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IWR-1-endo

Catalog No.
B2306
Potent Wnt signaling inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
10mg
$70.00
In stock
25mg
$150.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IWR-1-endo is a small molecule inhibitor of Wnt Response with IC50 value of 180nM [1].

IWR-1-endo is a small molecule antagonists of the Wnt/β-catenin pathway screened out from a diverse synthetic chemical library. It acts as an inhibitor of Wnt response. IWR-1-endo can inhibit the activity of Wnt1, 2 and 3. In cultured cells, IWR-1-endo inhibits Wnt-induced β-catenin accumulation which is a downstream event of Lrp6 and Dvl2. It is proved that IWR-1-endo promote β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo is also shown to inhibit tailfin regeneration and epithelial stem cell self-renewal in zebrafish. These two processes are both dependent on Wnt/β-catenin signaling. Furthermore, IWR-1-endo can block aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss [1].

References:
[1] Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt409.44
Cas No.1127442-82-3
FormulaC25H19N3O3
Solubilityinsoluble in EtOH; insoluble in H2O; ≥20.45 mg/mL in DMSO
Chemical Name4-((3aR,4S,7R,7aS)-1,3-dioxo-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindol-2(3H)-yl)-N-(quinolin-8-yl)benzamide
SDFDownload SDF
Canonical SMILESO=C([[email protected]@]1([H])[[email protected]]2([H])[[email protected]]3([H])C([H])([H])[[email protected]@]1([H])C([H])=C3[H])N(C4=C([H])C([H])=C(C(N([H])C5=C([H])C([H])=C([H])C6=C5N=C([H])C([H])=C6[H])=O)C([H])=C4[H])C2=O
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1]:

Cell lines

DLD-1 colorectal cancer (CRC) cell line

Preparation method

The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM, 2.5 μM, 10 μM

Applications

IWR-1-endo promoted β-catenin destruction through promoting stability of Axin-scaffolded destruction complexes in the DLD-1 colorectal cancer (CRC) cell line. IWR-1-endo blocked aberrant cell growth supported by hyperactivation of Wnt/β-catenin resulting from Apc loss.

Animal experiment [1]:

Animal models

Zebrafish

Dosage form

10 mM, 24 h

Application

IWR-1-endo inhibited tailfin regeneration and epithelial stem cell self-renewal in zebrafish.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

Biological Activity

Description IWR-1-endo is a potent inhibitor of Wnt signaling with IC50 value of 180 nM.
Targets Wnt signaling          
IC50 180 nM          

Quality Control

Chemical structure

IWR-1-endo

Related Biological Data

IWR-1-endo

Related Biological Data

IWR-1-endo