计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Wnt-C59 (C59), 豪猪 O-酰基转移酶抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Wnt-C59(C59)是高活性Wnt信号转导拮抗剂，IC50为74 pM。A porcupine homolog - Drosophila (PORCN) inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase
Information
Wnt-C59 (C59) Wnt-C59 (C59) is a PORCN inhibitor for Wnt3A-mediated activation of a multimerized TCF-binding site driving luciferase with IC50 of 74 pM in HEK293 cells.
In vitro
Wnt-C59 (C59) is claimed to inhibit PORCN enzyme activity at nanomolar concentrations. Wnt-C59 (10 nM) blocks the palmitoylation-dependent Wnt–WLS interaction in HeLa cells transfected with either WNT3A-V5 or WNT8A-V5 plasmids. Wnt-C59 (100 nM) prevents incorporation of palmitate into WNT3A in HeLa cells transfected with WNT3A-V5, consistent with inhibition of PORCN activity. Wnt-C59 (100 nM) inhibits the activity of all splice variants of murine PORCN in PORCN- HT1080 cells transfected with PORCN. Wnt-C59 is a nanomolar inhibitor of mammalian PORCN acyltransferase activity and blocks activation of all evaluated human Wnts. Wnt-C59 does not significantly inhibit the proliferation of any of 46 tested cancer cell lines in vitro at concentrations that completely inhibit PORCN. Wnt-C59 is capable to significantly inhibit proliferation and comparable to the ICG-001 treated NMuMG (NMG) cells. Wnt-C59 inhibits sphere formation by threefold in NMuMG (NMG) cells, which is dependent on Wnt10b-secretion. Wnt-C59 inhibits proliferation of human MDA-MB 231 cells by >50%. Wnt-C59 (a Porcupine inhibitor) blocks radiolabel incorporation of [125I]iodo-pentadecanoate in mouse L-Wnt3a cells transfected with Flag-Porcupine.
In vivo
Wnt-C59 concentration remains greater than 10-fold above the in vitro IC50 for at least 16 hours following a single oral dose (5 mg/kg) in mice. Wnt-C59 (10 mg/kg) prevents growth of MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors. Wnt-C59 (10 mg/kg) decreases Wnt pathway activity and decreased proliferation in MMTV-WNT1 tumors in female nude mice orthotopically transplanted with independent MMTV-WNT1 tumors as evident by decreased expression of β-catenin target gene expression. Wnt-C59 (10%) topically administered 4 weeks decreases the size of dysplasia of SmoM2-expressing cells in adult K14CREER/Rosa–SmoM2 mice.
Cell Data
cell lines：
Concentrations：--
Incubation Time：48 hours
Powder Purity:≥98%
规格
英文别名
2-(4-(2-methylpyridin-4-yl)phenyl)-N-(4-(pyridin-3-yl)phenyl)acetamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Wnt-C59 (C59)
生化机理
Wnt-C59 (C59) 是一种 PORCN 抑制剂，可用于激活 Wnt3A 介导的驱动荧光素酶的多聚 TCF 结合位点，在 HEK293 细胞中的 IC50 为 74 pM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
豪猪 O-酰基转移酶抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=NC=CC(=C1)C2=CC=C(C=C2)CC(=O)NC3=CC=C(C=C3)C4=CN=CC=C4
PubChem CID
分子量
379.45
技术文档
高级数据
关联靶点（人）
PORCN
Tchem
蛋白质-丝氨酸O-棕榈油酰转移酶豪猪(Protein-serine O-palmitoleoyltransferase porcupine)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
Wnt Signaling
目录： 技术文章
溶液计算器
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