中文名 | IWP-4 |
英文名 | N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-3-(2-methoxyphenyl)-4-oxothieno[3,2-d]pyrimidin-2-yl)thio]-acetamide |
别名 | 化合物IWP 4 2-((3-(2-甲氧基苯基)-4-氧代-3,4,6,7-四氢噻吩并[3,2-D]嘧啶-2-基)硫代)-N-(6-甲基苯并[D]噻唑-2-基)乙酰胺 |
英文别名 | IWP4 IWP 4 IWP-4 CS-2394 Wnt Inhibitor IWP-4 Inhibitor of Wnt Production-4 N-(6-Methyl-2-benzothiazolyl)-2-[(3,4,6,7-tetrahydro-3-(2-methoxyphenyl)-4-oxothieno[3,2-d]pyrimidin-2-yl)thio]-acetamide 2-((3-(2-methoxyphenyl)-4-oxo-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide Acetamide, N-(6-methyl-2-benzothiazolyl)-2-[[3,4,6,7-tetrahydro-3-(2-methoxyphenyl)-4-oxothieno[3,2-d]pyrimidin-2-yl]thio]- |
CAS | 686772-17-8 |
化学式 | C23H20N4O3S3 |
分子量 | 496.62 |
溶解度 | DMSO : 1mg/mL加热超声可适当增加溶解性母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配) |
存储条件 | -20°C |
外观 | 粉末 |
颜色 | white to light brown |
靶点 | Wnt |
体外研究 | IWP-4 is a small molecule Wnt inhibitor with an IC 50 of 25 nM. IWP-4 induces the expression of cardiac markers, including cardiac troponin I (CTNI) and cardiac myosin heavy chain bright cells (MYH hi + ). IWP-4 also results in the appearance of beating foci (0.44±0.10 SEM beats per second), which is absent in all cultures not receiving IWP-4. Further, flow cytometric analysis shows that there are significantly more MYH lo + cells in IWP-4 treated cultures (P<0.0002) compare with untreated cultures at day 16, being 17.0±1.3 SD% and 5.4±1.4 SD%, respectively. Quantification of NKX2-5 protein expression shows that 63% (481/817) of IWP-4 treated cells display nuclear NKX2-5 expression. Mesenchymal precursor cells (MPCs) treated with IWP-4 show no significant changes in the expression of AXIN2 , CTNNB1 and GSK3B as compare to osteogenic medium alone on day 7, but MPCs treated with IWP-4 express elevates levels of DKK1 and GSK3β on day 21. IWP-4 also causes a significant down regulation of SPARC and COL1A1 . |
WGK Germany | 3 |
参考资料 展开查看 | 1: García-Reyes B, Witt L, Jansen B, Karasu E, Gehring T, Leban J, Henne-Bruns D, Pichlo C, Brunstein E, Baumann U, Wesseler F, Rathmer B, Schade D, Peifer C, Knippschild U. 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 Apr 9. doi: 10.1021/acs.jmedchem.8b00095. [Epub ahead of print] PubMed PMID: 29630366. 2: Narytnyk A, Verdon B, Loughney A, Sweeney M, Clewes O, Taggart MJ, Sieber-Blum M. Differentiation of human epidermal neural crest stem cells (hEPI-NCSC) into virtually homogenous populations of dopaminergic neurons. Stem Cell Rev. 2014 Apr;10(2):316-26. doi: 10.1007/s12015-013-9493-9. PubMed PMID: 24399192; PubMed Central PMCID: PMC3969515. 3: Frith JE, Titmarsh DM, Padmanabhan H, Cooper-White JJ. Microbioreactor array screening of Wnt modulators and microenvironmental factors in osteogenic differentiation of mesenchymal progenitor cells. PLoS One. 2013 Dec 23;8(12):e82931. doi: 10.1371/journal.pone.0082931. eCollection 2013. PubMed PMID: 24376608; PubMed Central PMCID: PMC3871528. 4: Bilir B, Kucuk O, Moreno CS. Wnt signaling blockage inhibits cell proliferation and migration, and induces apoptosis in triple-negative breast cancer cells. J Transl Med. 2013 Nov 4;11:280. doi: 10.1186/1479-5876-11-280. PubMed PMID: 24188694; PubMed Central PMCID: PMC4228255. 5: Hudson J, Titmarsh D, Hidalgo A, Wolvetang E, Cooper-White J. Primitive cardiac cells from human embryonic stem c |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.014 ml | 10.068 ml | 20.136 ml |
5 mM | 0.403 ml | 2.014 ml | 4.027 ml |
10 mM | 0.201 ml | 1.007 ml | 2.014 ml |
5 mM | 0.04 ml | 0.201 ml | 0.403 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!