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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
3T3-L1 cells 25 μM Reverse the inhibitory effects of RAL on lipid droplets and adipogenic markers PMC6717377
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. PMC3809786
HUVECs 5 μM 2 h Inhibited Wnt/β-catenin signaling, reduced β-catenin nuclear translocation, thereby counteracting aFGF-mediated endothelial protection. PMC7772795
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. PMC8120464
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. PMC6704582
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. PMC6704582
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 PMC3858584
Neural Stem/Progenitor Cells (NSPCs) 10µM 4 days IWR-1 significantly inhibited the proliferative effect of MIF on NSPCs PMC3858584
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. PMC11304784
Rat primary hepatocytes 10 μM 0.5 h Blocked the effect of coronarin A on β-catenin phosphorylation and inhibited gluconeogenesis PMC9958036
Human lung endothelial cell (HLEC) 10 µM 24 h Restored HLEC tight-junction protein expression and inhibited prostate cancer cell transendothelial migration PMC5988746

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. PMC7772795
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. PMC6704582
Mice Breast cancer xenograft model Not specified 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. PMC11569202

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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