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  2. Cell Cycle/DNA Damage Epigenetics
  3. Sirtuin
  4. Selisistat

Selisistat (EX-527) 是一種有效和選擇性的 SirT1 (黑腹果蠅中的 Sir2) 抑制劑，IC50 值為 123 nM。Selisistat 緩解多種亨廷頓病動物和細(xì)胞模型的病理學(xué)。

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

Selisistat Chemical Structure

Selisistat Chemical Structure

CAS No. : 49843-98-3

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥528
In-stock
5 mg ￥480
In-stock
10 mg ￥640
In-stock
25 mg ￥1100
In-stock
50 mg ￥1900
In-stock
100 mg ￥3000
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

Other Forms of Selisistat:

MCE 顧客使用本產(chǎn)品發(fā)表的 193 篇科研文獻(xiàn)

WB

    Selisistat purchased from MCE. Usage Cited in: J Funct Foods. 2023 Mar.

    Selisistat (EX527) treatment significantly increases the levels of C-caspase3 and Bax but decreases the levels of Bcl-2, in 4-OI (4-Octyl Itaconate)-treated chondrocytes.

    Selisistat purchased from MCE. Usage Cited in: Metab Brain Dis. 2019 Feb;34(1):203-212.  [Abstract]

    Western analysis of the protein expression of Sirt1, FoxO1 and LC3 protein in the PC12 with the treatment of MPP+, ECH and EX527.

    Selisistat purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Aug 3;9:854.  [Abstract]

    Western blotting and quantitative analysis of XBP-1 and ATF6 levels normalized to GAPDH in mice (n=6). Western blotting and quantitative analysis of P-Smad3 and ac-Smad3 levels normalized to T-Smad3 (n=6). I stands for ISO, G stands for GE, and E stands for Ex-527.

    Selisistat purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2018 Mar 6;1863(6):595-603.  [Abstract]

    LC3 deacetylation levels after erythropoietin (EPO) treatment are detected in PA-treated cells that have been treated with or without the SIRT1 inhibitor EX-527.

    Selisistat purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 May 19;18(5). pii: E1063.  [Abstract]

    Inhibition of sirt1 and AMPK blocked Rb2-induced hepatic autophagy. HepG2 cells are pretreated with 50 μM Rb2 for 4 h in the presence or absence of the sirt1 inhibitor EX-528 (EX) and the specific AMPK inhibitor Compound C (CC), and then subjected to OA (1 mM for HepG2 and 2 mM for primary mouse hepatocytes) exposure for 12 h. For lipid content determination, intracellular TG are stained by Oil red O (ORO). ORO is then eluted with isopropanol and the optical absorbance of the eluate is measured

    Selisistat purchased from MCE. Usage Cited in: Oncotarget. 2017 Apr 18;8(32):52783-52791.  [Abstract]

    Immunoblot analysis of p-AKT (Ser473) and LC3-II in cells treated with 50 nM of TCO for 24 h in the presence and absence of EX-527.

    查看 Sirtuin 亞型特異性產(chǎn)品:

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Selisistat (EX-527) is a potent and selective SirT1 (Sir2 in Drosophila melanogaster) inhibitor with an IC50 of 123 nM for SirT1. Selisistat alleviates pathology in multiple animal and cell models of Huntington's disease[1][2].

    IC50 & Target

    IC50: 123 nM (SirT1)[2]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    29 μM
    Compound: EX-527
    Cytotoxicity against human A549 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    HCT-116 IC50
    37 μM
    Compound: EX-527
    Cytotoxicity against human HCT-116 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    HEK-293T IC50
    51 μM
    Compound: EX-527
    Cytotoxicity against human HEK293T cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HEK293T cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    HeLa IC50
    > 100 μM
    Compound: 1
    Inhibitory activity against human HDAC in HeLa cell extract by fluorimetric assay
    Inhibitory activity against human HDAC in HeLa cell extract by fluorimetric assay
    		[PMID: 16335928]
    HepG2 IC50
    44 μM
    Compound: EX-527
    Cytotoxicity against human HepG2 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    Hs 683 IC50
    115.9 μM
    Compound: 3; EX-527
    Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Hs683 cells after 72 hrs by MTT assay
    		[PMID: 28475330]
    HT-29 IC50
    > 100 μM
    Compound: EX-527
    Cytotoxicity against human HT-29 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    HUVEC IC50
    15 μM
    Compound: EX-527
    Cytotoxicity against human HUVEC cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HUVEC cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    K562 IC50
    60 μM
    Compound: EX-527
    Cytotoxicity against human K562 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    MCF7 IC50
    37 μM
    Compound: EX-527
    Cytotoxicity against human MCF7 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    NCI-H460 IC50
    1 μM
    Compound: 59
    Inhibition of SIRT-2 in human NCI-H460 cells assessed as inhibition of p53 deacetylation after 6 hrs by immunoprecipitation/immunoblotting analysis
    Inhibition of SIRT-2 in human NCI-H460 cells assessed as inhibition of p53 deacetylation after 6 hrs by immunoprecipitation/immunoblotting analysis
    		10.1039/C1MD00199J
    NCI-H460 IC50
    48 μM
    Compound: EX-527
    Cytotoxicity against human NCI-H460 cells assessed as cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H460 cells assessed as cell viability measured after 48 hrs by MTT assay
    		[PMID: 32711231]
    U-373MG ATCC IC50
    157.4 μM
    Compound: 3; EX-527
    Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
    Antiproliferative activity against human U373 cells after 72 hrs by MTT assay
    		[PMID: 28475330]
    體外研究
    (In Vitro)

    Selisistat (1-10 μM) 可抑制轉(zhuǎn)染細(xì)胞中人類 SirT1 和果蠅 Sir2 的去乙?；钚?sup>[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Selisistat（5 和 20 mg/kg，口服，每日；轉(zhuǎn)基因 R6/2 小鼠從 4.5 周齡開始直至死亡）對亨廷頓舞蹈癥 (HD) 的 R6/2 小鼠模型具有保護(hù)作用[1]。

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

    248.71

    Formula

    C13H13ClN2O
    CAS 號
    性狀

    固體

    顏色

    Off-white to light yellow

    運(yùn)輸條件

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

    DMSO 中的溶解度 : ≥ 100 mg/mL (402.07 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 4.0207 mL 20.1035 mL 40.2070 mL
    5 mM 0.8041 mL 4.0207 mL 8.0414 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(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

    動物實(shí)驗(yàn)：

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

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (10.05 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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

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

      Solubility: ≥ 2.5 mg/mL (10.05 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 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； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 10 mg/mL (40.21 mM); 澄清溶液; 超聲助溶

    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲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: 99.87%

    參考文獻(xiàn)
    Cell Assay
    [2]

    The immortal mouse macrophage cell line RAW264.7 are used. Cells are seeded in 96-well dishes at a density of 3 × 103 cells/cm2 and treated with high glucose at the concentrations of 5.6, 11.1, 25 and 30 mM, alone or with SRT1720 (1 μM) or Selisistat(10 μM) for 24 h. The stock solution of SRT1720 or Selisistat is prepared by dissolving each of them (in powder form) respectively in DMSO yielding a concentration of 100 μM and then stored at -80°C. MTT solution (0.5 mg/mL) is then added to each well and cells are incubated for 4 h at 37°C in a 5% CO2 incubator. Subsequently, the supernatant is removed, the formation of farmazan is solubilized with DMSO and measured at 540 nm with a Bio-Rad Model 680 Plate Reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3] Mice are injected with Resveratrol (RSV) 30mg/kg (4 mL/kg) or equivalent volume of DMSO (Vehicle) (4 mL/kg) intraperitoneally 18 hours pre-sepsis. This dose of RSV in mice is as per documented literature. In one group of mice, RSV pre-treated mice receive Selisistat (10 mg/kg intraperitoneally; 4mL/kg, Vehicle: DMSO) within 10 minutes of cecal ligation and puncture.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲存時(shí)，請?jiān)?年內(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 4.0207 mL 20.1035 mL 40.2070 mL 100.5175 mL
    5 mM 0.8041 mL 4.0207 mL 8.0414 mL 20.1035 mL
    10 mM 0.4021 mL 2.0103 mL 4.0207 mL 10.0517 mL
    15 mM 0.2680 mL 1.3402 mL 2.6805 mL 6.7012 mL
    20 mM 0.2010 mL 1.0052 mL 2.0103 mL 5.0259 mL
    25 mM 0.1608 mL 0.8041 mL 1.6083 mL 4.0207 mL
    30 mM 0.1340 mL 0.6701 mL 1.3402 mL 3.3506 mL
    40 mM 0.1005 mL 0.5026 mL 1.0052 mL 2.5129 mL
    50 mM 0.0804 mL 0.4021 mL 0.8041 mL 2.0103 mL
    60 mM 0.0670 mL 0.3351 mL 0.6701 mL 1.6753 mL
    80 mM 0.0503 mL 0.2513 mL 0.5026 mL 1.2565 mL
    100 mM 0.0402 mL 0.2010 mL 0.4021 mL 1.0052 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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    產(chǎn)品名稱：
    Selisistat
    目錄號：
    HY-15452
    需求量：