|IWP L6游离态|CsnPharm

CAS No.: 1427782-89-5

IWP L6/IWP L6游离态 Catalog No. CSN15919

Synonyms: Porcn Inhibitor III

IWP L6 is a Porcn inhibitor with EC50 of 0.5 nM.

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技术信息

生物活性

描述Porcupine (Porcn) is a membrane bound O-acyltransferase (MBOAT) family protein, which catalyzes the palmitoylation of Wnt to enable its exit from the secretory pathway and subsequent activation of cellular responses. IWP L6 is a subnanomolar Porcn inhibitor with IC50 value of 0.5 nM. In vitro, treatment of the HEK293 cells with 2.5 μM IWP L6 effectively suppressed the phosphorylation of the cytoplasmic Wnt pathway effector disheveled 2 (Dvl2)^[2]. Treatment of T.cruzi trypomastigotes infection of Bone marrow-derived macrophages (BMM) with 20 μM IWP L6 inhibited both p-CaMKII upregulation and NFATc1 activation. IWP L6 at concentration of 20μM resulted in a inhibitory effect on intracellular parasite growth by inhibiting the secretion of Wnt proteins in T.cruzi trypomastigotes infection of BMM^[3]. In vivo stability analysis of IWP L6 showed that IWP L6 was stable in human plasma over 24h, it was rapidly metabolized in rat plasma, murine plasma and the murine liver S9 fractions with t_1/2 of 190 min, 2 min and 26 min, respectively. IWP L6 effectively inhibited posterior axis formation of juvenile zebrafish, a Wnt/β-catenin dependent developmental process, at concentration range of 1 – 5 μM^[2]. Intraperitoneal administration of IWP L6 at 7.5 mg/kg could maintain inhibited both Wnt/β-catenin as well as Wnt/Ca^{2+^{signaling pathways until 18 days post-infection in B6 mice infected with 5,000 T. cruzi trypomastigotes. In addition, treatment with IWP-L6 significantly reduced parasite load in liver and heart of B6 mice infected with 5,000 T. cruzi trypomastigotes during the chronic phase of the disease^[3].}}
参考文献

[1] Wang X, et al. J Med Chem. 2013, 56(6), 2700-2704.
[2] Wang X, Moon J, Dodge M E, et al. The Development of Highly Potent Inhibitors for Porcupine. Journal of Medicinal Chemistry, 2013, 56(6): 2700-2704.
[3] Volpini X, Ambrosio L F, Fozzatti L, et al. Trypanosoma cruzi Exploits Wnt Signaling Pathway to Promote Its Intracellular Replication in Macrophages. Frontiers in Immunology, 2018

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1160 mL
- 10.5802 mL
- 21.1604 mL
- 5 mM
- 0.4232 mL
- 2.1160 mL
- 4.2321 mL
- 10 mM
- 0.2116 mL
- 1.0580 mL
- 2.1160 mL

技术信息

CAS号	1427782-89-5	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C25H20N4O2S2	运输	蓝冰
分子量	472.58	别名	Porcn Inhibitor III

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IWP L6/IWP L6游离态 Catalog No. CSN15919

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