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  2. Stem Cell/Wnt Epigenetics Cell Cycle/DNA Damage
  3. β-catenin PARP
  4. XAV-939

XAV-939 是一種 Tankyrase 抑制劑。XAV-939 對(duì) TNKS1 和 TNKS2 具有抑制活性，IC50 值分別為 5 nM 和 2 nM。XAV-939 也是 hMSCs 成骨細(xì)胞分化的增強(qiáng)劑。XAV-939 可用于研究與激活的 Wnt 信號(hào)傳導(dǎo)相關(guān)的疾病，例如癌癥、纖維化疾病和與低骨形成相關(guān)的疾病。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

XAV-939 Chemical Structure

XAV-939 Chemical Structure

CAS No. : 284028-89-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥500
In-stock
5 mg ￥418
In-stock
10 mg ￥558
In-stock
50 mg ￥1860
In-stock
100 mg ￥2790
In-stock
200 mg ￥3713
In-stock
500 mg   詢價(jià)  
1 g   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of XAV-939:

MCE 顧客使用本產(chǎn)品發(fā)表的 130 篇科研文獻(xiàn)

WB

    XAV-939 purchased from MCE. Usage Cited in: EMBO Mol Med. 2023 Apr 20;e17101.  [Abstract]

    XAV939 (20 μM; 3 days) restores the expression of Homer1, PSD95, and GluR1 in Shank3 knockout (KO) human neurons.

    XAV-939 purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410.  [Abstract]

    XAV-939 (5?μM) significantly decreases the expression level of β-catenin in A549 cells.

    XAV-939 purchased from MCE. Usage Cited in: Am J Physiol Renal Physiol. 2020 Sep 1;319(3):F458-F468.  [Abstract]

    Representative Western blot showing FN protein abundance in HMCs cultured in media containing NG or HG in the absence or presence of liraglutide (100 nM) or DMSO (1:1000) or XAV-939 (5 μM) for 24 h.

    XAV-939 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 18;9(2):27.  [Abstract]

    The cellular locations of β-catenin are detected by western blot. GAPDH, Histone H3, and ATP1A1 are used to normalize protein expression in total lysates and nuclear and membrane fractions, respectively. SGC-7901 cells with PCDHGA9 overexpression or vector control cells are grown in media with or without 10 μg/mL inhibitor of β-catenin (XAV-939).

    XAV-939 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 21;9:660.  [Abstract]

    By Western blotting, the α-SMA and palladin proteins are determined in cells that are pretreated with NF-κB (JSH-23), Wnt/β-catenin (XAV939), EGFR (CP-358774), p38 MAPK (TAK-715), and Smad3 (SIS3) inhibitors and are followed by TWEAK stimulation.

    XAV-939 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):2061-2067.  [Abstract]

    Western blot analysis and alizarin red staining of hDFSCs transfected by EZH2-siRNA and treated by XAV-939. DMSO is used as a vehicle control.

    XAV-939 purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphere-forming cells are treated with GDC-0449 (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.

    XAV-939 purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

    XAV-939 purchased from MCE. Usage Cited in: Biomed Res Int. 2017;2017:1972608.  [Abstract]

    To investigate the roles of β-catenin, XAV939 (β-catenin inhibitor) was added to MNT group. Total protein is used to observe the expression of Nrf2 and LC3.

    XAV-939 purchased from MCE. Usage Cited in: Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1898-906.  [Abstract]

    Analysis of the in vitro role of the Wnt/β–catenin pathway in the regulation of AQP2 expression in response to sPRR-His treatment. Effect of XAV on sPRR-His-induced AQP2 expression (n = 6 per group).

    XAV-939 purchased from MCE. Usage Cited in: Comp Biochem Phys B. 2016 Jan;191:155-62.  [Abstract]

    The protein expression of Wnt10b and p-GSK-3β is significantly induced by LiCl treatment (A and B). Nevertheless, XAV939 treatment significantly inhibits the protein expression of p-GSK-3β (B). Moreover, the protein expression of p-β-catenin is significantly inhibited by LiCl treatment, but significantly induced by XAV939 treatment (C).

    XAV-939 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016;39(1):360-70.  [Abstract]

    EGF upregulates the expression of follicle-regulatory genes via Wnt/β-catenin signaling pathway. (A) The mRNA and (B, C) the protein levels of Survivin, Msx2 and SGK3 in the ORS cells with EGF treatment/overexpression and/or XAV-939 treatment.

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    XAV-939 is a Tankyrase inhibitor. XAV-939 has inhibitory activity for TNKS1 and TNKS2 with IC50 values of 5 nM and 2 nM, respectively. XAV-939 also is an enhancer of osteoblastic differentiation of hMSCs. XAV-939 can be used for the research of conditions associated with activated Wnt signaling, such as cancer, fibrotic diseases and conditions associated with low bone formation[1][2][3].

    IC50 & Target[6]

    TNKS2

    2 nM (IC50)

    TNKS1

    5 nM (IC50)

    ARTD2

    479 nM (IC50)

    ARTD1

    5500 nM (IC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    12.3 μM
    Compound: XAV939
    Growth inhibition of human A549 cells after 72 hrs by MTT assay
    Growth inhibition of human A549 cells after 72 hrs by MTT assay
    		[PMID: 29934219]
    COLO 320DM GI50
    17 μM
    Compound: XAV939
    Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
    Antiproliferative activity against human COLO320DM cells assessed as inhibition of cell growth measured after 4 days by CellTiter-Glo assay
    		[PMID: 30883102]
    DLD-1 IC50
    0.707 μM
    Compound: 1, XAV-939
    Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay
    Inhibition of tankyrase in human DLD1 cells assessed as reduction in Wnt activity after 24 hrs by TCF-luciferase reporter gene assay
    		[PMID: 25299683]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay
    Inhibition of mouse Wnt3A signaling in human HEK293 cells after 1 day by super top flash luciferase reporter gene assay
    		[PMID: 22260203]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay
    Inhibition of Wnt signaling in human HEK293 cells assessed as inhibition of forskolin-induced cAMP response element activation by STF luciferase reporter gene assay
    		[PMID: 23879431]
    HEK293 IC50
    0.078 μM
    Compound: 1, XAV939
    Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin
    Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin
    		[PMID: 23844574]
    HEK293 IC50
    272 μM
    Compound: 3, XAV939
    Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
    Inhibition of Tankyrase in human HEK293 cells assessed as inhibition of Wnt pathway by Wnt3a-induced STF assay
    		[PMID: 23316926]
    HEK-293T IC50
    51 nM
    Compound: 2, XAV939
    Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
    Inhibition of beta-casein-dependent canonical Wnt3 pathway in human HEK293T cells by luciferase reporter gene assay
    		[PMID: 22191557]
    Sf21 IC50
    0.0053 μM
    Compound: 1, XAV939
    Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis
    Inhibition of N-terminal GST-tagged TNKS2 (unknown origin) expressed in baculovirus infected sf21 cells after 60 mins by LC-MS analysis
    		[PMID: 23879431]
    Sf21 IC50
    17 nM
    Compound: 5; XAV939
    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
    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
    		[PMID: 27163581]
    Sf9 IC50
    2.1 nM
    Compound: XAV939
    Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human N-terminal GST-tagged TNKS2 (667 to 1166 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    		[PMID: 31042381]
    Sf9 IC50
    4.2 nM
    Compound: XAV939
    Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    Inhibition of human N-terminal GST-tagged TNKS1 (1001 to 1327 residues) expressed in baculovirus infected Sf9 insect cells using histone as substrate measured after 1 hr by horseradish peroxidase-coupled chemiluminescence assay
    		[PMID: 31042381]
    SW480 GI50
    > 50 μM
    Compound: XAV939
    Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay
    Growth inhibition of human SW480 cells by Cell-titer-fluor reagent based assay
    		[PMID: 31769984]
    SW480 EC50
    0.371 μM
    Compound: 1, XAV939
    Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA
    Stabilization of Axin2 in human SW480 cells after 24 hrs by sandwich ELISA
    		[PMID: 22260203]
    體外研究
    (In Vitro)

    XAV-939 對(duì) TNKS1 和 TNKS2 具有活性，IC50 值分別為 5 nM 和 2 nM[1]。
    XAV-939 (0.3-30 μM；3 或 10 天) 增強(qiáng) hBMSCs 的成骨細(xì)胞分化[2]。
    XAV-939 (3 μM) 通過(guò) SH3BP2 的積累促進(jìn) hMSCs 的成骨細(xì)胞分化[2]。
    XAV-939 (3 μM；10 天) 在成骨細(xì)胞分化過(guò)程中上調(diào) hBMSC 細(xì)胞中 OPG 的表達(dá)并下調(diào) RANKL 的表達(dá)[2]。
    XAV-939 抑制 Wnt/β-catenin 信號(hào)并促進(jìn) SFRP3 和 SFRP4 的表達(dá)[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 0.3, 3, and 30 μM
    Incubation Time: 3 days
    Result: Showed no significant effect on proliferation at day 1, 2, and 3 at dose of 0.3 and 3 μM but inhibited hMSCs cell proliferation on day 3 at dose of 30 μM.

    Apoptosis Analysis[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 3 μM
    Incubation Time: 3 days
    Result: Showed a minute percentage of cell death (apoptosis and necrosis) in the XAV-939-treated hBMSC

    RT-PCR[2]

    Cell Line: hMSC-TERT cell line
    Concentration: 3 μM
    Incubation Time: 10 days
    Result: Upregulated gene expression of osteoblast-associated gene markers including: ALP, COL1A1, RUNX2, and OC.
    體內(nèi)研究
    (In Vivo)

    XAV-939 在體內(nèi)修復(fù)機(jī)械應(yīng)力誘導(dǎo)的軟骨退化[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    312.31

    Formula

    C14H11F3N2OS
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 15.62 mg/mL (50.01 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 3.2019 mL 16.0097 mL 32.0195 mL
    5 mM 0.6404 mL 3.2019 mL 6.4039 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 1.56 mg/mL (5.00 mM); 懸濁液; 超聲助溶

      此方案可獲得 1.56 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 15.6 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 1.56 mg/mL (5.00 mM); 懸濁液; 超聲助溶

      此方案可獲得 1.56 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 15.6 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 5 mg/mL (16.01 mM); 懸濁液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.91%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.2019 mL 16.0097 mL 32.0195 mL 80.0487 mL
    5 mM 0.6404 mL 3.2019 mL 6.4039 mL 16.0097 mL
    10 mM 0.3202 mL 1.6010 mL 3.2019 mL 8.0049 mL
    15 mM 0.2135 mL 1.0673 mL 2.1346 mL 5.3366 mL
    20 mM 0.1601 mL 0.8005 mL 1.6010 mL 4.0024 mL
    25 mM 0.1281 mL 0.6404 mL 1.2808 mL 3.2019 mL
    30 mM 0.1067 mL 0.5337 mL 1.0673 mL 2.6683 mL
    40 mM 0.0800 mL 0.4002 mL 0.8005 mL 2.0012 mL
    50 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6010 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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