1. Apoptosis
  2. Apoptosis
  3. SecinH3

SecinH3 是 cytohesins 的拮抗剂,对于 hCyh1hCyh2mCyh3hCyh3drosophila steppkeyGea2-S7IC50 值分别为 5.4 μM,2.4 μM,5.4 μM,5.6 μM,5.6 μM 和 65 μM。

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SecinH3 Chemical Structure

SecinH3 Chemical Structure

CAS No. : 853625-60-2

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10 mM * 1 mL in DMSO ¥860
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

SecinH3 is an antagonist of cytohesins with IC50s of 5.4 μM, 2.4 μM, 5.4 μM, 5.6 μM, 5.6 μM and 65 μM for hCyh1, hCyh2, mCyh3, hCyh3, drosophila steppke and yGea2-S7, respectively.

IC50 & Target

IC50: 5.4 μM (hCyh1),2.4 μM (hCyh2),5.4 μM (mCyh3),5.6 μM (hCyh3),5.6 μM (drosophila steppke), 65 μM (yGea2-S7)[1]

体外研究
(In Vitro)

SecinH3 is a Sec7-specific guanine nucleotide exchange factor (GEF) inhibitor with preference for the small GEFs of the cytohesin family. SecinH3 almost completely blocks the insulin-dependent transcriptional repression of IGFBP1 with an IC50 of 2.2 μM. Insulin-stimulated translocation of ARF6 to the plasma membrane is also inhibited by SecinH3. It is found that SecinH3 inhibits the insulin-dependent phosphorylation of Akt and FoxO1A in a concentration-dependent manner. Insulin-induced exclusion of FoxO1A from the nucleus is completely prevented by SecinH3. The binding of IRS1 to the insulin receptor is also inhibited by SecinH3[1].

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

体内研究
(In Vivo)

Compare to mice fed the same chow without SecinH3, the expression levels of the insulin-repressed gluconeogenic genes are elevated, whereas the insulin-induced glycolytic genes are reduced in SecinH3-treated mice. Insulin-stimulated Akt phosphorylation is also inhibited in SecinH3-treated mice. The expression of the genes for two key enzymes of mitochondrial β-oxidation, carnitine palmitoyltransferase 1a (Cpt1a) and hydroxyacyl-CoA dehydrogenase (Hadha), both of which are repressed by insulin, is increased in the SecinH3-treated mice. It is found significantly increased levels of serum insulin with slightly elevated glucose concentrations in SecinH3-treated mice. Accordingly, 3-hydoxybutyrate is increased in the serum of SecinH3-treated mice[1].

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

分子量

460.51

Formula

C24H20N4O4S

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 : 130 mg/mL (282.30 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 2.1715 mL 10.8575 mL 21.7151 mL
5 mM 0.4343 mL 2.1715 mL 4.3430 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: 10% DMSO    90% Corn Oil

    Solubility: ≥ 3.25 mg/mL (7.06 mM); 澄清溶液

    此方案可获得 ≥ 3.25 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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
参考文献
Cell Assay
[1]

105 HepG2 cells are seeded in 12 well plates and cultured for 24 h in EMEM containing 10 % FCS. Cells are then serum starved in EMEM for 24 h and stimulated for 12 h with 10 nM insulin in the presence of SecinH3, the negative control D5 or vehicle (0.2% final concentration of DMSO). Total mRNA is prepared using Kit and cDNA for qPCR is generated from 1 μg RNA. qPCR is performed and data are normalized to β2-microglobulin expression[1].

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

Animal Administration
[1]

C57/Bl6N mice are kept on a 12 h light/dark cycle in a pathogen-free animal facility and fed ad libitum with standard mice diet. After feeding with standard diet or with the same diet containing 0.9 μmol/g SecinH3 for 3 days, mice are intraperitoneally injected with 100 μL saline containing or not 40 μg recombinant human insulin. After 10 min the mice are anaesthetized and the liver is removed and lysed in lysis buffer. Normalized amounts of protein are either separated by SDS-PAGE and transferred onto nitrocellulose, or immunoprecipitated using agarose-conjugated antibodies against IRβ or IRS1[1].

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

参考文献

SecinH3 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 2.1715 mL 10.8575 mL 21.7151 mL 54.2876 mL
5 mM 0.4343 mL 2.1715 mL 4.3430 mL 10.8575 mL
10 mM 0.2172 mL 1.0858 mL 2.1715 mL 5.4288 mL
15 mM 0.1448 mL 0.7238 mL 1.4477 mL 3.6192 mL
20 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7144 mL
25 mM 0.0869 mL 0.4343 mL 0.8686 mL 2.1715 mL
30 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8096 mL
40 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
50 mM 0.0434 mL 0.2172 mL 0.4343 mL 1.0858 mL
60 mM 0.0362 mL 0.1810 mL 0.3619 mL 0.9048 mL
80 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6786 mL
100 mM 0.0217 mL 0.1086 mL 0.2172 mL 0.5429 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:
SecinH3
目录号:
HY-100559
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