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AB120897

XAV939, Tankyrase inhibitor

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(10 Publications)

MW 312.31 g/mol, Purity >98%. Potent tankyrase (TNKS) inhibitor. Inhibitor of Wnt/β-catenin signaling. (IC50 values are 11 and 4 nM for TNKS1 and 2, respectively). Inhibits TNKS PARP activity. Selectivity over other PARP enzymes and CRE, NK-κB and TGF-β.
2 Images
Immunocytochemistry/ Immunofluorescence - XAV939, Tankyrase inhibitor (AB120897)
  • ICC/IF

Unknown

Immunocytochemistry/ Immunofluorescence - XAV939, Tankyrase inhibitor (AB120897)

ab16051 staining ß-catenin in SW480 cells treated with XAV939 (ab120897), by ICC/IF. Increase of ß-catenin cytoplasmic expression and decrease in nuclear expression correlates with increased concentration of XAV939, as described in literature.
The cells were incubated at 37°C for 6 hours in media containing different concentrations of ab120897 (XAV939) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab16051 (1 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight® 488 anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

Chemical Structure - XAV939, Tankyrase inhibitor (AB120897)
  • Chemical Structure

Lab

Chemical Structure - XAV939, Tankyrase inhibitor (AB120897)

2D chemical structure image of ab120897, XAV939, Tankyrase inhibitor

Key facts

CAS number

284028-89-3

Purity

>98%

Form

Solid

form

Molecular weight

312.31 g/mol

Molecular formula

C<sub>1</sub><sub>4</sub>H<sub>1</sub><sub>1</sub>F<sub>3</sub>N<sub>2</sub>OS

Nature

Synthetic

Solubility

Soluble in DMSO to 25 mM

Biological description

Potent tankyrase (TNKS) inhibitor. Inhibitor of Wnt/β-catenin signaling. (IC50 values are 11 and 4 nM for TNKS1 and 2, respectively). Inhibits TNKS PARP activity. Selectivity over other PARP enzymes and CRE, NK-κB and TGF-β.

Canonical smiles

OC1=NC(C2=CC=C(C(F)(F)F)C=C2)=NC3=C1CSCC3

IUPAC Name

3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-one

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Complementary Products

Secondary Antibodies

AB150113

Goat Anti-Mouse IgG H&L (Alexa Fluor® 488)

Immunocytochemistry/ Immunofluorescence - Goat Anti-Mouse IgG H&L (Alexa Fluor® 488) (AB150113)

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  • 16
Biochemicals

AB142216

C59, Wnt Antagonist, Wnt signaling pathway inhibitor

Chemical Structure - C59, Wnt Antagonist, Wnt signaling pathway inhibitor (AB142216)

  • 0
  • 0
Biochemicals

AB120962

SB 415286, GSK3 inhibitor

Chemical Structure - SB 415286, GSK3 inhibitor (AB120962)

  • 0
  • 0
Primary Antibodies

AB32572

Anti-beta Catenin antibody [E247] - ChIP Grade

BOND RX™ Validated|Advanced Validation|RabMAb|Recombinant|KO Validated|Lab Essentials|20ul selling size

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-beta Catenin antibody [E247] - ChIP Grade (AB32572)

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  • 75
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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Tankyrase also known as TNKS and tankyrase-1 is an enzyme belonging to the poly(ADP-ribose) polymerase (PARP) family with a molecular mass of about 142 kDa. It is expressed in various tissues including brain heart and liver as well as in certain types of cancer cells. Mechanically tankyrase catalyzes the addition of ADP-ribose polymers to protein substrates a process known as poly(ADP-ribosyl)ation. This activity modulates the stability localization or interactions of target proteins.
Biological function summary

Tankyrase functions in diverse cellular processes. It participates in telomere maintenance by ADP-ribosylating TRF1 a telomere-binding protein leading to TRF1's disassembly from telomeres. Moreover tankyrase acts in the regulation of Wnt/β-catenin signaling where it associates with components like AXIN influencing the stability of the β-catenin destruction complex. Tankyrase can also be part of larger protein complexes such as the shelterin complex playing a role in safeguarding chromosome ends.

Pathways

Tankyrase integrates into key signaling networks. In the Wnt/β-catenin pathway tankyrase's interaction with AXIN controls the availability of β-catenin an important transcription co-activator in cell proliferation and differentiation. This enzyme also connects with the telomere maintenance pathway engaging TRF1 and contributing to telomere elongation and stability. Through these pathways tankyrase engages in processes vital for cell growth and genome integrity.

Tankyrase is implicated in cancer and heritable disorders of telomere dysfunction. Abnormal tankyrase activity correlates with increased β-catenin levels promoting oncogenesis in colorectal and other cancers. Additionally disruptions in tankyrase-mediated telomere regulation can lead to conditions like dyskeratosis congenita. Tankyrase links with proteins such as β-catenin in cancer while in telomere-related disorders it connects with TRF1 indicating its significance in maintaining cellular homeostasis.
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Product protocols

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Publications (10)

Recent publications for all applications. Explore the full list and refine your search

Theranostics 15:7127-7153 PubMed40585989

2025

FAK signaling suppression by OCT4-ITGA6 mediates the effectively removal of residual pluripotent stem cells and enhances application safety.

Applications

Unspecified application

Species

Unspecified reactive species

Wenpeng Song,Jian Wang,Shixin Gong,Xiaoyan Wang,Junji Xu,Ruiqing Wu,Zongmin Jiang,Huiyuan Zhang,Lida Wu,Yilong Wang,Yingying Su,Hao Wang,Yuchun Gu

iScience 27:109821 PubMed38770131

2024

Hypomethylation-enhanced CRTC2 expression drives malignant phenotypes and primary resistance to immunotherapy in hepatocellular carcinoma.

Applications

Unspecified application

Species

Unspecified reactive species

Ruizhi Zhang,Jingjing Dai,Feifan Yao,Suiqing Zhou,Wei Huang,Jiali Xu,Kai Yu,Yining Chen,Boqiang Fan,Liren Zhang,Jing Xu,Qing Li

Cell reports methods 3:100542 PubMed37671016

2023

Rat post-implantation epiblast-derived pluripotent stem cells produce functional germ cells.

Applications

Unspecified application

Species

Unspecified reactive species

Kenyu Iwatsuki,Mami Oikawa,Hisato Kobayashi,Christopher A Penfold,Makoto Sanbo,Takuya Yamamoto,Shinichi Hochi,Kazuki Kurimoto,Masumi Hirabayashi,Toshihiro Kobayashi

Cellular and molecular gastroenterology and hepatology 15:717-739 PubMed36516930

2022

Glycoprotein (GP)96 Is Essential for Maintaining Intestinal Epithelial Architecture by Supporting Its Self-Renewal Capacity.

Applications

Unspecified application

Species

Unspecified reactive species

Janine Häfliger,Marlene Schwarzfischer,Kirstin Atrott,Claudia Stanzel,Yasser Morsy,Marcin Wawrzyniak,Silvia Lang,Tomas Valenta,Konrad Basler,Gerhard Rogler,Michael Scharl,Marianne R Spalinger

Tissue engineering and regenerative medicine 19:823-837 PubMed35467329

2022

Distinctive Roles of Wnt Signaling in Chondrogenic Differentiation of BMSCs under Coupling of Pressure and Platelet-Rich Fibrin.

Applications

Unspecified application

Species

Unspecified reactive species

Baixiang Cheng,Fan Feng,Fan Shi,Jinmei Huang,Songbai Zhang,Yue Quan,Teng Tu,Yanli Liu,Junjun Wang,Ying Zhao,Min Zhang

Experimental and therapeutic medicine 20:3138-3146 PubMed32855682

2020

Long non-coding RNA MALAT1 suppresses the proliferation and migration of endothelial progenitor cells in deep vein thrombosis by regulating the Wnt/β-catenin pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Binghui Du,Jian Wang,Sheng Zang,Xin Mao,Yaming Du

International journal of cell biology 2020:2045969 PubMed32328102

2020

Asporin Reduces Adult Aortic Valve Interstitial Cell Mineralization Induced by Osteogenic Media and Wnt Signaling Manipulation .

Applications

Unspecified application

Species

Unspecified reactive species

Anisha Polley,Riffat Khanam,Arunima Sengupta,Santanu Chakraborty

Development (Cambridge, England) 147: PubMed32014865

2020

Mesenchymal-epithelial transition regulates initiation of pluripotency exit before gastrulation.

Applications

Unspecified application

Species

Unspecified reactive species

Sofiane Hamidi,Yukiko Nakaya,Hiroki Nagai,Cantas Alev,Takeya Kasukawa,Sapna Chhabra,Ruda Lee,Hitoshi Niwa,Aryeh Warmflash,Tatsuo Shibata,Guojun Sheng

Nature communications 7:11903 PubMed27301576

2016

A Myc-driven self-reinforcing regulatory network maintains mouse embryonic stem cell identity.

Applications

Unspecified application

Species

Unspecified reactive species

Luca Fagnocchi,Alessandro Cherubini,Hiroshi Hatsuda,Alessandra Fasciani,Stefania Mazzoleni,Vittoria Poli,Valeria Berno,Riccardo L Rossi,Rolland Reinbold,Max Endele,Timm Schroeder,Marina Rocchigiani,Żaneta Szkarłat,Salvatore Oliviero,Stephen Dalton,Alessio Zippo

PeerJ 2:e617 PubMed25332845

2014

VERO cells harbor a poly-ADP-ribose belt partnering their epithelial adhesion belt.

Applications

Unspecified application

Species

Unspecified reactive species

Laura Lafon-Hughes,Salomé C Vilchez Larrea,Alejandra Kun,Silvia H Fernández Villamil
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