2. Neuronal Signaling Stem Cell/Wnt Autophagy Apoptosis
  3. Organoid γ-secretase Amyloid-β Autophagy Notch Apoptosis
  4. DAPT

DAPT  (Synonyms: GSI-IX)

目录号: HY-13027 纯度: 99.97%
COA 产品使用指南

摩尔计算器

DAPT (GSI-IX) 是一种有效的，口服活性的 γ 分泌酶 (γ-secretase) 抑制剂，对总 amyloid-β (Aβ) 和 Aβ42 的 IC50 分别为 115 nM 和 200 nM。DAPT 抑制 Notch 1 信号传导并诱导细胞分化。DAPT 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis)。DAPT 具有神经保护活性，并可用于自身免疫性和淋巴增生性疾病，退化性疾病和癌症的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

DAPT Chemical Structure

DAPT Chemical Structure

CAS No. : 208255-80-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥567
In-stock
5 mg ￥515
In-stock
10 mg ￥893
In-stock
50 mg ￥2727
In-stock
100 mg ￥3820
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of DAPT:

DAPT 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 99 篇科研文献

WB
IHC
Proliferation Assay

    DAPT purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2022 Oct 19;246:114183.  [Abstract]

    DAPT treatment enhances the protein expression of Bax and decreases the expression of Bcl2. And the expression of cleaved-caspase3 is upregulated after DAPT treatment (10 μM; for 24 h).

    DAPT purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2022 Oct 19;246:114183.  [Abstract]

    Detection of cell viability after treatment with different concentrations of DAPT (5 μM, 10 μM, 15 μM, 20 μM; for 24 h).

    DAPT purchased from MCE. Usage Cited in: Neural Regen Res. 2019 Mar;14(3):452-461.  [Abstract]

    Western blot assay for Hes1 (left) and Hes5 (right) protein expression in the right prefrontal cortex of cerebral I/R mice following DAPT treatment.

    DAPT purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Nov;107:1370-1376.  [Abstract]

    ECa109 and EC9706 cells are treated with concentrations of GSI-DAPT (0, 10 and 20 μM) for 48 h. The expressions of Notch3, DTX1 and Hes1 are investigated by Western blotting.

    DAPT purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Nov;107:1370-1376.  [Abstract]

    ECa109 and EC9706 cells are treated with concentrations of GSI-DAPT (0, 10 and 20 μM) for 48 h. The expressions of LSD1 and H3K4me2 are investigated by Western blotting.

    DAPT purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656.  [Abstract]

    Evaluation of expression change of Notch downstream under the androgen-deprived condition with or without the treatment of DAPT by western blot assay.

    DAPT purchased from MCE. Usage Cited in: J Cell Physiol. 2018 Mar;233(3):2225-2237.  [Abstract]

    DAPTprevents Nicd splitting from Notch1 and has been recognized as a Notch1 pathway inhibitor. Treatment with DAPT also inhibits the expression of Col IV and FN, resembling the effect of Notch1 siRNA.

    DAPT purchased from MCE. Usage Cited in: Drug Des Devel Ther. 2018 Nov 8;12:3847-3854.  [Abstract]

    Western anslysis of protein analysis of NOX2, NICD, Hes1, Hes5 in the treatment of TBI, TBI+vehicle, TBI+DAPT and TBI+DPI, respectively.

    DAPT purchased from MCE. Usage Cited in: J Cell Biochem. 2018 Oct 26;120(2):1903-1915.  [Abstract]

    The distribution of aggrecan is increased in the DAPT group.

    DAPT purchased from MCE. Usage Cited in: PLoS One. 2018 Feb 15;13(2):e0193037.  [Abstract]

    After DAPT treatment, the protein levels of Notch, Hes1 and Hes5 are downregulated in severe injury group. After DAPT treatment, the protein levels of Bcl-2 are upregulated while those of Bax, caspase-3 and caspase-9 are downregulated.

    DAPT purchased from MCE. Usage Cited in: World J Gastroenterol. 2017 Apr 7;23(13):2330-2336.  [Abstract]

    Notch γ-secretase inhibitor attenuates notch and transforming growth factor-β signaling pathways in peripheral blood mononuclear cells of liver fibrosis rats. Western blot analysis of protein expression of Notch1, Hes1, Hes5, TGF-β and Smad3 and quantification in PBMCs (2 × 106) from rats treated with DAPT or DMSO for 24 h.

    DAPT purchased from MCE. Usage Cited in: Department Medicine. Yale University. 2016 Jan.

    Treatment with DAPT does not markedly alter expression of p27Kip1 in bulk or CD133- cells, but dramatically enhances its expression in CD133+ 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

    DAPT (GSI-IX) is a potent and orally active γ-secretase inhibitor with IC50s of 115 nM and 200 nM for total amyloid-β (Aβ) and Aβ42, respectively. DAPT inhibits the activation of Notch 1 signaling and induces cell differentiation. DAPT also induces autophagy and apoptosis. DAPT has neuroprotection activity and has the potential for autoimmune and lymphoproliferative diseases, degenerative disease and cancers treatment[1][2].

    IC50 & Target

    IC50: 115 nM (Aβ), 200 nM (Aβ42)[5]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    Hep 3B2 IC50
    5 μM
    Compound: DAPT
    Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human Hep3B cells assessed as growth inhibition after 72 hrs by SRB assay
    		[PMID: 30108693]
    Huh-7 IC50
    5 μM
    Compound: DAPT
    Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay
    		[PMID: 30108693]
    Mahlavu IC50
    5 μM
    Compound: DAPT
    Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human Mahlavu cells assessed as growth inhibition after 72 hrs by SRB assay
    		[PMID: 30108693]
    SNU-475 IC50
    0.6 μM
    Compound: DAPT
    Cytotoxicity against human SNU475 cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human SNU475 cells assessed as growth inhibition after 72 hrs by SRB assay
    		[PMID: 30108693]
    体外研究
    (In Vitro)

    DAPT 抑制 Aβ 的产生超过 90%，仅适度降低培养基中的 APPβ。尽管 DAPT 处理后 APPβ 减少了约 30%，但这种作用不依赖于浓度，并且可以通过去除 DAPT 来逆转[1]。
    DAPT 的浓度 (0、25、50 和 75 μM) 和 γ-分泌酶产生的 Notch 1 片段 Val1744-NICD 在 48 小时后以剂量依赖性方式降低 (P <0.01)。在 50 μM 浓度下，γ-分泌酶的激活几乎完全被 DAPT 抑制[3]。

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

    DAPT 相关抗体:
    体内研究
    (In Vivo)

    将 DAPT 施用于 PDAPP 小鼠 (100 mg/kg sc)，并检查大脑皮层中的 DAPT 和 Aβ 水平。处理后 3 小时大脑中达到 490 ng/g 的峰值 DAPT 水平，并且在前 18 小时内持续超过 100 ng/g (~200 nM) 的水平。这些 DAPT 的脑浓度超过了其降低神经元培养物中 Aβ 的 IC50 (115 nM)，并产生了稳健和持续的药效学效应[1]。
    DAPT 通过下调大鼠Notch 1和核因子kappa B的表达来保护大脑免受脑缺血。Western blot 分析还显示，DAPT (0.03 mg/kg) 组 Notch 1 和 NF-κB 表达显著降低 (P<0.05 vs. MCAO 组)[2]。

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

    432.46

    Formula

    C23H26F2N2O4
    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
    细胞实验： 

    DMSO 中的溶解度 : 62.5 mg/mL (144.52 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)

    Ethanol 中的溶解度 : 10 mg/mL (23.12 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3124 mL 11.5618 mL 23.1235 mL
    5 mM 0.4625 mL 2.3124 mL 4.6247 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

    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: ≥ 2.5 mg/mL (5.78 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.78 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 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。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 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： Corn Oil

      Solubility: 10 mg/mL (23.12 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 15% Cremophor EL    85% Saline

      Solubility: 20 mg/mL (46.25 mM); 悬浊液; 超声助溶

    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: 99.97%

    COA (283 KB) HNMR (258 KB) RP-HPLC (245 KB) LCMS (96 KB) 元素分析报告 (207 KB)

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

    Human embryonic kidney cells, transfected with the gene for APP751 (HEK 293) are used for routine Aβ reduction assays. Cells are plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. Cells are pre-treated for 2 h at 37°C with DAPT (0, 0.4, 2, 10, 50 and 250 nM), media are aspirated off and fresh compound solutions applied. After an additional 2-h treatment period, conditioned media are drawn off and analyzed by a sandwich ELISA (266-3D6) specific for total Aβ. Reduction of Aβ production is measured relative to control cells treated with 0.1% DMSO and expressed as a percentage inhibition. Data from at least six doses in duplicate are fitted to a four-parameter logistical model using XLfit software in order to determine potency[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    The three- to four-month-old heterozygous PDAPP transgenic mice overexpressing the APPV717F mutant form of the amyloid precursor protein. Each treatment group (n=10) consists of equal numbers of age-matched male and female animals that are fasted overnight prior to treatment. Both treatment and control groups are dosed at a volume of 10 mL/kg with DAPT or vehicle alone. Tissues are processed and all Aβ and APP measurements are made. After removal of the brain, the cortex from one hemisphere is homogenized, centrifuged, and the supernatant is used for Aβ measurements. Cortex from the other hemisphere is snap frozen for analysis of compound levels. Aβ levels are expressed as ng/g of wet tissue weight, and percentage reductions are calculated relative to the mean Aβ level of tissue from vehicle-treated control animals. Data are analyzed with Mann-Whitney non-parametric statistics to assess significance.
    Rats[3]
    Male Sprague-Dawley rats (260-290 g) are used. DAPT solution is stereotactically injected into the lateral cerebral ventricle (LV) immediately after MCAO. The stereotactic injections into the LVs are performed at coordinates −0.8 mm anteroposterior, ±1.5 mm mediolateral and −4.5 mm dorsoventral from the bregma. 30 rats are randomly assigned to three operating groups (10 rats in each group): sham-operated group that receive equal volume of PBS without MCAO operation; MCAO group that receive equal volume PBS after MCAO (MCAO); and DAPT group that receive DAPT as 0.03 mg/kg after MCAO. 24 h after operation the first neurological function is assessed and then 48 h after operation the second neurological function is assessed. Meanwhile, brain water content and infarction volume are measured and compared among different groups.

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

    DAPT 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
    Ethanol / DMSO 1 mM 2.3124 mL 11.5618 mL 23.1235 mL 57.8088 mL
    5 mM 0.4625 mL 2.3124 mL 4.6247 mL 11.5618 mL
    10 mM 0.2312 mL 1.1562 mL 2.3124 mL 5.7809 mL
    15 mM 0.1542 mL 0.7708 mL 1.5416 mL 3.8539 mL
    20 mM 0.1156 mL 0.5781 mL 1.1562 mL 2.8904 mL
    DMSO 25 mM 0.0925 mL 0.4625 mL 0.9249 mL 2.3124 mL
    30 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9270 mL
    40 mM 0.0578 mL 0.2890 mL 0.5781 mL 1.4452 mL
    50 mM 0.0462 mL 0.2312 mL 0.4625 mL 1.1562 mL
    60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9635 mL
    80 mM 0.0289 mL 0.1445 mL 0.2890 mL 0.7226 mL
    100 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5781 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:

    DAPT208255-80-5GSI-IXOrganoidγ-secretaseAmyloid-βAutophagyNotchApoptosisGamma secretaseβ-amyloid peptideAβAbetaInhibitorinhibitorinhibit

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