IWP-2

CAS号

686770-61-6

分子式

C22H18N4O2S3

主要靶点

Casein Kinase|Wnt/beta-catenin|Porcupine

仅限科研使用

Cat No : CM06892

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Synonyms

betacatenin|beta-catenin|bcatenin|Casein Kinase|CaseinKinase|IWP 2|IWP2|IWP-2|Inhibitor|inhibit|Porcn|Porcupine|Wnt/β-catenin|Wnt/betacatenin|Wnt/b-catenin|Wnt|βcatenin



产品信息

CAS号 686770-61-6
分子式 C22H18N4O2S3
主要靶点 Casein Kinase|Wnt/beta-catenin|Porcupine
主要通路 代谢|干细胞|干细胞|干细胞|细胞骨架
分子量 466.6
纯度 99.76%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 betacatenin|beta-catenin|bcatenin|Casein Kinase|CaseinKinase|IWP 2|IWP2|IWP-2|Inhibitor|inhibit|Porcn|Porcupine|Wnt/β-catenin|Wnt/betacatenin|Wnt/b-catenin|Wnt|βcatenin

靶点活性

Wnt:27 nM

体内活性

方法: 为研究对脱发的作用,用 AA 抗氧化剂 (100 mg/mL,局部用于皮肤)、PBMT 和 IWP-2 (20 mg/kg,静脉注射,每两天一次) 治疗 C57/BL6 小鼠。 结果: 在休止期剃须刺激后,PBMT 促进了头发再生。重要的是,使用 AA 和 IWP-2 消除了 PBMT 在体内诱导的 HF 生长速率的差异。[3]

体外活性

方法: 人胃癌细胞 MKN28 用 IWP-2 (5-50 μM) 处理 1-5 天,通过 CellTiter Assay 检测细胞增殖。 结果: 在 MKN28 细胞系中治疗四天后,10-50 μM IWP-2 显著抑制了 MKN28 细胞的增殖。[1] 方法: L-Wnt3A 细胞用 IWP-2 (5 μM) 处理 24 h,通过 Western Blot 检测靶点蛋白表达水平。 结果: IWP-2 阻断了所有检测到的 Wnt 依赖性生化变化,Lrp6 受体和 Dvl2 的磷酸化,以及 β-catenin 的积累。[2]

溶解度

DMSO:4.67 mg/mL (10.01 mM)

细胞实验

IWP-2 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. The human RCC cell lines 786O and Caki-2 (5×103) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20 μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490 nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera[2].

参考文献

1.Mo ML, et al. Inhibition of the Wnt palmitoyltransferase porcupine suppresses cell growth and downregulates the Wnt/β-catenin pathway in gastric cancer. Oncol Lett. 2013 May;5(5):1719-1723.
2.Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.
3.Jin H, et al. Photobiomodulation therapy for hair regeneration: A synergetic activation of β-CATENIN in hair follicle stem cells by ROS and paracrine WNTs. Stem Cell Reports. 2021 Jun 8;16(6):1568-1583.

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