2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. SP2509

SP2509 是有效，选择性的 LSD1 拮抗剂，IC50 值为 13 nM。

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SP2509 Chemical Structure

SP2509 Chemical Structure

CAS No. : 1423715-09-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1089
In-stock
1 mg ￥450
In-stock
5 mg ￥990
In-stock
10 mg ￥1590
In-stock
50 mg ￥4150
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

SP2509 相关抗体

Top Publications Citing Use of Products

    SP2509 purchased from MCE. Usage Cited in: Oncotarget. 2017 Aug 10;8(43):74434-74450.  [Abstract]

    ARK2 and TOV112D cells are treated with an LSD1 inhibitor SP2509 (100 nM) for 24 h. Equal amounts of protein lysates are analyzed with western blots with appropriate antibodies. Increased levels of H3K4Me2 indicated an inhibition of LSD1. GAPDH is used to confirm that equal amounts of proteins are present in all lanes.

    查看 Histone Demethylase 亚型特异性产品:

    查看所有亚型
    KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SP2509 is a potent and selective antagonist of lysine specific demethylase 1 (LSD1) with an IC50 of 13 nM[1].

    IC50 & Target

    KDM1/LSD1

     

    体外研究
    (In Vitro)

    SP2509 (250, 500, 1000 nM) inhibits LSD1 activity, depletes colony growth and induces apoptosis and cell death of cultured human acute myeloid leukemia cells, and increases H3K4Me3 on the promoters of p57 Kip, KLF4, and p21 and induces mRNA expression of p57Kip, KLF4 and p21 in AML cells. SP2509 (250, 1000 nM) induces features of morphologic differentiation of cultured and primary AML cells. Besides, SP2509 in combination with PS exerts synergistic lethal activity against cultured and primary AML cells[1]. SP2509 does not destabilize the CoREST-LSD1 interaction, and has no major destabilizing effect on the CRC. SP2509 (1 or 10 µM) induces cell death, but there are no morphological changes at a low concertation of 0.1 µM. SP2509 likewise interferes with the viability of medulloblastoma cells[2].

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

    SP2509 相关抗体:
    体内研究
    (In Vivo)

    Treatment with SP2509 (25 mg/kg) and/or PS (5 mg/kg) significantly enhances PS-mediated loss of viability of CD34+ primary AML cells and improves the survival of mice bearing AML xenografts and primagrafts[2].

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

    437.90

    Formula

    C19H20ClN3O5S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, protect from light

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 33 mg/mL (75.36 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2836 mL 11.4181 mL 22.8363 mL
    5 mM 0.4567 mL 2.2836 mL 4.5673 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (protect from light)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.75 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

    *In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.90%

    COA (191 KB) LCMS (100 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    Daoy and D283 Med cells are used in the assay. ONS-76 cells used. All medulloblastoma cell lines are kept in an incubator at 37°C in a 5% CO2/5% O2/90% N2 atmosphere with maximum humidity. XTT assays are performed in triplicates (n = 3) with three replicates for each using 1×103 Daoy cells/well, 4×103 D283 Med cells/well, and 1×103 ONS-76 cells/well in 100 µL of medium at initial seeding in 96-well plates.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Female NOD/SCID mice are exposed to 2.5 Gy of radiation. The following day, 5 million OCI-AmL3 cells are injected into the lateral tail vein of the mice and the mice are monitored for 7 days. Following treatments are administered in cohorts of 8 mice for each treatment: vehicle alone, 25 mg/kg SP2509, 5 mg/kg LBH589 and SP2509 plus LBH589. Treatments are initiated on day 7 for OCI-AmL3 cells. SP2509 (formulated in solubilization buffer [20% Cremaphor, 20% DMSO, 60% sterile water]) is administered twice per week (Tues and Thurs) intraperitoneally (IP) for 3 weeks, and then discontinued. LBH589 (formulated in 5% DMSO/ 95% normal saline) is administered by IP injection 3 days per week (M-W-F) for 3 weeks and discontinued. The doses of PS utilized in these studies are determined to be safe and effective. A separate in vivo experiment is conducted utilizing NSG mice and primary AmL cells. Following engraftment of the AmL cells (presence of greater than 1% CD45+ cells in the peripheral blood), mice are treated with SP2509 and/or PS, for three weeks.

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

    SP2509 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year (protect from light)。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2836 mL 11.4181 mL 22.8363 mL 57.0907 mL
    5 mM 0.4567 mL 2.2836 mL 4.5673 mL 11.4181 mL
    10 mM 0.2284 mL 1.1418 mL 2.2836 mL 5.7091 mL
    15 mM 0.1522 mL 0.7612 mL 1.5224 mL 3.8060 mL
    20 mM 0.1142 mL 0.5709 mL 1.1418 mL 2.8545 mL
    25 mM 0.0913 mL 0.4567 mL 0.9135 mL 2.2836 mL
    30 mM 0.0761 mL 0.3806 mL 0.7612 mL 1.9030 mL
    40 mM 0.0571 mL 0.2855 mL 0.5709 mL 1.4273 mL
    50 mM 0.0457 mL 0.2284 mL 0.4567 mL 1.1418 mL
    60 mM 0.0381 mL 0.1903 mL 0.3806 mL 0.9515 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.

    Keywords:

    SP25091423715-09-6SP 2509SP-2509Histone DemethylaseApoptosisInhibitorinhibitorinhibit

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