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WAY-262611

Catalog No. T1971 CAS 1123231-07-1

WAY262611 is a Wnt/β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay.

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WAY-262611, CAS 1123231-07-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 58.00
10 mg	In stock	$ 89.00
25 mg	In stock	$ 175.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 493.00
1 mL * 10 mM (in DMSO)	In stock	$ 64.00

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Purity: 99.27%

Purity: 99.09%

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Description	WAY262611 is a Wnt/β-catenin agonist and an inhibitor of Dkk1. It increases bone formation rate with EC50 of 0.63 μM in TCF-luciferase assay.
Targets&IC50	β-catenin (TCF-Luciferase assay):0.63 μM
In vitro	WAY-262611 has the most potent activity, low kinase inhibition potential, and high solubility in the primary assay[1].
In vivo	WAY-262611 exhibits exceptional pharmacokinetic properties and, upon oral administration, demonstrates a dose-dependent increase in trabecular bone formation in ovariectomized rats. Calvariae from wild-type mice treated with WAY-262611 display significantly increased bone formation rates (BFR), whereas knockout (KO) animals treated in the same manner show no difference from control, suggesting that WAY-262611 operates through the Wnt β-catenin pathway, likely via inhibition of Dkk-1[1].
Kinase Assay	PI3K and mTOR kinase assay : Enzyme assays are done in fluorescent polarization (FP) format, adapted from the Echelon K-1100 PI3K FP assay kit protocol. Human class I PI3Ks and PI3K-α mutants (E545K and H1047R) are produced in Sf9 or purchased from Upstate Biotech. GST-GRP1 (murine) is produced in Escherichia coli and isolated by GST-Sepharose. Assay buffers are reaction buffer [20 mM HEPES (pH 7.1), 2 mM MgCl2, 0.05% CHAPS, and 0.01% β-mercaptoethanol] and stop/detection buffer [100 mM HEPES (pH 7.5), 4 mM EDTA, 0.05% CHAPS]. FP reaction is run for 30 minutes at room temperature in 20 μL of reaction buffer containing 20 μM phosphatidylinositol 4,5-bisphosphate (PIP2), 25 μM ATP, and <4% DMSO. FP reaction is stopped with 20 μL of stop/detection buffer (10 nM probe and 40 nM GST-GRP), and after 2 hours, data are collected using an Envision plate reader. The routine assays with purified FLAG-TOR (FL and 3.5) are performed in 96-well plates as follows. Enzymes are first diluted in kinase assay buffer (10 mM Hepes (pH 7.4), 50 mM NaCl, 50 mM β-glycerophosphate, 10 mM MnCl2, 0.5 mM DTT, 0.25 μM microcystin LR, and 100 μg/mL BSA). To each well, 12 μL of the diluted enzyme is mixed briefly with 0.5 μL test inhibitor or control vehicle dimethyl sulfoxide (DMSO). The kinase reaction is initiated by adding 12.5 μL kinase assay buffer containing ATP and His6-S6K to give a final reaction volume of 25 μL containing 800 ng/mL FLAG-TOR, 100 μM ATP, and 1.25 μM His6-S6K. The reaction plate is incubated for 2 hours (linear at 1–6 hours) at room temperature with gentle shaking and then terminated by adding 25 μL Stop buffer (20 mM Hepes (pH 7.4), 20 mM EDTA, and 20 mM EGTA).

Molecular Weight	318.42
Formula	C20H22N4
CAS No.	1123231-07-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 42 mg/mL (131.90 mM)

References and Literature

1. Pelletier JC, et al. (1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate. J Med Chem. 2009 Nov 26;52(22):6962-5.

Citations

1. Wu M, Zhang X, Zhang W, et al. Cancer Stem Cell Regulated Phenotypic Plasticity Protects Metastasized Cancer Cells from Ferroptosis. Nature Communications. 2022, 13(1): 1-16.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Neural Regeneration Compound Library Wnt/Hedgehog/Notch Compound Library Anti-Cancer Compound Library Anti-Ovarian Cancer Compound Library Stem Cell Differentiation Compound Library Bioactive Compounds Library Max Cytoskeletal Signaling Pathway Compound Library Cancer Cell Differentiation Compound Library Anti-Aging Compound Library

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Keywords

WAY-262611 1123231-07-1 Cytoskeletal Signaling Stem Cells Wnt/beta-catenin Beta catenin Inhibitor β-catenin WAY 262611 inhibit WAY262611 inhibitor

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