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WAY-262611

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Chemical Structure| 1123231-07-1 同义名 : BML-WN110;Dkk1 Inhibitor;WAY-262611 dihydrochloride WAY 262611 dihydrochloride;WAY 262611 dihydrochloride;WAY262611 2HCl;Dickkopf-1 Inhibitor
CAS号 : 1123231-07-1
货号 : A318831
分子式 : C20H22N4
纯度 : 98%
分子量 : 318.416
MDL号 : MFCD20527803
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(125.62 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Dkk-1, short for Dickkopf-related protein 1, is a soluble extracellular protein which antagonizes canonical Wnt signaling[3]. Dkk-1 plays an important role in vertebrate development. In the adult, Dkk-1 is implicated in bone formation and bone disease, cancer and Alzheimer disease[4]. WAY-262611 is a Dkk-1 inhibitor. The EC50 of WAY-262611 in potentiating a TCF-luciferase response was 0.63 μM[5]. In a wound scratch assay, fibroblast-like synoviocytes treated by 5 μM WAY-262611 showed significant attenuated migration compared with the control group in a time-dependent manner[6]. WAY-262611 was orally dosed daily for 28 days at the doses of 0.3, 1, 3, 10 mg/kg in an ovariectomized rat model. WAY-262611 dose dependently increased trabecular bone formation rate in the tibia of the animals and activity was observed at the low dose of 0.3 mg/kg[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.14mL

0.63mL

0.31mL

15.70mL

3.14mL

1.57mL

31.41mL

6.28mL

3.14mL
参考文献

[1]Enochson L, Stenberg J, et al. GDF5 reduces MMP13 expression in human chondrocytes via DKK1 mediated canonical Wnt signaling inhibition. Osteoarthritis Cartilage. 2014 Apr;22(4):566-77.

[2]Pelletier JC, Lundquist JT 4th, 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.

[3]Ahn VE, Chu ML, Choi HJ, Tran D, Abo A, Weis WI. Structural basis of Wnt signaling inhibition by Dickkopf binding to LRP5/6. Dev Cell. 2011 Nov 15;21(5):862-73. doi: 10.1016/j.devcel.2011.09.003. Epub 2011 Oct 13. PMID: 22000856; PMCID: PMC3215855.

[4]Niehrs C. Function and biological roles of the Dickkopf family of Wnt modulators. Oncogene. 2006 Dec 4;25(57):7469-81. doi: 10.1038/sj.onc.1210054. PMID: 17143291.

[5]Pelletier JC, Lundquist JT 4th, Gilbert AM, Alon N, Bex FJ, Bhat BM, Bursavich MG, Coleburn VE, Felix LA, Green DM, Green P, Hauze DB, Kharode YP, Lam HS, Lockhead SR, Magolda RL, Matteo JJ, Mehlmann JF, Milligan C, Murrills RJ, Pirrello J, Selim S, Sharp MC, Unwalla RJ, Vera MD, Wrobel JE, Yaworsky P, Bodine PV. (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. doi: 10.1021/jm9014197. PMID: 19856966.

[6]Choe JY, Hun Kim J, Park KY, Choi CH, Kim SK. Activation of dickkopf-1 and focal adhesion kinase pathway by tumour necrosis factor α induces enhanced migration of fibroblast-like synoviocytes in rheumatoid arthritis. Rheumatology (Oxford). 2016 May;55(5):928-38. doi: 10.1093/rheumatology/kev422. Epub 2015 Dec 29. PMID: 26715774.