1. Apoptosis
  2. Caspase
  3. M190S

M109S 是一种新型小分子,在体外和体内均可保护细胞免受线粒体依赖性凋亡。M109S 有潜力成为研究细胞死亡 (cell death) 机制的研究工具,并开发针对线粒体依赖性细胞死亡途径的治疗方法。M109S 具有良好的脑通透性。

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M190S Chemical Structure

M190S Chemical Structure

CAS No. : 2578300-07-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability[1].

IC50 & Target

caspase-3

23.4 nM (EC50)

Caspase 3

23.4 nM (EC50)

体外研究
(In Vitro)

M109S (0.1-10000 nM, 24-48 h) 抑制 BaxBak 诱导的细胞凋亡 (apoptosis)[1]。< br / > M109S (0-10 μM, 4 h) 抑制 Staurosporine (HY-15141 STS) 诱导的 MEF 细胞凋亡 (apoptosis)。< br / > M109S (0-10μM, 24 h) 抑制 Etoposide (HY-13629) 诱导的 Neuro2a 细胞凋亡 (apoptosis)[1]。< br / > M109S (500 nM, 24 h) 抑制 Obatoclax (HY-10969A) 诱导的 ARPE19 细胞凋亡 (apoptosis)[1]。< br / > M109S (500 nM, 48 h) 抑制 Bax 的构象改变 (N 端暴露) 和线粒体易位[1]。< br / > M109S (1.0 μM, 4h) 降低线粒体耗氧量和活性氧,而 M109S (0.1-1 nM, 4 h) 增加糖酵解[1]。< br / >

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

Apoptosis Analysis[1]

Cell Line: MEF(Wt, Bax only, Bak only)
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 10000 nM
Incubation Time: 24 h((WT and Bax-only), 48 h (Bak-only)
Result: Showed a dose-dependent suppression of caspase activation in all three types of MEFs.

Apoptosis Analysis[1]

Cell Line: MEF
Concentration: 0 nM, 1.6 nM, 8 nM, 40 nM, 200 nM, 10000 nM
Incubation Time: 4 h
Result: Suppressed STS-induced caspase activation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: Neuro2a
Concentration: 0 nM, 40 nM, 200 nM, 10000 nM
Incubation Time: 24 h
Result: Suppressed Etoposide-induced caspase activation in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: ARPE19
Concentration: 500 nM
Incubation Time: 24 h
Result: Significantly inhibited Obatoclax-induced apoptosis in ARPE19 cells comparing to control.

Western Blot Analysis[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: Significantly suppressed the amount of immunoprecipitated Bax without a significant change in the total Bax expression.

Immunofluorescence[1]

Cell Line: iBax cells
Concentration: 500 nM
Incubation Time: 48 h
Result: Showed the frequency of the punctuated staining was significantly reduced.
体内研究
(In Vivo)

M109S (10 mg/kg, 灌胃, 48 h 内 3 次) 可保护视网膜免受强光诱导的光感受器死亡[1]
M109S (1mg /kg, 腹腔注射, 5 mg /kg, 静脉注射, 或10 mg /kg, 口服灌胃, 1次) 是一种穿透血脑/视网膜屏障的口服生物活性细胞死亡 (cell death) 抑制剂[1]

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

Animal Model: Abca4-/-Rdh8-/- mice
Dosage: 10 mg/kg
Administration: Oral Gavage (p.o.)
Result: Comparing to mice with M109S, the number of AF spots was similar to that detected in the dark-adapted mice.
Animal Model: Mice and Rat
Dosage: Intraperitoneal injection (i.p., 1 mg/kg), Intravenous injection (i.v., 5 mg/kg), or Oral gavage (p.o., 10 mg/kg)
Administration: Intraperitoneal injection (i.p.), Intravenous injection (i.v.), or Oral gavage (p.o.).
Result: Showed plasma concentration reached 1.0 mg/mL (2.6 mM) within 30 min from p.o. in mice, and it remained at 596± 134 ng/mL (1.6±0.36 mM) after 24 h, the same as in rat. Plasmic M109S was 565.3±188.3 nM in rats, and 171.0±52.0 nM in retina, 222.7±74.7 nM in brain, respectively.
分子量

375.42

Formula

C21H21N5O2

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
纯度 & 产品资料
参考文献

M190S 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
M190S
目录号:
HY-156168
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