2. Stem Cell/Wnt Cell Cycle/DNA Damage
  3. β-catenin Wnt CDK
  4. β-catenin-IN-3

β-catenin-IN-3 (Compound C2) 是一种选择性 β-catenin 抑制剂。β-catenin-IN-3 与 β-catenin 表面的新型变构位点结合， KD 值为 54.96 nM。 β-catenin-IN-3 通过靶向隐蔽的变构调节位点选择性地抑制 β-catenin， 降低其细胞负荷。 β-catenin-IN-3 显著降低 β-catenin 驱动的癌细胞的活力，在 β-catenin 过表达癌细胞中通过蛋白酶体系统触发其降解。

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β-catenin-IN-3

β-catenin-IN-3 Chemical Structure

CAS No. : 1005288-15-2

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β-catenin-IN-3 相关抗体

Top Publications Citing Use of Products

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells[1].

IC50 & Target[1]

Cdk4/cyclin D1

 

体外研究
(In Vitro)

β-catenin-IN-3 (24 h)以剂量依赖性方式降低 DLD1，SW480，HCT116，SW48，MCF10A 和 H460 细胞的活力，IC50s为 0.85 μM、1.35 μM、5.35 μM、3.45 μM 和 20 μM 以上。[1]。
β-catenin-IN-3 (1 μM，3 μM，7 天) 抑制 DLD1 和 SW48 细胞的集落形成能力。[1]。
β-catenin-IN-3 (0，1，5 μM，24 h) 以剂量依赖的方式选择性抑制 DLD1 和 SW480 细胞中 β-catenin、 Axin1、 CyclinD1 和 TCF4 的水平[1]。
β-catenin-IN-3 (1 μM，3 h) 在 DLD1 细胞中通过泛素-蛋白酶体机制触发 β-catenin 的降解，可能是通过募集 APC 介导的破坏复合物[1]。
β-catenin-IN-3 (1 μM，1-24 h) 增加 DLD1 细胞中 β-catenin 的磷酸化[1] 。
β-catenin-IN-3 (1，5 μM，24 h) 分别降低了细胞核和细胞质中的 β-catenin 45%，40%，85% 和 55%[1]。
β-catenin-IN-3 (3，5 μM， 4 天) 抑制 APC 缺陷类器官克隆形成能力约 70% 和 55%，相反，野生型类器官的存活率为90%[1] 。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

β-catenin-IN-3 相关抗体:

Cell Viability Assay[1]

Cell Line: DLD1,SW4808, HCT116, SW48, MCF10A, H460 cells
Concentration: 10 nM-100 μM
Incubation Time: 24 h
Result: Reduced viability of DLD1 and SW480 cells in dose-dependent manner with IC50s of 0.85 μM and 1.35 μM.
Reduced viability of HCT116 and SW48 cells in dose-dependent manner with IC50s of 5.35 μM and 3.45 μM.
Impacted two WNT-independent cell lines, MCF10A and H460, with IC50 above 20μM.

Western Blot Analysis[1]

Cell Line: DLD1 cells
Concentration: 1μM
Incubation Time: 1,3,6,12,24 h
Result: Phosphorylated β-catenin starting at 1 hour point, which was further amplified to 2-2.5-fold at 12 and 24 hour points, and can be blocked by CHIR99021 (HY-10182).
Levels of active β-catenin markedly reduced at these time points, and can be arrested by MG132 (HY-13259).

Immunofluorescence[1]

Cell Line: DLD1 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Reduced β-catenin that co-localized with nucleic acids inside the nucleus by 55-60% (co-localization dropped from 0.62 to 0.25).
体内研究
(In Vivo)
分子量

484.25

Formula

C19H20Br2N2OS
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

纯度 & 产品资料
参考文献

β-catenin-IN-3 相关分类

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Keywords:

β-catenin-IN-31005288-15-2β-cateninWntCDKBeta cateninCyclin dependent kinaseAnticancerWnt pathwayβ-catenin-driven cancer cellstherapeutic targetingInhibitorinhibitorinhibit

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