1. Stem Cell/Wnt Cell Cycle/DNA Damage
  2. β-catenin Wnt CDK
  3. 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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MCE 顾客使用本产品发表的 1 篇科研文献

  • 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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
SW480 IC50
1.35 μM
Compound: 65; C2
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
Antiproliferative activity against human SW480 cells assessed as inhibition of cell growth incubated for 72 hrs by alamar blue assay
[PMID: 36183504]
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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
β-catenin-IN-3
目录号:
HY-147007
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