|2-(4-(三氟甲基)苯基)-3,5,7,8-四氢-4H-硫代吡喃并[4,3-d]嘧啶-4-酮|CsnPharm

CAS No.: 284028-89-3

XAV-939/3,5,7,8-四氢-2-[4-(三氟甲基)苯基]-4H-硫代吡喃并[4,3-d]嘧啶-4-酮 Catalog No. CSN13593

Synonyms: NVP-XAV939

XAV-939 is a selective Wnt pathway β-catenin-mediated transcription inhibitor and axin stabilizing agent with IC50 values of 11 and 4 nM for the inhibition of TNKS1 and TNKS2, respectively.

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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 PARP5A

IC50:11nM PARP5B

IC50:4nM
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].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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
- 3.2019 mL
- 16.0097 mL
- 32.0194 mL
- 5 mM
- 0.6404 mL
- 3.2019 mL
- 6.4039 mL
- 10 mM
- 0.3202 mL
- 1.6010 mL
- 3.2019 mL

技术信息

CAS号

284028-89-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H11F3N2OS

运输

蓝冰

分子量

312.31

别名

NVP-XAV939

溶解度

DMSO	12.0 mg/mL (38.4 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

4% DMSO+corn oil

1 mg/mL

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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

靶点	Description	IC50
PARP5A		IC50:11nM
PARP5B		IC50:4nM

XAV-939/3,5,7,8-四氢-2-[4-(三氟甲基)苯基]-4H-硫代吡喃并[4,3-d]嘧啶-4-酮 Catalog No. CSN13593

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