XAV-939 | NVP-XAV939 | Tankyrase Inhibitor | AmBeed-信号通路专用抑制剂

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XAV-939 {[allProObj[0].p_purity_real_show]}

货号：A180960 同义名： NVP-XAV939

XAV-939是一种 Tankyrase 抑制剂，可作为细胞疗法中的辅助试剂。

XAV-939 化学结构
CAS号：284028-89-3

XAV-939 3D分子结构
CAS号：284028-89-3

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XAV-939 纯度/质量文件产品仅供科研

货号：A180960 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • JMC, 2024. Ambeed. [ A919389 , A918471 , A995972 ]; • Anal. Chem., 2024, 96(50): 19947-19954. Ambeed. [ A261947 , A1165388 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A220462 ]; • ACS Biomater. Sci. Eng., 2024. Ambeed. [ A165235 , A110205 ]; • Pharmaceutics, 2024, 16(12): 1546. Ambeed. [ A272538 , A187261 , A691302 , A506702 ]; 更多 >

PARP 亚型比较

产品名称	PARP ↓ ↑	PARP1 ↓ ↑	PARP2 ↓ ↑	PARP3 ↓ ↑	纯度
PJ34 HCl	++ PARP, EC50: 20 nM				99%+
Rucaparib phosphate	++++ PARP, Ki: 1.4 nM				99%+
3-Aminobenzamide	++ PARP, IC50: <50 nM				98%
AZD-2461	✔				99%+
BGP-15	✔				99%+
NU1025	+ PARP, IC50: 400 nM				97%
Benzamide	+ PARP, IC50: 3.3 μM				98%
Picolinamide	+ PARP, IC50: 95 μM				98%
AG14361		+++ PARP1, Ki: <5 nM			98+%
Iniparib		✔			98%
Talazoparib		++++ PARP1, IC50: 0.57 nM			99%+
NMS-P118		++ PARP1, Kd: 0.009 μM			98+%
UPF 1069		+ PARP1, IC50: 8.0 μM	++ PARP2, IC50: 0.3 μM		98%
A-966492		++++ PARP1, Ki: 1 nM PARP1, EC50: 1 nM	+++ PARP2, Ki: 1.5 nM		99%+
Veliparib		++ PARP1, Ki: 5.2 nM	+++ PARP2, Ki: 2.9 nM		98%
Niraparib tosylate		+++ PARP1, IC50: 3.8 nM	+++ PARP2, IC50: 2.1 nM		99%+
Stenoparib		++++ PARP1, IC50: 1 nM	++++ PARP2, IC50: 1.2 nM		98%
Olaparib		+++ PARP1, IC50: 5 nM	++++ PARP2, IC50: 1 nM		98%
Niraparib		+++ PARP1, IC50: 3.8 nM	+++ PARP2, IC50: 2.1 nM		98%
ME0328		+ PARP1, IC50: 6.3 μM		+ PARP3, IC50: 0.89 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

XAV-939 生物活性

描述

Poly (ADP-ribose) polymerase (PARP) 1 is an essential molecule in DNA damage response by sensing DNA damage and docking DNA repair proteins on the damaged DNA site through a type of posttranslational modification, poly (ADP-Ribosyl)ation (PARylation). PARP inhibitors, which inhibit PARylation through competitively binding to NAD+ binding site of PARP1 and PARP2, have improved clinical benefits for BRCA mutated tumors, leading to their accelerated clinical application^[3]. XAV-939 is a potent tankyrase inhibitor that targets Wnt/β-catenin signaling. XAV-939 stabilizes axin by inhibiting tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM, respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively)^[4].XAV939 (0.5 μM, 1.0 μM) reduces DNA-PKcs protein levels 50% of the relative DMSO control in human lymphoblasts^[5]. XAV939 induces a second wave of pro-cardiomyocyte gene expression as shown by increased Mesp1 and Isl1expression 2 to 4 days after Wnt inhibition, and by increased Nkx2.5 expression 4 to 6 days after XAV939 addition^[6]. XAV-939 (10 nM) has a suppressive effect on elevated MMP-13 levels in both IL-1β-induced SW 1353 cells. XAV-939 (3 mL, 10 nM) has a suppressive effect on elevated MMP-13 levels in the rat OA model^[7].XAV-939(1mg/mL,i.p.) ameliorates the psoriasiform skin disease induced by IMQ. XAV-939 results in a significant decrease in the IMQ-induced epidermal hyperplasia (indicated by acanthosis) and dermal inflammatory infiltrates in mice^[8].

XAV-939 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
DLD1	20 μM	Function Assay	24 h	Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity	24527792
DLD1	20 μM	Cytotoxic Assay	10 d	Cytotoxicity assessed as growth inhibition	24527792
HEK293T		Function Assay		Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM	23879431
HEK293T	10 μM	Function Assay		Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM	22191557

XAV-939 参考文献

[1] Ahrum Min ,et al. PARP Inhibitors as Therapeutics: Beyond Modulation of PARylation. Cancers (Basel). 2020 Feb 8;12(2):394.

[2] Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-620.

[3] Ahrum Min ,et al. PARP Inhibitors as Therapeutics: Beyond Modulation of PARylation. Cancers (Basel). 2020 Feb 8;12(2):394.

[4] Huang SM, et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling. Nature. 2009 Oct 1;461(7264):614-620.

[5]Dregalla RC, et al. Regulatory roles of tankyrase 1 at telomeres and in DNA repair: suppression of T-SCE and stabilization of DNA-PKcs. Aging (Albany NY). 2010 Oct;2(10):691-708.

[6]Ao A, et al. DMH1, a Novel BMP Small Molecule Inhibitor, Increases Cardiomyocyte Progenitors and Promotes Cardiac Differentiation in Mouse Embryonic Stem Cells.,PLoS One. 2012;7(7):e41627.

XAV-939 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.01mL

3.20mL

1.60mL

32.02mL

6.40mL

3.20mL

XAV-939 技术信息

CAS号	284028-89-3
分子式	C₁₄H₁₁F₃N₂OS
分子量	312.31

别名	NVP-XAV939
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C

溶解方案

细胞实验：

DMSO: 15 mg/mL(48.03 mM)，配合低频超声，并水浴加热至45℃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

动物实验配方

4% DMSO+corn oil 1 mg/mL

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

DLD1	20 μM	Function Assay	24 h	Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity	24527792
DLD1	20 μM	Cytotoxic Assay	10 d	Cytotoxicity assessed as growth inhibition	24527792
HEK293T		Function Assay		Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM	23879431
HEK293T	10 μM	Function Assay		Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM	22191557
HEK293T		Function Assay	24 h	Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM	22260203
HEK293T	50 μM	Function Assay		Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE	22260203
HeLa	10 μM	Function Assay	48 h	Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
IEC-6		Function Assay	6 h	Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced axin2 expression with IC50 of 0.64 μM	24060489
IEC-6		Function Assay	6 h	Antagonist activity at Beta-catenin/TCF assessed as inhibition of Wnt-3a-induced lgr5 expression with IC50 of 2.9 μM	24060489
Sf-21	18.75 μM	Kinase Assay	60 min	Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM	23879431
SiHa	10 μM	Function Assay	48 h	Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
SW480	10 μM	Function Assay	24 h	Stabilization of Axin2 with EC50 of 0.371 μM	22260203
VERO	25 μM	Function Assay		Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion	25332845

XAV-939 {[allProObj[0].p_purity_real_show]}

XAV-939 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

XAV-939 质控信息

XAV-939 生物活性

XAV-939 细胞研究

XAV-939 参考文献

XAV-939 实验方案

XAV-939 技术信息

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XAV-939 {[allProObj[0].p_purity_real_show]}

XAV-939 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

XAV-939 质控信息

XAV-939 生物活性

XAV-939 细胞研究

XAV-939 参考文献

XAV-939 实验方案

XAV-939 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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XAV-939 纯度/质量文件产品仅供科研