WAY-262611

Catalog No.S9828 Synonyms: BML-WN110

For research use only.

WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1).

WAY-262611 Chemical Structure

CAS No. 1123231-07-1

Purity & Quality Control

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Biological Activity

Description WAY-262611 (BML-WN110, Compound 5) is a beta-catenin (β-Catenin) agonist that increases bone formation rate with EC50 of 0.63 μM in TCF-Luciferase assay. WAY-262611 is also an inhibitor of dickkopf 1 (DKK1).
Targets
DKK1 [2]
()
β-Catenin [1]
(TCF-Luciferase assay)
0.63 μM(EC50)
In vitro

WAY-262611, the DKK1 inhibitor, blocks DKK1 and restores the GDF5 reduced MMP13 gene expression.[2]

In vivo

WAY-262611 has excellent pharmacokinetic properties and shows a dose dependent increase in the trabecular bone formation rate in ovariectomized rats following oral administration.[1]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: Surplus human chondrocytes
  • Concentrations: 0.01 μM, 0.1 μM, 1 μM
  • Incubation Time: 21 days
  • Method:

    Chondrocytes are resuspended at 1.25×106 cells/ml in basic differentiation media (BDM) consisting of DMEM high glucose supplemented with 100 nM dexamethasone, 1× insulin-transferrin-selenous acid premix (ITS), 1.0 mg/ml human serum albumin supplemented with 5.0 μg/ml linoleic acid, 14 μg/ml L-ascorbic acid 2-phosphate and 1× Penicilline-Streptomycin. The cell suspension is divided into aliquots of 200 μl to each well of an uncoated flat bottom 96-well plate. The plate is centrifuged at 1,500 rpm for 5 min and incubated for 48 h at 37°C in 5% CO2 and 90% relative humidity to allow for pellet formation. After 48 h the culture medium is changed to BDM supplemented with appropriate growth factors (GFs); 2, 10, 100 or 200 ng/ml recombinant GDF5, 50 ng/ml recombinant Wnt3a, 0.5 μM GSK3b inhibitor CHIR-99021, 0.01, 0.1 or 1 μM DKK1 inhibitor WAY-262611. Medium is changed three times per week for 21 days, whereafter the pellets are snap-frozen in liquid nitrogen and stored at -80°C.

Animal Research:

[1]

  • Animal Models: OVX rats
  • Dosages: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg; 2 mg/kg
  • Administration: Oral gavage; IV

Solubility (25°C)

In vitro

DMSO 64 mg/mL
(200.99 mM)
Water 10 mg/mL
(31.4 mM)
Ethanol '10 mg/mL

Chemical Information

Molecular Weight 318.42
Formula

C20H22N4

CAS No. 1123231-07-1
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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