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  3. H-89 dihydrochloride

H-89 dihydrochloride 

目录号: HY-15979A 纯度: 99.14%
COA 产品使用指南

H-89 dihydrochloride 是一种有效、选择性的 cAMP 依赖性蛋白激酶A (PKA) 抑制剂,IC50 值为 48 nM。也可轻微抑制 PKG,PKC,酪蛋白激酶活性。

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H-89 dihydrochloride Chemical Structure

H-89 dihydrochloride Chemical Structure

CAS No. : 130964-39-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥678
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5 mg ¥385
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10 mg ¥606
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50 mg ¥2325
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100 mg ¥3990
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500 mg   询价  

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Other Forms of H-89 dihydrochloride:

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 93 篇科研文献

Proliferation Assay
WB
RT-PCR

    H-89 dihydrochloride purchased from MCE. Usage Cited in: Cell Mol Immunol. 2023 Jan 5.  [Abstract]

    H89 (5 μM; 6 h) reverses ISO (Isoprenaline hydrochloride)-triggered decreases in the mRNA levels of the IFNB1 gene, the expression of which has been induced by SeV infection, in THP1 cells.

    H-89 dihydrochloride purchased from MCE. Usage Cited in: Int J Biol Sci. 2023 Apr 2,19.

    H-89 dihydrochloride (H-89; 10 μM; 2 h) blocks the epinephrine-induced phosphorylation of CREB1 in MC38 and HT-29 cells.

    H-89 dihydrochloride purchased from MCE. Usage Cited in: Aging (Albany NY). 2018 Jul 24;10(7):1722-1744.  [Abstract]

    Expressions of p-eNOS (Ser1177) and total eNOS are measured in HUVECs treated with or without H2O2 and Hemin in the presence or absence of Akt inhibitor MK-2206, PKA inhibitor H-89 or AMPK inhibitor Compound C (CP-C).

    H-89 dihydrochloride purchased from MCE. Usage Cited in: Infect Immun. 2018 Dec 19;87(1). pii: e00508-1  [Abstract]

    J774A.1 cells are pre-treated with 473 U0126 (10 μM), SB208530 (10 μM), SP600125 (10 μM), or H89 (50 μM), then infected with ΔeseH E. piscicida at the MOI of 10 for 3.5 h. Cell lysates were probed with anti-phospho-p65 (Ser276), anti-p65, and anti-β-actin antibodies.

    H-89 dihydrochloride purchased from MCE. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573.  [Abstract]

    The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.

    IC50 & Target

    IC50: 48 nM (protein kinase A)

    体外研究
    (In Vitro)

    H-89 inhibits protein kinase A, in competitive fashion against ATP. H-89 causes a dose-dependent inhibition of the forskolin-induced protein phosphorylation, with no decrease in intracellular cyclic AMP levels in PC12D cells. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells. H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates[1]. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential. H-89 (10-100 μM) inhibits net Ca2+ uptake by the SR and affectes the Ca2+-sensitivity of the contractile apparatus in rat skinned fibres[2].

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

    体内研究
    (In Vivo)

    H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold[3].

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

    分子量

    519.28

    Formula

    C20H22BrCl2N3O2S

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (192.57 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)

    H2O 中的溶解度 : 5 mg/mL (9.63 mM; 超声助溶 (<80°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.9257 mL 9.6287 mL 19.2574 mL
    5 mM 0.3851 mL 1.9257 mL 3.8515 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 (sealed storage, away from moisture)。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 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    90% Saline

      Solubility: 5 mg/mL (9.63 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.75 mg/mL (5.30 mM); 澄清溶液

    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

    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 (sealed storage, away from moisture)

    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: 99.34%

    参考文献
    Cell Assay
    [1]

    After 48 h in culture, PCl2D cells are cultured in test medium containing 30 μM H-89 for 1 h and then exposed to fresh medium that contained both 10 μM forskolin and 30 μM H-89. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5 mL of 6% trichloroacetic acid. To extract trichloroacetic acid, 2 mL of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination.

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

    Animal Administration
    [1]

    Male albino mice weighing 20-25 g are obtained. BL-191 (25, 50, 100 mg/kg), bucladesine (50, 100, 300 nM/mouse) and H-89 (0.05, 0.1, 0.2 mg/100 g) are administered intraperitoneally (i.p.) 30 min before intravenous (i.v.) infusion of PTZ. In combination groups, the first and second components are injected 45 and 30 min before PTZ infusion. In all groups, the respective control animalsreceive an appropriate volume of vehicle. For the i.v. infusion, the needle is inserted into the lateral tail vein, fixed to the tail vein by a narrow piece of adhesive tape, and the animal is allowed to move freely. PTZ solution is infused at a concentration rate of 1 mL/min.

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

    参考文献

    H-89 dihydrochloride 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 (sealed storage, away from moisture)。-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
    H2O / DMSO 1 mM 1.9257 mL 9.6287 mL 19.2574 mL 48.1436 mL
    5 mM 0.3851 mL 1.9257 mL 3.8515 mL 9.6287 mL
    DMSO 10 mM 0.1926 mL 0.9629 mL 1.9257 mL 4.8144 mL
    15 mM 0.1284 mL 0.6419 mL 1.2838 mL 3.2096 mL
    20 mM 0.0963 mL 0.4814 mL 0.9629 mL 2.4072 mL
    25 mM 0.0770 mL 0.3851 mL 0.7703 mL 1.9257 mL
    30 mM 0.0642 mL 0.3210 mL 0.6419 mL 1.6048 mL
    40 mM 0.0481 mL 0.2407 mL 0.4814 mL 1.2036 mL
    50 mM 0.0385 mL 0.1926 mL 0.3851 mL 0.9629 mL
    60 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8024 mL
    80 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.6018 mL
    100 mM 0.0193 mL 0.0963 mL 0.1926 mL 0.4814 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    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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    目录号:
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