|N-(6-甲基-2-苯并噻唑基)-2-[(3,4,6,7-四氢-4-氧代-3-苯基噻吩并[3,2D]嘧啶-2-基)硫基]乙酰胺|CsnPharm

CAS No.: 686770-61-6

N-(6-Methylbenzo[d]thiazol-2-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide Catalog No. CSN16481

Synonyms: Inhibitor of Wnt Production-2

IWP-2 is an inhibitor of porcn-mediated Wnt palmitoylation and secretion with IC50 of 27 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Wnt

IC50:27nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

动物研究
剂量
Mice: 0.3 mg/kg^[3] (i.p., thrice weekly for 10 weeks), 20 mg/kg^[4] (i.p.); 10 mg/kg^[5] (i.g.)

给药途径
i.p., i.g.

动物研究
剂量	Mice: 0.3 mg/kg^[3] (i.p., thrice weekly for 10 weeks), 20 mg/kg^[4] (i.p.); 10 mg/kg^[5] (i.g.)
给药途径	i.p., i.g.

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
- 2.1432 mL
- 10.7158 mL
- 21.4317 mL
- 5 mM
- 0.4286 mL
- 2.1432 mL
- 4.2863 mL
- 10 mM
- 0.2143 mL
- 1.0716 mL
- 2.1432 mL

技术信息

CAS号

686770-61-6

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H18N4O2S3

运输

蓝冰

分子量

466.60

别名

Inhibitor of Wnt Production-2

溶解度

DMSO	4.0 mg/mL (8.6 mM) warming
Water	insoluble
DMF	60.0 mg/mL (128.6 mM) warming

动物实验配方

IP	25% DMSO+water	1 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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N-(6-Methylbenzo[d]thiazol-2-yl)-2-((4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)acetamide Catalog No. CSN16481

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