化合物WAY-262611 T1971

Product Introduction
Bioactivity


英文名: WAY-262611

描述: WAY262611是一种 Wnt/β- 联蛋白激动剂，也是一种Dkk1的抑制剂。它能够增加骨形成速率，在 TCF- 荧光素酶测定实验中的EC50=0.63 μM。

激酶实验: 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).

体外活性: WAY-262611在初级检测中显示出了最强的活性、较低的激酶抑制潜力和高溶解性[1]。

体内活性: WAY-262611 has excellent pharmacokinetic properties and shows a increase in the trabecular bone formation rate in ovariectomized rats following oral administration in a dose-dependent manner. Calvariae from wt mice treated with WAY-262611 shows statistically increased BFR, but similarly treated KO animals are no different from control. This indicates that WAY-262611 is acting via the Wnt β-catenin pathway and most likely through inhibition of Dkk-1[1].

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

溶解度: DMSO : 42 mg/mL (131.90 mM)


关键字: Beta catenin | Inhibitor | β-catenin | WAY 262611 | WAY-262611 | inhibit | WAY262611

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