XAV-939

別名：NVP-XAV939

製品コード：S1180 純度：99.95%

XAV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition with IC50 of 11 nM/4 nM in cell-free assays, regulates axin levels and does not affect CRE, NF-κB or TGF-β.

CAS No. 284028-89-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
1g	JPY 220500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（387）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

XAV-939と併用されることが多い化合物

SU5402

XAV-939 promotes anterior central nervous system identity, while SU5402 accelerates hPSC differentiation toward neuroectodermal lineages.

Chen S, Stem Cell Reports. 2018 Dec 11;11(6):1312-1323.

LDN-193189

XAV-939 and LDN-193189 are the least effective in improving the morphology of low-density P0 RPE cultures to varying extents.

Radeke MJ, et al. Genome Med. 2015 Jun 19;7(1):58.

SB431542

XAV-939 and SB431542 significantly suppress MSC gene expression.

Zhang Y, et al. Commun Biol. 2023 May 1;6(1):476.

ICG-001

XAV939 and ICG-001 decrease the proliferation of the IGROV1 and SKOV3 ovarian cancer cell lines.

Bocchicchio S, et al. J Cell Physiol. 2019 Dec;234(12):22130-22143.

XAV-939関連製品

関連ターゲット	PARP1 PARP2 PARP3 Tankyrase-1 Tankyrase-2 PARP14 PARP7 TNKS1 TNKS2	もっと見る
関連製品	Veliparib (ABT-888) PJ34 HCl AG-14361 Iniparib (BSI-201) A-966492 G007-LK UPF 1069 AZD2461 Pamiparib ME0328 3-Aminobenzamide NMS-P118 Stenoparib (E7449) NVP-TNKS656 WIKI4 Benzamide BGP-15 2HCl NU1025 BYK204165 Fluzoparib (SHR-3162) Picolinamide	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Stem Cell Signaling Compound Library GPCR Compound Library Stem Cell Differentiation Compound Library	もっと見る

シグナル伝達経路

PARPシグナル伝達経路

PARP阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
SW480	Function Assay	10 μM	24 h	Stabilization of Axin2 with EC50 of 0.371 μM	22260203
Sf-21	Kinase Assay	18.75 μM	60 min	Inhibition of N-terminal GST-tagged TNKS2 expressed with IC50 of 0.0053 μM	23879431
DLD1	Function Assay	20 μM	24 h	Inhibition of tankyrase assessed as inhibition of TCF-dependent transcriptional activity	24527792
DLD1	Cytotoxic Assay	20 μM	10 d	Cytotoxicity assessed as growth inhibition	24527792
HeLa	Function Assay	10 μM	48 h	Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
SiHa	Function Assay	10 μM	48 h	Reduction of cytoplasmic distribution and nuclear translocation of β-catenin	25061499
HEK293T	Function Assay	50 μM		Has no Effect on forskolin-induced cAMP signaling in human HEK293T cells coexpressing CRE	22260203
HEK293T	Function Assay	10 μM		Inhibition of beta-casein-dependent canonical Wnt3 pathway with IC50 of 0.051 μM	22191557
VERO	Function Assay	25 μM		Disturbes PAR belt synthesis, affecting the actin cytoskeleton, cell shape and cell adhesion	25332845
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
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
HEK293T	Function Assay		24 h	Inhibition of mouse Wnt3A signaling with IC50 of 0.078 μM	22260203
DLD1	Function assay		24 hrs	Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay, IC50 = 0.707 μM.	25299683
Sf21	Function assay		2 hrs	Inhibition of N-terminal GST-tagged human TNKS-2 (849 to 1166 residues) expressed in in insect sf21 cells preincubated for 2 hrs followed by substrate addition measured after 30 mins, IC50 = 0.017 μM.	27163581
A549	Growth inhibition assay		72 hrs	Growth inhibition of human A549 cells after 72 hrs by MTT assay, IC50 = 12.3 μM.	29934219
HEK293T	Function Assay			Inhibition of Wnt signaling assessed as inhibition of forskolin-induced cAMP response element activation with IC50 of 0.078 μM	23879431
HEK293	Function assay			Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50 = 0.078 μM.	23844574
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

TNKS2 ^[1] (Cell-free assay)	TNKS1 ^[1] (Cell-free assay)
4 nM	11 nM

In Vitro
In vitro	XAV-939 specifically inhibits tankyrase PARP activity. XAV-939 dramatically decreases DNA-PKcs protein levels, confirming the critical role of tankyrase poly-ADP-ribosylation activity in maintaining stability of the DNA-PKcs protein. The greatest reduction of DNA-PKcs protein levels (< 25% relative expression compared to DMSO treated controls) occurs at 12 hours with 1.0 μM XAV-939 exposure. Treatment of human lymphoblasts with 1.0 μM XAV-939 results in marked elevation of tankyrase 1 levels. ^[1] XAV-939 is axin stabilizing agent. XAV-939 stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex. XAV-939 stabilizes axin by blocking the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2. Both tankyrase isoforms interact with a highly conserved domain of axin and stimulate its degradation through the ubiquitin-proteasome pathway. XAV-939 deregulates the Wnt/b-catenin pathway which has been implicated in many cancers. ^[2]
細胞実験	細胞株	WTK1 lymphoblasts
	濃度	1.0 μM
	反応時間	8 hours
	実験の流れ	XAV-939 is solubilized in DMSO at 55 °C to make a 10 mM stock solution which may be diluted later to a working concentration of 100 μM. WTK1 lymphoblasts treated with either DMSO or 1.0 μM XAV-939 for 8 hours are loaded into independent wells of a 4-20% gradient SDS-PAGE every 2 hours over the course of 6 hours. At each time point, DMSO and XAV-939 samples are loaded into wells immediately adjacent to the prior time point. The corresponding load times at 0, 2 and 4 hours results in total run times of 2, 4 and 6 hours respectively. The gel is analyzed via western blot for DNA-PKcs following completion of the final run time and is quantified after normalization to actin loading controls.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	β-catenin / E-cadherin / N-cadherin β-catenin / c-Myc / cyclin D1 / E-cadherin / N-cadherin / Vimentin		31060551
	Immunofluorescence	β-catenin / E-cadherin Actin / PAR Hes1 / β-catenin / p-STAT3		31060551

In Vivo
In Vivo	AV-939 (NVP-XAV939) selectively inhibits Wnt/β-catenin-mediated transcription through tankyrase1/2 inhibition.
動物実験	動物モデル	Male Sprague-Dawley rats
	投与量	3 mg/kg
	投与経路	i.p.

参考
[1] Dregalla RC, et al. Aging, 2010, 2(10), 691-708. [2] Huang SM, et al. Nature, 2009, 461(7264), 614-620. [3] Kim HK, et al. Neurotherapeutics. 2021 Jan;18(1):601-614.

参考

化学情報

分子量	312.31	化学式	C₁₄H₁₁F₃N₂OS
CAS No.	284028-89-3	SDF	Download XAV-939 SDFをダウンロードする
Smiles	C1CSCC2=C1N=C(NC2=O)C3=CC=C(C=C3)C(F)(F)F
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 12 mg/mL ( (38.42 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問（FAQ）

質問1:
I want to inject XAV 939 (Cat # S1180) into mice through I.P. and just wonder what kind of solvent/solution I can use for this.

回答
S1180 XAV-939 can be dissolved in 4% DMSO+corn oil at 1 mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. You can sonicate and warm it in water bath at about 45 degree to help dissolving. Then dilute with corn oil.

C1=C0/X	C1:	LOG(C1):
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C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):