1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. LMK-235

LMK-235 是一种有效的,选择性的 HDAC4/5 抑制剂,可抑制 HDAC5,HDAC4,HDAC6,HDAC1,HDAC2,HDAC11HDAC8 的活性,IC50 值分别为 4.22 nM,11.9 nM,55.7 nM,320 nM,881 nM,852 nM 和 1278 nM,可用于癌症研究。

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LMK-235 Chemical Structure

LMK-235 Chemical Structure

CAS No. : 1418033-25-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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5 mg ¥500
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10 mg ¥800
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50 mg ¥2500
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100 mg ¥4500
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200 mg ¥7800
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1 g   询价  

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Top Publications Citing Use of Products

    LMK-235 purchased from MCE. Usage Cited in: Life Sci. 2018 Aug 15;207:386-394.  [Abstract]

    The protein levels of HDAC4, HDAC5, HO-1, histone 3 acetylation, histone 4 acetylation and Smad7 in CCRF-SB cells are detected by Western blot after LMK-235 treatment at 0.25, 0.5, 1, 2 and 4 μM for 24 h. β-Actin is used as internal reference.

    LMK-235 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834.  [Abstract]

    OCI-LY3 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.

    LMK-235 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018;19(9):825-834.  [Abstract]

    OCILY10 cells are treated with different concentration of LMK-235 (0.5, 1.0, 1.5, 2.0 and 2.5 μM) for 24 hours,24 hours, 36 hours and 48 hours, and HDAC4 and HDAC5 protein levels are examined by Western blot .All experiments are conducted three times.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    LMK-235 is a potent and selective HDAC4/5 inhibitor, inhibits HDAC5, HDAC4, HDAC6, HDAC1, HDAC2, HDAC11 and HDAC8, with IC50s of 4.22 nM, 11.9 nM, 55.7 nM, 320 nM, 881 nM, 852 nM and 1278 nM, respectively, and is used in cancer research.

    IC50 & Target[1]

    HDAC5

    4.22 nM (IC50)

    HDAC4

    11.9 nM (IC50)

    HDAC6

    55.7 nM (IC50)

    HDAC1

    320 nM (IC50)

    HDAC11

    852 nM (IC50)

    HDAC2

    881 nM (IC50)

    HDAC8

    1278 nM (IC50)

    体外研究
    (In Vitro)

    LMK-235 shows cytotoxic activity against human ovarian cancer cell lines A2780 and A2780 CisR, with IC50s of 0.49 μM and 0.32 μM, respectively. LMK-235 inhibits HDAC in A2780 and A2780 CisR cell lines, with IC50s of 0.65 μM and 0.32 μM, respectively. LMK-235 produces a higher reduction in cell viability in comparison to the combination of cisplatin and vorinostat in all cell lines[1]. LMK-235 (0, 0.625, 1.25, 2.5, 5, 10, and 20 μM) reduces the proliferation of BC cells in a dose- and time-dependent manner. LMK-235 (0-800 nM) also inhibits the growth of BC cells. Moreover, LMK-235 synergizes with bortezomib in BC cell lines[2]. LMK235 (2, 20?nM) decreases in HDAC4 nuclear accumulation in Cdkl5 -/Y NPCs, completely restores the reduced number of neurons generated from Cdkl5 -/Y NPCs. LMK235 also restores histone 3 acetylation in Cdkl5 -/Y NPCs. LMK235 causes a notable increase in the isoform IV, but does not affect BDNF isoforms I or II[3].

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

    体内研究
    (In Vivo)

    LMK235 (5 and 20?mg/kg) restores survival and maturation of postmitotic granule neurons in Cdkl5 -/Y mice. LMK235 also restores synapse development in the dentate gyrus and hippocampus of Cdkl5 -/Y mice. Furthermore, LMK235 restores hippocampus-dependent learning and memory in Cdkl5 -/Y mice[3].

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

    分子量

    294.35

    Formula

    C15H22N2O4

    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
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 30 mg/mL (101.92 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 3.3973 mL 16.9866 mL 33.9732 mL
    5 mM 0.6795 mL 3.3973 mL 6.7946 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 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

    In Vivo:

    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 (7.07 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。

      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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (7.07 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。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    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

    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)。
    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: 99.61%

    参考文献
    Cell Assay
    [1]

    The rate of cell survival under the action of test substances is evaluated by an improved MTT assay. The assay is based on the ability of viable cells to metabolize yellow 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to violet formazan that can be detected spectrophotometrically. In brief, A2780, Cal27, Kyse510, and MDA-MB-231 cell lines are seeded at a density of 5000, 7000, 8000, and 10 000 cells/well in 96-well plates. After 24 h, cells are exposed to increased concentrations of the test compounds. Incubation is ended after 72 h, and cell survival is determined by addition of MTT solution (5 mg/mL in phosphate buffered saline). The formazan precipitate is dissolved in DMSO. Absorbance is measured at 544 and 690 nm in a FLUOstar microplate reader[1].

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

    参考文献

    LMK-235 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.3973 mL 16.9866 mL 33.9732 mL 84.9329 mL
    5 mM 0.6795 mL 3.3973 mL 6.7946 mL 16.9866 mL
    10 mM 0.3397 mL 1.6987 mL 3.3973 mL 8.4933 mL
    15 mM 0.2265 mL 1.1324 mL 2.2649 mL 5.6622 mL
    20 mM 0.1699 mL 0.8493 mL 1.6987 mL 4.2466 mL
    25 mM 0.1359 mL 0.6795 mL 1.3589 mL 3.3973 mL
    30 mM 0.1132 mL 0.5662 mL 1.1324 mL 2.8311 mL
    40 mM 0.0849 mL 0.4247 mL 0.8493 mL 2.1233 mL
    50 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
    60 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4155 mL
    80 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
    100 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 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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    产品名称:
    LMK-235
    目录号:
    HY-18998
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