2. Stem Cell/Wnt
  3. Organoid Wnt
  4. IWR-1

IWR-1  (Synonyms: endo-IWR 1; IWR-1-endo)

目录号: HY-12238G
产品使用指南 技术支持

IWR-1 (IWR-1-endo) (GMP) 是 GMP 级别的 IWR-1 (HY-12238)。GMP 级别的小分子可用做细胞疗法中的辅助试剂。IWR-1 (IWR-1-endo) 是一种靶向 Wnt/β-catenin 的 tankyrase 抑制剂 (IC50 = 180 nM)。IWR-1 参与经典 Wnt 信号转导的关键步骤，即 β-catenin 转位至细胞核，随后激活 TCF/LEF 并表达 Wnt/β-catenin 下游靶标。IWR-1 诱导 Axin 蛋白水平升高，同时伴随 β-catenin 水平升高。IWR-1 可用于抗肿瘤研究，以及骨肉瘤、结直肠癌和牛皮癣等疾病的研究。

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IWR-1 Chemical Structure

IWR-1 Chemical Structure

CAS No. : 1127442-82-3

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IWR-1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IWR-1 (IWR-1-endo) (GMP) is the IWR-1 (HY-12238) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. IWR-1 (IWR-1-endo) is a tankyrase inhibitor targeting Wnt/β-catenin (IC50 = 180 nM). IWR-1 compromises critical steps of the canonical Wnt signaling, namely translocation of β-catenin to the nucleus and subsequent TCF/LEF activation and expression of Wnt/β-catenin downstream targets. IWR-1 induces increase in Axin protein levels accompanied by elevated levels of β-catenin. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis[1][2][4].

体外研究
(In Vitro)

IWR-1 (GMP) 对骨肉瘤癌干细胞样细胞 (CSC) 具有细胞毒性[1]。
IWR-1 (GMP) 可抑制结直肠癌细胞系的细胞迁移、侵袭和基质金属蛋白酶活性[2]。
IWR-1 (GMP) (2.5-10 μM，48-96 小时) 能够有效降低 MG-63 和 MNNG-HOS 细胞系来源的细胞球以及亲本细胞球中的细胞球活力，且这种降低呈浓度和时间依赖性[1]。
IWR-1 (GMP) (10 μM，96 小时) 可增加 TUNEL 阳性细胞的数量，在 96 小时时与对照组相比分别增加 4.65 倍和 15.83 倍，并促进 caspases 3/7 的活化，在 MG-63 和 MNNG-HOS 细胞球中分别增加 2.15 倍和 1.27 倍[1]。
IWR-1 (GMP) (10 μM，48 小时) 可诱导 MG-63 和 MNNG-HOS 细胞系来源的细胞球细胞周期停滞在 G2/M 期，并增加 S 期细胞占比[1]。
IWR-1 (GMP) (10 μM，48 小时) 可抑制 MG-6t4 和 MNNG-HOS 细胞中第一代 7 天龄球体的次级球体形成率，分别约为 53% 和 55%[1]。
IWR-1 (GMP) (5-50 μM，24-48 小时) 以剂量和时间依赖性方式降低 HCT116 细胞的增殖[2]。
IWR-1 (GMP) (5-50 μM，24-48 小时) 可抑制 TNF-α 刺激的 HCT116 和 HT29 细胞迁移[2]。

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

IWR-1 相关抗体:

Cell Viability Assay[1]

Cell Line: MG-63 and MNNG-HOS spheres and parent cells
Concentration: 2.5, 5, 7.5, 10 μM
Incubation Time: 48 and 96 h
Result: Reduced cell viability when concentration is higher than 5 μM.
Elicited more than 70% reduction of cell viability in spheres derived from the two cell lines at 96 h with 10 μM.
Had minimal effect on parental cells since the Wnt/β-catenin signaling is absent in these cells. Increased the susceptibility of spheres towards Doxorubicin (HY-15142) when treated in combination with increasing concentrations of Doxorubicin (0.01-100 μM).

Western Blot Analysis[1]

Cell Line: MG-63 and MNNG-HOS spheres and parent cells
Concentration: 10 μM
Incubation Time: 96 h
Result: Led to an upregulation of Bak and a downregulation of Bcl-2 (key proteins involved in mitochondrial-dependent apoptosis), which contributes to a Bak/Bcl-2 ratio >1 that prone the cells to undergo apoptosis.

RT-PCR[1]

Cell Line: MG-63 and MNNG-HOS spheres and parent cells
Concentration: 10 μM
Incubation Time: 96 h
Result: Led to an upregulation of Bak and a downregulation of Bcl-2 (key proteins involved in mitochondrial-dependent apoptosis), which contributes to a Bak/Bcl-2 ratio >1 that prone the cells to undergo apoptosis.
Results in a higher β-catenin nuclear/cytoplasmic ratio in spheres, indicating an increased Wnt/β-catenin pathway activation in osteosarcoma spheres.
Stabilized Axin2 protein levels.
Diminished the protein expression levels of Cyclin D1 in both parental cells and spheres.

Western Blot Analysis[2]

Cell Line: HCT116 cells
Concentration: 5, 10, 20, 50 μM
Incubation Time: 0, 4, 8, 24, 48 h
Result: Increased the levels of the epithelial marker E-cadherin whilst decreased the mesenchymal markers N-cadherin, Vimentin, and Snail dose- and time-dependently.
Inhibited the EMT process in HCT116 cells effectively.
Decreased β-catenin expression and inhibited the EMT-like expressional changes whereby decreasing N-cadherin and Snail and increasing E-cadherin expressions, even in the presence of TNF-α (HY-P1860) (10 ng/mL for 24 h)-induced EMT stimulation.
Decreased the phosphorylation of Akt in a concentration- and time-dependent manner.
Decreased the surviving expression in a concentration- and time-dependent manner, thereby promoting tumor proliferation directly or indirectly through regulating cancer cell homeostasis.
Reduced MMP activities only when surviving was suppressed.
体内研究
(In Vivo)

IWR-1 (GMP) (5 mg/kg，瘤内注射，每天两次，共注射 12 天) 可显著抑制骨肉瘤小鼠模型中的肿瘤生长[1]。
IWR-1 (GMP) (10 mg/kg，皮下注射，第 1、3、5 天) 可改善 Imiquimod (HY-B0180) 诱发的银屑病样小鼠模型中 IL-36γ (2 μg/只小鼠，第 1、3、5 天) 介导的银屑病皮肤病变加重[3]。

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

Animal Model: Immunocompromised nude mice (6-week old female Swiss nude) were injected sub-cutaneously the pGL4-transfected MNNG-HOS cells (2×106 cells/100 mL PBS)[1]
Dosage: 5 mg/kg
Administration: Intratumorally, each 2 d for 12 d
Result: Resulted in slower tumor growth rate and reduction in tumor size by 73% and 71% in comparison to control and to Doxorubicin-treated (8 mg/kg, i.p., each 4 d for 12 d) groups.
Enhanced the therapeutic efficacy of Doxorubicin shown by a greater reduction of tumor burden at the end of the treatment in opposite to Doxorubicin alone.
Animal Model: Balb/c mice (aged 6-8 weeks) with shaven back and treated with a daily topical dose of IMQ cream[3]
Dosage: 10 mg/kg
Administration: Subcutaneous injection (s.c.) on days 1, 3, 5
Result: Increased epidermal thickening with keratinocyte thickness.
Significantly diminished the effect of IMQ on hyperplasia in the IMQ+IWR-1 group.
Ameliorated the pathological changes in IL-36γ-induced psoriasiform skin lesion.
Reversed IL-36γ-mediated upregulation of inflammatory factors (IL-17 A and IFN-γ) in psoriatic lesions.
Reversed IL-36γ-mediated upregulation of β-catenin and DKK1 expression.
分子量

409.44

同用名

endo-IWR 1; IWR-1-endo

Formula

C25H19N3O3
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

IWR-1 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

IWR-1 (GMP)1127442-82-3endo-IWR 1 (GMP)IWR-1-endo (GMP)OrganoidWntInhibitorinhibitorinhibit

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