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S80898

IWP-2

源叶(MedMol) 97%
  • 英文名:
  • IWP-2
  • 别名:
  • Acetamide, N-(6-methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-4-oxo-3-phenylthieno[3,2-d]pyrimidin-2-yl)thio]-
  • CAS号:
  • 686770-61-6
  • 分子式:
  • C22H18N4O2S3
  • 分子量:
  • 466.6
  • MDL:
  • MFCD04457599
  • 核磁/质谱:
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源叶(MedMol) S80898-5mg 97% ¥280.00元 6 - - - EA 加入购物车
源叶(MedMol) S80898-10mg 97% ¥480.00元 9 - - - EA 加入购物车
源叶(MedMol) S80898-50mg 97% ¥1680.00元 7 - - - EA 加入购物车
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参考文献

质检证书(COA)

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  • 提示:详情请下载说明书。
  • 产品描述: IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ
  • 靶点: CK1δ:40 nM (IC50);CaseinKinase;Wnt/beta-catenin;Porcupine
  • 体内研究:
    To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the anti-inflammatory cytokine IL-10
  • 参考文献:
    1. Chen B, et al. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7. 2. García-Reyes B, et al. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J Med Chem. 2018 May 10;61(9):4087-4102. 3. Maiti G, et al. The Wingless homolog Wnt5a stimulates phagocytosis but not bacterial killing. Proc Natl Acad Sci U S A. 2012 Oct 9;109(41):16600-5.
  • 溶解性: DMF  :  12.5  mg/mL  (26.79  mM;  ultrasonic  and  warming  and  heat  to  60°C)    DMSO  :  2  mg/mL  (4.29  mM;  Need  ultrasonic)
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.143 ml 10.716 ml 21.432 ml
    5 mM 0.429 ml 2.143 ml 4.286 ml
    10 mM 0.214 ml 1.072 ml 2.143 ml
    50 mM 0.043 ml 0.214 ml 0.429 ml
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