Enzymes for Research, Diagnostic and Industrial Use

WAY 316606

Cat No.
Product Overview
WAY 316606 is a selective small-molecule inhibitor of secreted frizzled-related protein-1 (sFRP-1) with EC50 value of 0.65 μM. The Wnt signaling has been proved to be a drug target of treatment for metabolic bone diseases such as osteoporosis. The studies found that loss-of-function mutations of Wnt antagonists caused increased bone formation and deletion of the Wnt antagonist sFRP-1 resulted in increased trabecular bone formation in aged mice. Thus small-molecule inhibitors of Wnt antagonist (sFRP-1) have been discovered and developed. WAY 316606 was screened out from a library of over 440,000 compounds by the cell-based assay measuring activation of Wnt signaling. It bound to sFRP-1 preferentially (Kd value of 0.08 μM) and inhibited the negative regulation of Wnt caused by sFRP-1.WAY 316606 has been proved to promote bone formation in an organ culture assay. WAY 316606 is a selective inhibitor of sFRP-1. It bound to sFRP-2 with 10-fold weaker affinity (Kd value of 1 μM). In a fluorescence polarization binding assay, WAY 316606 inhibited sFRP-1 with IC50 value of 0.5 μM. Although sequence of sFRP-1,-2 and-5 showed high identity, WAY 316606 selectively inhibited sFRP-1 against other two proteins. In the osteosarcoma U2-OS cell line used in a cell-based transient transfection and luciferase reporter assay, treatment of WAY 316606 dose-dependently increased Wnt-signaling with EC50 value of 0.65 μM. In an ex vivo assay using neonatal murine calvarium, treatment of WAY 316606 dose-dependently enhanced the osteoblast activity and stimulated bone formation up to 60% with EC50 value of 1 nM. Although WAY 316606 had good aqueous solubility and good stability, WAY 316606 exerted high plasma clearance (77 mL/min/kg) in rats, which suppressed sustained exposure and limited the compounds advancement as an orally administered anabolic bone agent.
Molecular Weight
Store at -20°C
WAY-316606; WAY316606
Molecular Formula
Chemical Name
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
Download Datasheet:

Online Inquiry
*E-mail Address:
Country or Region:
*Products or Services Interested:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy  Terms and Conditions
Copyright ©2011 - 2018 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Tel: 1-631-562-8517 1-516-512-3133
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country:
Click unfold / close
Inquiry Basket
Delete selected Check Out
Decide to move out of the shopping cart??

Sure No, Back

Please choose product!

< Go Back
You have already added to buy this product