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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIWR-1Cat. No.: HY-12238CAS No.: 1127442-82-3Synonyms: endo-IWR 1; IWR-1-endo分式: CHNO分量: 409.44作靶点: Wnt作通路: Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 46 mg/mL (112.35 mM)*

2、 means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4424 mL 12.2118 mL 24.4236 mL5 mM 0.4885 mL 2.4424 mL 4.8847 mL10 mM 0.2442 mL 1.2212 mL 2.4424 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的

3、作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.11 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.11 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www

4、.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 IWR-1是端锚聚合酶抑制剂,抑制Wnt/-catenin信号传导途径。IC50 & Target IC50: 180 nM (Wnt)体外研究 Both IWR-1 and XAV939 act as reversible Wnt pathway inhibitors and exhibit similar pharmacological effectsin vitr

5、o. IWR-1 exerts its effect via interaction with Axin, while XAV939 binds TNKS directly 1. IWR-1 (10 M) induces stabilization of -catenin disruption complex. IWR-1 (10 M) is added to the medium together withMIF, the size of cell colonies is extremely decreased, and that indicates the promoting effect

6、 of MIF on NSPCproliferation is inhibited by IWR-1 in any MIF concentration group. 2, 5 and 10 M of IWR-1 significantlyinhibits the proliferation of NSPC dose-dependently. IWR-1 inhibites the promoting effect of MIF on NSPCdifferentiation to neuron lineage 2. IWR-1 treatment in the presence of maxim

7、al stimulatory dose of FSH(0.5 ng/mL) results in a dose dependent inhibition of the stimulatory effect of FSH with 75% inhibitionobserved at the maximal inhibitory dose of IWR-1 (1 M). IWR-1 treatment partially reverses the FSH-induced inhibition of granulosa cell CARTPT mRNA expression 3.户使本产品发表的科研

8、献 Cell Biosci. 2019 Jun. Oncol Rep. 2018 Aug;40(2):877-886. Cell Biol Int. 2017 May;41(5):534-543. Ren Fail. 2019 Nov;41(1):159-166. iScience. April.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lu J, et al. Structure-activity relationship studies of small-molecule inhibitors

9、 of Wnt response. Bioorg Med Chem Lett. 2009 Jul15;19(14):3825-7.2. Zhang X, et al. Macrophage migration inhibitory factor promotes proliferation and neuronal differentiation of neural stem/precursor cellsthrough Wnt/-catenin signal pathway. Int J Biol Sci. 2013 Nov 28;9(10):1108-20.3. Gupta PS, et al. Regulation and Regulatory Role of WNT Signaling in Potentiating FSH Action during Bovine Dominant FollicleSelection. PLoS One. 2014 Jun 17;9(6):e100201.McePdfHeightCaution: Product has not been fully validated f

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