IWR-1-endo (Synonyms: endo-IWR 1; IWR-1-endo) |
| カタログ番号GC10950 |
IWR-1-endoは、Wnt/β-カテニンシグナル伝達経路を抑制するタンキラーゼ阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1127442-82-3
Sample solution is provided at 25 µL, 10mM.
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IWR-1-endo is a potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response with an IC50 value of 180 nM. IWR-1-endo induces Axin2 protein levels and promotes β-catenin phosphorylation by stabilizing the Axin scaffold destruction complex[1].
IWR-1-endo (10 µM; 1h) attenuated the protective effect of Intermedin/adrenomedullin-2, inhibited cell motility and the number of migrating cells [2]; IWR-1-endo (0.2 µM; 6 days) reduced the protein expression of ALB, AFP, CYP3A4, β-catenin and TCF1 in the nucleus [3]. IWR-1-endo (5-50μM; 24h; 48h) reduced the proliferation of HCT116 cells in a dose- and time-dependent manner [4].
IWR-1-endo (10 μM, ip, q2d; 30 days) partially rescued the cardiomyocyte proliferation defect caused by impaired endocardial Notch signaling[5]. In vivo, IWR-1-endo (5 μM; 24 h) inhibited zebrafish tail fin regeneration with a minimum inhibitory concentration of 0.5 μM. The IWR-1-exo diastereoisomer has much lower activity on the Wnt/β-catenin pathway and has been used as a control[6].
[1]. Lu J, Ma Z, Hsieh JC, Fan CW, Chen B, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7. [2]. [2].Wang Y, Wu Z, Tian J, Mi Y, Ren X, Kang J, Zhang W, Zhou X, Wang G, Li R. Intermedin protects HUVECs from ischemia reperfusion injury via Wnt/β-catenin signaling pathway. Ren Fail. 2019 Nov;41(1):159-166.
[3]. Gao W, Zhou P, Ma X, Tschudy-Seney B, Chen J, Magner NL, Revzin A, Nolta JA, Zern MA, Duan Y. Ethanol negatively regulates hepatic differentiation of hESC by inhibition of the MAPK/ERK signaling pathway in vitro. PLoS One. 2014 Nov 13;9(11):e112698.
[4]. Lee SC, Kim OH, Lee SK, Kim SJ. IWR-1 inhibits epithelial-mesenchymal transition of colorectal cancer cells through suppressing Wnt/β-catenin signaling as well as survivin expression. Oncotarget. 2015 Sep 29;6(29):27146-59.
[5]. Zhao L, Ben-Yair R, Burns CE, Burns CG. Endocardial Notch Signaling Promotes Cardiomyocyte Proliferation in the Regenerating Zebrafish Heart through Wnt Pathway Antagonism. Cell Rep. 2019 Jan 15;26(3):546-554.e5.
[6]. Lu J, Ma Z, Hsieh JC, Fan CW, Chen B, Longgood JC, Williams NS, Amatruda JF, Lum L, Chen C. Structure-activity relationship studies of small-molecule inhibitors of Wnt response. Bioorg Med Chem Lett. 2009 Jul 15;19(14):3825-7.
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