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  4. IWR-1

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

目录号: HY-12238G
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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 通过增强 Axin 支架破坏复合物的稳定性来促进 β-catenin 磷酸化。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

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 promotes β-catenin phosphorylation by promoting stability of Axin-scaffolded destruction complexes. IWR-1 can be studied in research for anti-tumor purposes, and diseases such as osteosarcoma, colorectal cancer and psoriasis[1][2][4].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 GI50
> 100 μM
Compound: IWR1
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
[PMID: 24950489]
HEK-293T IC50
26 nM
Compound: 1, IWR-1
Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
[PMID: 22191557]
HEK293 IC50
136 μM
Compound: 1, IWR1
Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
[PMID: 23316926]
HT-29 GI50
> 100 μM
Compound: IWR1
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
[PMID: 24950489]
HT-29 IC50
24.4 μM
Compound: IWR1
Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control
Inhibition of Wnt signaling in human HT29 cells assessed as inhibition of beta-catenin-mediated Tcf/Lef transcriptional activity after 24 hrs by dual luciferase reporter gene assay relative to control
[PMID: 24950489]
HT-29 IC50
9.52 μM
Compound: IWR-1
Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method
Cytotoxicity against human HT-29 cells assessed as cell viability at 1.563 to 50 uM measured after 72 hrs by plate reader method
[PMID: 34062253]
HepG2 GI50
95.4 μM
Compound: IWR1
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 24950489]
LoVo GI50
63.1 μM
Compound: IWR1
Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay
Antiproliferative activity against human LoVo cells after 72 hrs by MTT assay
[PMID: 24950489]
SW480 EC50
2.5 μM
Compound: 1, IWR1
Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method
Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method
[PMID: 23701517]
SW480 IC50
0.25 μM
Compound: 1, IWR1
Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs
Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs
[PMID: 23701517]
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

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

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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