| WAY 316606 HClsFRP-1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.58%
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Chemical structure
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| Cas No. | N/A | SDF | Download SDF |
| Synonyms | WAY-316606 HCl;WAY316606 HCl | ||
| Chemical Name | 5-(phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide hydrochloride | ||
| Canonical SMILES | O=S(NC1CCNCC1)(C2=C(C(F)(F)F)C=CC(S(=O)(C3=CC=CC=C3)=O)=C2)=O.Cl | ||
| Formula | C18H19F3N2O4S2.HCI | M.Wt | 484.94 |
| Solubility | ≥24.25mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
WAY 316606 is a selective small-molecule inhibitor of secreted frizzled-related protein-1 (sFRP-1) with EC50 value of 0.65 μM [1].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 [1].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 [1 and 2]. 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 compound"s advancement as an orally administered anabolic bone agent [1]. References:[1] Bodine P V N, Stauffer B, Ponce-de-Leon H, et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone, 2009, 44(6): 1063-1068.[2] Moore W J, Kern J C, Bhat R, et al. Modulation of Wnt Signaling Through Inhibition of Secreted Frizzled-Related Protein I (sFRP-1) with N-Substituted Piperidinyl Diphenylsulfonyl Sulfonamides†. Journal of medicinal chemistry, 2008, 52(1): 105-116.
