IWP-2

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Chemical Structure| 686770-61-6 同义名 : -
CAS号 : 686770-61-6
货号 : A250953
分子式 : C22H18N4O2S3
纯度 : 99%
分子量 : 466.599
MDL号 : MFCD12912418
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(4.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 10 mg/mL(21.43 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：

IP 25% DMSO+water 1 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • CK1

    M82FCK1δ, IC50:40 nM
描述 Wnt signaling, one of the key cascades regulating development and stemness, has been tightly associated with cancer, abnormalities and degenerative diseases[3]. IWP-2 is an inhibitor of Wnt pathway with IC50 of 27 nM, and it targets the O-acyltransferase Porcupine without inducing Porcupine destruction or mislocalization[4]. The anti-proliferative effect of LEF was significantly enhanced by co-incubating with 20 μM IWP-2 for 48 hours in Caki-2 cells. And the combination of LEF and IWP-2 could minimize the expression of β-catenin, c-Myc, Cyclin D1, Bcl2 and Bax to the largest extent compared with single agents[5]. Treatment with IWP-2 on the dose of 20 μM for 24 hours can decreased the viability of NP cells by decreasing the expression of cleaved caspases 3, 8, 9, and Bax and increasing the expression of Bcl-2[6]. To evaluate the efficacy of IWP-2 In vivo, 200 μl each of IWP-2-liposome or free liposome was 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 caused significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 hours. Additionaly, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice were reduced by 2–4-fold compared with control values[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
mouse L cells Function assay 24 h Inhibition of porcupine-mediated Wnt signalling in mouse L cells after 24 hrs by SpringerImages-Topflash reporter assay, EC50=30 nM 23477365
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.43mL

4.29mL

2.14mL
参考文献

[1]36(11):1461-1473.

[2]5(2):100-7.

[3]Zhan T, Rindtorff N, Boutros M. Wnt signaling in cancer. Oncogene. 2017 Mar;36(11):1461-1473.

[4]Chen B, Dodge ME, Tang W, Lu J, Ma Z, Fan CW, Wei S, Hao W, Kilgore J, Williams NS, Roth MG, Amatruda JF, Chen C, Lum L. Small molecule-mediated disruption of Wnt-dependent signaling in tissue regeneration and cancer. Nat Chem Biol. 2009 Feb;5(2):100-7.

[5]Chen Y, Huang Q, Zhou H, Wang Y, Hu X, Li T. Inhibition of canonical WNT/β-catenin signaling is involved in leflunomide (LEF)-mediated cytotoxic effects on renal carcinoma cells. Oncotarget. 2016 Aug 2;7(31):50401-50416.