074 mL
- 31.8148 mL
- 5 mM
- 0.6363 mL
- 3.1815 mL
- 6.3630 mL
- 10 mM
- 0.3181 mL
- 1.5907 mL
- 3.1815 mL

技术信息

CAS号

292168-79-7

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H10N4O3S

运输

蓝冰

分子量

314.32

别名

溶解度

DMSO	63.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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工作液计算器 ✕

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