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  2. Epigenetics
  3. Histone Demethylase
  4. GSK2879552 dihydrochloride

GSK2879552 dihydrochloride是一種可口服的，不可逆的 LSD1/ KDM1A 抑制劑，具有抗腫瘤活性。

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GSK2879552 dihydrochloride Chemical Structure

GSK2879552 dihydrochloride Chemical Structure

CAS No. : 1902123-72-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥970
In-stock
1 mg ￥400
In-stock
5 mg ￥880
In-stock
10 mg ￥1400
In-stock
25 mg ￥2500
In-stock
50 mg ￥4000
In-stock
100 mg 現(xiàn)貨 詢價(jià)
200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of GSK2879552 dihydrochloride:

    GSK2879552 dihydrochloride purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287.  [Abstract]

    The protein expression of LSD1, PRB and H3K4me2 is detected through Western blot with GSK2879552 treatment in different cells.

    查看 Histone Demethylase 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].

    IC50 & Target

    KDM1/LSD1

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    DU-145 GI50
    > 10 μM
    Compound: GSk2879552; 2
    Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    		[PMID: 34908406]
    ECa-109 cell line IC50
    > 50 μM
    Compound: GSK2879552
    Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay
    		[PMID: 27769034]
    Kasumi 1 GI50
    0.02 μM
    Compound: 3; GSK2879552
    Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay
    Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay
    		[PMID: 32551003]
    MGC-803 IC50
    > 125 μM
    Compound: GSK2879552
    Antiproliferative activity against human MGC803 cells after 5 days by MTT assay
    Antiproliferative activity against human MGC803 cells after 5 days by MTT assay
    		[PMID: 28435523]
    MGC-803 IC50
    > 50 μM
    Compound: GSK2879552
    Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay
    		[PMID: 27769034]
    MV4-11 EC50
    0.023 μM
    Compound: 5; GSK2879552
    Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis
    Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis
    		[PMID: 35200034]
    MV4-11 EC50
    0.054 μM
    Compound: 3; GSK2879552
    Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method
    Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method
    		[PMID: 32551003]
    MV4-11 IC50
    1.16 μM
    Compound: GSK2879552
    Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay
    Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay
    		[PMID: 30713023]
    MV4-11 IC50
    1.19 μM
    Compound: 5; GSK2879552
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
    		[PMID: 35200034]
    PC-3 GI50
    > 10 μM
    Compound: GSk2879552; 2
    Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay
    		[PMID: 34908406]
    RPMI-8226 IC50
    > 20 μM
    Compound: 5; GSK2879552
    Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
    Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay
    		[PMID: 35200034]
    體外研究
    (In Vitro)

    GSK2879552 dihydrochloride 抑制 KDM1A 組蛋白去甲基化酶活性，誘導(dǎo)索拉非尼耐藥細(xì)胞的分化并減弱干細(xì)胞特性。GSK2879552 dihydrochloride 在索拉非尼耐藥細(xì)胞中抑制 Wnt 拮抗劑的轉(zhuǎn)錄并下調(diào) β-catenin 信號(hào)活性[1]。

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

    Cell Viability Assay[2].

    Cell Line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
    Concentration: 0-10000 nM.
    Incubation Time: 6 days.
    Result: Inhibited cell proliferation.

    RT-PCR[1].

    Cell Line: Resistant HCC cells (PLC/PRF/5 and Huh7).
    Concentration: 0, 1, 2 μM.
    Incubation Time: 24 h.
    Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.
    體內(nèi)研究
    (In Vivo)

    GSK2879552 dihydrochloride (1.5 mg/kg，po) 處理在攜帶 SCLC 異種移植物的小鼠中表現(xiàn)出腫瘤生長(zhǎng)抑制[2]。

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

    Animal Model: NCI-H526 and NCI-H1417 xenografts[2].
    Dosage: 1.5 mg/kg.
    Administration: PO daily for 25-35 days.
    Result: There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.
    Clinical Trial
    分子量

    437.40

    Formula

    C23H30Cl2N2O2
    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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    H2O 中的溶解度 : 100 mg/mL (228.62 mM; 超聲助溶)

    DMSO 中的溶解度 : 31.25 mg/mL (71.44 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.2862 mL 11.4312 mL 22.8624 mL
    5 mM 0.4572 mL 2.2862 mL 4.5725 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 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: ≥ 2.5 mg/mL (5.72 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(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: ≥ 2.5 mg/mL (5.72 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(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： PBS

      Solubility: 8.33 mg/mL (19.04 mM); 澄清溶液; 超聲助溶 (<60°C)

    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
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳，請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    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，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.19%

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 / H2O 1 mM 2.2862 mL 11.4312 mL 22.8624 mL 57.1559 mL
    5 mM 0.4572 mL 2.2862 mL 4.5725 mL 11.4312 mL
    10 mM 0.2286 mL 1.1431 mL 2.2862 mL 5.7156 mL
    15 mM 0.1524 mL 0.7621 mL 1.5242 mL 3.8104 mL
    20 mM 0.1143 mL 0.5716 mL 1.1431 mL 2.8578 mL
    25 mM 0.0914 mL 0.4572 mL 0.9145 mL 2.2862 mL
    30 mM 0.0762 mL 0.3810 mL 0.7621 mL 1.9052 mL
    40 mM 0.0572 mL 0.2858 mL 0.5716 mL 1.4289 mL
    50 mM 0.0457 mL 0.2286 mL 0.4572 mL 1.1431 mL
    60 mM 0.0381 mL 0.1905 mL 0.3810 mL 0.9526 mL
    H2O 80 mM 0.0286 mL 0.1429 mL 0.2858 mL 0.7144 mL
    100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5716 mL

    * 備注：如您選擇水作為儲(chǔ)備液，請(qǐng)稀釋至工作液后，再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    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：
    GSK2879552 dihydrochloride
    目錄號(hào)：
    HY-18632A
    需求量：