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  • IWP-3
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IWP-3

An inhibitor of Wnt production

原价
¥887-3525
价格
710-2820
IWP-3的二维码

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  • 货号: ajci18384
  • CAS: 687561-60-0
  • 别名: Inhibitor of Wnt Production-3
  • 分子式: C22H17FN4O2S3
  • 分子量: 484.6
  • 纯度: >98%
  • 溶解度: ≤0.1mg/ml in DMSO;2mg/ml in dimethyl formamide
  • 储存: Store at -20°C
  • 库存: 现货

Background

IC50: 40 nM


IWP-3 is an inhibitor of Wnt production.


Wnt signaling proteins, a group of small secreted proteins, are active in tissue homeostasis, embryonic development, as well as tumorigenesis. Wnt proteins can bind to the cell surface receptors, initiating a signaling cascade that results in the β-catenin activation of gene transcription.


In vitro: In previous study, IWP-3 was identified as an inhibitor of Wnt production that could regulate in vitro Wnt pathway activity with an IC50 value of 40 nM. In addition, IWP-3 was found to be able to inactivate porcupine, a O-acyltransferase for palmitoylating Wnt proteins that was critical for the signaling ability and secretion. Moreover, IWP-3 at 5 μM was found to block Wnt-dependent phosphorylation of the low-density lipoprotein receptor-related protein 6 and the scaffold protein Dishevelled, resulting in preventing the accumulation of β-catenin [1]. In another study, IWP-3 was applied to promote cardiomyocyte generation from human embryonic stem cells by inhibiting Wnt signaling [2].


In vivo: So far, there is no animal in vivo data reported.


Clinical trial: Up to now, IWP-3 is still in the preclinical development stage.

参考文献:
[1] B.? Chen, M. E. Dodge, W. Tang, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nature Chemical Biology 5(2), 100-107 (2009).
[2] E.? Willems, S. Spiering, H. Davidovics, et al. Small molecule inhibitors of the Wnt pathway potently promote cardiomyocytes from human embryonic stem cell derived mesoderm. Circulation Research 109(4), 360-364 (2011).

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