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Merck
CN

I0161

Sigma-Aldrich

IWR-1

≥98% (HPLC), powder, Tankyrase1/2 inhibitor

别名:

4-(1,3,3a,4,7,7a-六氢-1,3-二氧代-4,7-亚甲基-2H-异吲哚-2-基)-N-8-喹啉基-苯甲酰胺, IWR1

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About This Item

经验公式(希尔记法):
C25H19N3O3
分子量:
409.44
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

产品名称

IWR-1, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

颜色

white to beige

溶解性

DMSO: 5 mg/mL, clear

储存温度

room temp

SMILES字符串

O=C(Nc1cccc2cccnc12)c3ccc(cc3)N4C(=O)[C@@H]5[C@H]6C[C@H](C=C6)[C@@H]5C4=O

InChI

1S/C25H19N3O3/c29-23(27-19-5-1-3-14-4-2-12-26-22(14)19)15-8-10-18(11-9-15)28-24(30)20-16-6-7-17(13-16)21(20)25(28)31/h1-12,16-17,20-21H,13H2,(H,27,29)/t16-,17+,20-,21+

InChI key

ZGSXEXBYLJIOGF-ALFLXDJESA-N

应用

IWR-1已被用作人类胚胎干细胞(hESCs)、小鼠lewis肺癌(LLC)和Sepia胚胎中Wingless/Integrated(WNT)信号通路的拮抗剂。

生化/生理作用

IWR-1是一种端锚聚合酶抑制剂,其对癌症干细胞样细胞具有细胞毒性。它可抑制 体内 骨肉瘤的进展。IWR-1可与RNA聚合酶II相互作用,对于预启动复合物的形成至关重要。
Wnt/b-连环蛋白(‘经典′)途径维持转录程序,使干细胞保持多能性。Wnt/b-连环蛋白途径超活化会导致疾病分期。IWR-3充当Wnt反应的抑制剂。似乎IWR化合物通过直接相互作用诱导Axin蛋白稳定化,该蛋白是b-连环蛋白破坏复合体(由Apc、Axin、Ck1和Gsk3b组成)的一部分。

特点和优势

该化合物是基因调控研究的推荐产品。点击此处,了解更多推荐基因调控产品。了解更多有关用于其他研究领域的生物活性小分子的信息,请访问sigma.com/discover-bsm

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Jessica E Frith et al.
PloS one, 8(12), e82931-e82931 (2014-01-01)
Cellular microenvironmental conditions coordinate to regulate stem cell populations and their differentiation. Mesenchymal precursor cells (MPCs), which have significant potential for a wide range of therapeutic applications, can be expanded or differentiated into osteo- chondro- and adipogenic lineages. The ability
IWR-1, a tankyrase inhibitor, attenuates Wntbeta-catenin signaling in cancer stem-like cells and inhibits in vivo the growth of a subcutaneous human osteosarcoma xenograft
Martins-Neves SR, et al.
Cancer Letters, 414, 1-15 (2018)
Efficient differentiation of TBX18+/WT1+ epicardial-like cells from human pluripotent stem cells using small molecular compounds
Zhao J, et al.
Stem Cells and Development, 26(7), 528-540 (2017)
A serine in exon 11 determines the full transcriptional activity of TCF-4 in lung carcinoma cells
Yang B, et al.
Biochemical and biophysical research communications, 508(3), 675-681 (2019)
Fei Gao et al.
Cancer letters, 402, 177-189 (2017-06-13)
Akt1 is essential for the oncogenic transformation and tumor growth in various cancers. However, the precise role of Akt1 in advanced cancers is conflicting. Using a neuroendocrine TRansgenic Adenocarcinoma of the Mouse Prostate (TRAMP) model, we first show that the

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