2. Epigenetics
  3. Epigenetic Reader Domain Histone Acetyltransferase
  4. A-485

A-485 是 p300/CBP 的强效选择性催化抑制剂，对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC50 值分别为 9.8 nM 和 2.6 nM。

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A-485 Chemical Structure

A-485 Chemical Structure

CAS No. : 1889279-16-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3895
In-stock
1 mg ￥1100
In-stock
5 mg ￥3300
In-stock
10 mg ￥5000
In-stock
50 mg ￥9900
In-stock
100 mg
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Customer Review

A-485 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 42 篇科研文献

WB

    A-485 purchased from MCE. Usage Cited in: Nat Immunol. 2023 Jan;24(1):162-173.  [Abstract]

    A485 (10 μM; 24 h) leads to the downregulation of H3K9bhb and CPS1 in BHB-treated CD8+ TM cells; however, the use of 3-TYP (10 μM; 24 h) or Trichostatin A (TSA; 5 nM; 24 h) result in the increase of H3K9bhb and CPS1.

    A-485 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2023 Feb 13;160:114402.  [Abstract]

    A485 (1, 3 µM; 4 h) reduces endogenous acetylation of NPM1 in HA-NPM1-transfected Huh7/SR NPM1 KD cells.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively[1].

    IC50 & Target

    IC50: 9.8 nM (p300), 2.6 nM (CBP)[1]
    体外研究
    (In Vitro)

    A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC50) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.
    The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines[1].

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

    A-485 相关抗体:
    体内研究
    (In Vivo)

    After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen[1].

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

    536.48

    Formula

    C25H24F4N4O5
    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 125 mg/mL (233.00 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.8640 mL 9.3200 mL 18.6400 mL
    5 mM 0.3728 mL 1.8640 mL 3.7280 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。-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

    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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 11 mg/mL (20.50 mM); 悬浊液; 超声助溶

    • 方案 二

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

      Solubility: ≥ 2.08 mg/mL (3.88 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）。
    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: 99.83%

    COA (194 KB) LCMS (94 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    Cell lines are plated in 96 well or 384 well plates and allowed to adhere for 24 h. The cells are then treated with A-485 for 3, 4, or 5 days. Experiments are run in triplicate and the fraction of viable cells is determined using the Cell Viability Assay according to the manufacturer’s recommendations. For Thymidine incorporation assays, cells are treated with A-485 for 1, 2, 3, or 4 days. Twenty four hours prior to the time point, tritiated thymidine is added and cells are incubated for an additional 24 h. Genomic DNA is then isolated on filter plates[1].

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

    The LuCap-77 CR prostate PDX model is used in this study. Donor tumors are dissociated and injected as a brie (1:2) into the right flank of 16 week old male C.B.-17 SCID mice on day 0 in a volume of 0.2 mL. Tumors are size matched on day 26 post-inoculation with a mean tumor volume of 211±3 (SEM) mm3 with dosing beginning on day 28. Mice are randomized into treatment groups using Studylog software based on tumor volume. LuCap-77 CR xenograft tumors are established in SCID mice and animals are dosed with A-485 as for 7 days. Three hours post the final dose, tumors are harvested and snap frozen on dry ice[1].

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

    A-485 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。-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 1.8640 mL 9.3200 mL 18.6400 mL 46.6001 mL
    5 mM 0.3728 mL 1.8640 mL 3.7280 mL 9.3200 mL
    10 mM 0.1864 mL 0.9320 mL 1.8640 mL 4.6600 mL
    15 mM 0.1243 mL 0.6213 mL 1.2427 mL 3.1067 mL
    20 mM 0.0932 mL 0.4660 mL 0.9320 mL 2.3300 mL
    25 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8640 mL
    30 mM 0.0621 mL 0.3107 mL 0.6213 mL 1.5533 mL
    40 mM 0.0466 mL 0.2330 mL 0.4660 mL 1.1650 mL
    50 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9320 mL
    60 mM 0.0311 mL 0.1553 mL 0.3107 mL 0.7767 mL
    80 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5825 mL
    100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4660 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:

    A-4851889279-16-6A485A 485Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

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    目录号：
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