WAY-262611

Catalog No.S9828 Batch:S982801

Technical Data

Formula	C₂₀H₂₂N₄
Molecular Weight	318.42	CAS No.	1123231-07-1
Solubility (25°C)*	In vitro	DMSO	64 mg/mL (200.99 mM)
		Water	10 mg/mL (31.4 mM)
		Ethanol	10 mg/mL (31.4 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[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

Cell Assay:^{^[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 Study:^{^[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

References

Selleck's WAY-262611 has been cited by 2 publications

Decreased expression of GEM in osteoarthritis cartilage regulates chondrogenic differentiation via Wnt/β-catenin signaling [ J Orthop Surg Res, 2023, 18(1):751]	PubMed: 37794464
Osteoblast/osteocyte-derived interleukin-11 regulates osteogenesis and systemic adipogenesis [ Nat Commun, 2022, 13(1):7194]	PubMed: 36424386

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.