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

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.

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IWR-1 Chemical Structure

IWR-1 Chemical Structure

CAS No. : 1127442-82-3

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IWR-1 Related Antibodies

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Description

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].

In Vitro

IWR-1 (GMP) is cytotoxic for osteosarcoma cancer stem-like cells (CSCs)[1].
IWR-1 (GMP) suppresses cell migration, invasion, and matrix metalloproteinase activities of colorectal cancer cell lines[2].
IWR-1 (GMP) (2.5-10 μM, 48-96 h) is effective in reducing spheres’ viability in a concentration- and time- dependent manner in parental and spheres from MG-63 and MNNG-HOS cell lines[1].
IWR-1 (GMP) (10 μM, 96 h) increases the number of TUNEL-positive cells, reaching 4.65- and 15.83-fold differences relative to control at 96 h and promoted the activation of caspases 3/7 reaching 2.15- and 1.27-fold in MG-63 and MNNG-HOS spheres[1].
IWR-1 (GMP) (10 μM, 48 h) induces a cell cycle arrest in the G2/M phase in spheres derived from MG-63 and MNNG-HOS cell lines and increases the percentage of cells in the S phase slightly[1].
IWR-1 (GMP) (10 μM, 48 h) inhibits secondary sphere-forming efficacy by approximately 53% and 55% of the first-generation 7-day old spheres in MG-6t4 and MNNG-HOS cells[1].
IWR-1 (GMP) (5-50 μM, 24-48 h) decreases the proliferation of HCT116 cells in a dose- and time-dependent manner[2].
IWR-1 (GMP) (5-50 μM, 24-48 h) inhibits TNF-α-stimulated migration in HCT116 and HT29 cells[2].

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

IWR-1 Related Antibodies

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.
In Vivo

IWR-1 (5 mg/kg, intratumorally, each 2 d for 12 d) induces a marked inhibition of tumor growth in osteosarcoma mouse model[1].
IWR-1 (GMP) (10 mg/kg, s.c., on days 1, 3, 5) ameliorates IL-36γ (2 μg/mouse on days 1, 3, 5)-mediated exacerbation of psoriatic skin lesions in an Imiquimod (IMQ) (HY-B0180)-induced psoriasis-like mice model[3].

MedChemExpress (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.
Molecular Weight

409.44

Formula

C25H19N3O3
CAS No.
SMILES

O=C(NC1=C2N=CC=CC2=CC=C1)C3=CC=C(N(C([C@]4([H])[C@](C5)([H])C=C[C@]5([H])[C@]64[H])=O)C6=O)C=C3
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Purity & Documentation
References
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IWR-1 Related Classifications

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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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