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Chemical Structure| 1127442-82-3 Chemical Structure| 1127442-82-3

Structure of IWR-1
CAS No.: 1127442-82-3

Chemical Structure| 1127442-82-3

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IWR-1 is a tankyrase inhibitor that inhibits the Wnt/β-catenin signaling pathway.

Synonyms: IWR-1-endo; endo-IWR 1

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Product Details of IWR-1

CAS No. :1127442-82-3
Formula : C25H19N3O3
M.W : 409.44
SMILES Code : 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
Synonyms :
IWR-1-endo; endo-IWR 1
MDL No. :MFCD18086875

Safety of IWR-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
iPSC-AETII cells 100 mM 7 days IWR-1 induced the differentiation of iPSC-AETII cells to the AETI cell phenotype, significantly increasing the expression of AETI markers AQ5, T1α, and caveolin-1. J Clin Invest. 2013 Nov;123(11):4950-62.
HUVECs 5 μM 2 h Inhibited Wnt/β-catenin signaling, reduced β-catenin nuclear translocation, thereby counteracting aFGF-mediated endothelial protection. Redox Biol. 2021 Feb;39:101811.
3T3-L1 cells 25 μM Reverse the inhibitory effects of RAL on lipid droplets and adipogenic markers J Biomed Sci. 2019 Aug 31;26(1):62.
CD44+CD133+ Caco-2 cells 4.0-64 µM 6 days To evaluate the anti-proliferative effects of IWR-1 on CD44+CD133+ Caco-2 cells. The results showed that IWR-1 significantly inhibited the proliferation and colony formation of CD44+CD133+ Caco-2 cells. Int J Biol Sci. 2021 Apr 12;17(7):1644-1659.
mouse primary hepatic cells 10 μM 3 h To investigate the effect of IWR-1 on ethanol-induced lipid accumulation in hepatic cells, results showed that IWR-1 reversed the inhibitory effect of parkin deficiency on lipid accumulation. Cell Commun Signal. 2019 Aug 22;17(1):104.
human hepatic cancer cell line HepG2 10 μM 3 h To investigate the effect of IWR-1 on β-catenin signaling in HepG2 cells, results showed that IWR-1 inhibited β-catenin ubiquitination. Cell Commun Signal. 2019 Aug 22;17(1):104.
Neural Stem/Progenitor Cells (NSPCs) 1µM or 10µM 7 days IWR-1 significantly inhibited the promoting effect of MIF on NSPC differentiation to neuron lineage Int J Biol Sci. 2013 Nov 28;9(10):1108-20.
Neural Stem/Progenitor Cells (NSPCs) 10µM 4 days IWR-1 significantly inhibited the proliferative effect of MIF on NSPCs Int J Biol Sci. 2013 Nov 28;9(10):1108-20.
Porcine embryonic stem cells 1.5 µM 10 days To evaluate the role of IWR-1 in establishing porcine embryonic stem cells, results showed that IWR-1 helps maintain self-renewal and proliferation capacity of stem cells. Stem Cell Res Ther. 2024 Aug 7;15(1):245.
rat primary hepatocytes 10 μM 0.5 h blocked the effect of coronarin A on β-catenin phosphorylation and inhibited gluconeogenesis Acta Pharmacol Sin. 2023 Mar;44(3):596-609.
human lung endothelial cell (HLEC) 10 µM 24 h restored HLEC tight-junction protein expression and inhibited prostate cancer cell transendothelial migration Br J Cancer. 2018 May;118(11):1464-1475.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Dbb mice Intraperitoneal injection 5 mg/kg Single injection Inhibited Wnt/β-catenin signaling, attenuated aFGF-mediated endothelial protection, manifested as increased aortic endothelial cell apoptosis and increased mitochondrial ROS generation. Redox Biol. 2021 Feb;39:101811.
Mice Parkin knockout mice Intraperitoneal injection 25 μM/kg Single injection To investigate the effect of IWR-1 on ethanol-induced hepatic lipid accumulation, results showed that IWR-1 reversed the inhibitory effect of parkin deficiency on hepatic lipid accumulation. Cell Commun Signal. 2019 Aug 22;17(1):104.
Mice Breast cancer xenograft model 5 mg/kg Every other day for 2 weeks The combination of IWR-1 with paclitaxel significantly suppressed breast cancer growth and enhanced the anti-tumor efficacy of paclitaxel. Cell Death Dis. 2024 Nov 16;15(11):835

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.42mL

4.88mL

2.44mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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