1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis Epigenetics
  2. Microtubule/Tubulin Apoptosis Histone Demethylase
  3. MY-943

MY-943 是一种有效的 tubulin polymerizationLSD1 抑制剂,具有抗癌活性。 MY-943 诱导 G2/M 期阻滞和细胞凋亡,并抑制细胞迁移,可用于胃癌的研究。

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MY-943 Chemical Structure

MY-943 Chemical Structure

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2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥7819
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1 mg ¥1900
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5 mg ¥5800
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Customer Review

查看 Histone Demethylase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MY-943 is a potent tubulin polymerization and LSD1 inhibitor with anticancer activity. MY-943 induces G2/M phase arrest and apoptosis, and inhibits cell migration. MY-943 can be used for gastric cancer research[1].

体外研究
(In Vitro)

MY-943 对三种癌细胞具有抗增殖活性,MGC-803 细胞的 IC50 值为 0.019 μM,HCT-116 细胞为 0.044 μM,KYSE450 细胞为 0.030 μM[1]
MY-943(10, 20, 30 nM; 20, 40, 48, 60 h)剂量依赖性和时间依赖性抑制 MGC-803 和 SGC-7901 细胞的细胞活力[1]
MY-943(1, 5, 10 μM; 48 h)剂量依赖性地减弱 EBI 存在下 β-微管蛋白的烷基化作用,并防止 MGC-803 和 SGC-7901 细胞中 β-微管蛋白:EBI 加合物带的形成[1]
MY-943(10, 20, 30 nM; 8, 16, 24 nM; 48 h)浓度依赖性地抑制 MGC-803 和 SGC-7901 细胞中的微管蛋白聚合[1]
MY-943(10, 20, 30 nM; 8, 16, 24 nM; 48 h)剂量依赖性诱导细胞凋亡[1]
MY-943 以剂量依赖性方式下调 Bcl-2 和 Mcl-1(抗凋亡蛋白)的表达水平,并以剂量依赖性方式增加裂解的 Caspase-3 和 Caspase-7 的表达水平[1]
MY-943(10, 20, 30 nM; 8, 16, 24 nM; 48 h)剂量依赖性下调 Weel、CyclinB1 和 CDC2 的表达水平,并剂量依赖性地增加 p-组蛋白 H3,H3K4me1 和 H3K4me2 的表达水平
[1]
MY-943(10, 20, 30 nM; 8, 16, 24 nM; 48 h)有效且剂量依赖性地诱导 G2/M 期停滞[1]
MY-943(10, 20, 30 nM; 8, 16, 24 nM; 48 h)显著抑制胃癌细胞MGC-803和SGC-7901的迁移能力[1]

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

Cell Viability Assay[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM
Incubation Time: 20, 40, 48, 60 h
Result: Dose-dependently inhibited the cell viability of MGC-803 and SGC-7901 cells (10, 20, 30 nM; 48 h). Time-dependently inhibited the cell viability of MGC-803 and SGC-7901 cells (10, 20, 30 nM; 20, 40, 60 h).

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 1, 5, 10 μM
Incubation Time: 48 h
Result: Dose-dependently weakened the alkylation of β-tubulin in the presence of EBI, and prevented the formation of β-tubulin:EBI adduct band in MGC-803 and SGC-7901 cells.

Immunofluorescence[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Concentration-dependently inhibited tubulin polymerization in MGC-803 and SGC-7901 cells, thereby destroying the microtubule network.

Immunofluorescence[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: A concentration-dependently made cell nuclei brighten, shrink, and vary in size, and when the concentration was 24 nM for MGC-803 cells or 30 nM for SGC-7901 cells, the nucleus appeared broken, showing the morphological characteristics of apoptotic cells and the proportion of dead cells increased.

Cell Proliferation Assay[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Effectively and dose-dependently induced G2/M phase arrest. After the treatment with 24 nmol/L (MGC-803 cells) or 30 nmol/L (SGC-7901 cells), the percentages of G2/M phase in MGC-803 and SGC-7901 cells were 60% and 74%. While the percentages of G2/M in untreated groups were 33% (MGC-803 cells) and 32% (SGC-7901 cells), respectively.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Down-regulated the expression levels of Bcl-2 and Mcl-1 (anti-apoptotic proteins) in a dose-dependent manner, significantly increased the protein levels of cleaved Caspase-3 and Caspase-7.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Down-regulated the expression levels of the proliferation related proteins Weel and CDC2 in dose-dependent manners, thus leading to the decrease of cdc2 phosphorylation (thr161). While decreased the expression level of CyclinB1 (a G2 phase related protein), and obviously increased the expression level of p-Histone H3 (a M phase marker protein) in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: With the increase of concentrations, increased the expression levels of H3K4me1 and H3K4me2, indicating that inhibited cellular activity of LSD1 in MGC-803 and SGC-7901 cells.

Cell Migration Assay [1]

Cell Line: MGC-803 and SGC-7901 cells
Concentration: 10, 20, 30 nM for SGC-7901 cells; 8, 16, 24 nM for MGC-803 cells
Incubation Time: 48 h
Result: Exhibited significant inhibitory effects on the migratory ability of gastric cancer cells MGC-803 and SGC-7901 cells.
体内研究
(In Vivo)

MY-943(25 mg/kg/天;腹腔注射;21 天)显著抑制小鼠胃癌的生长,并大大降低小鼠肿瘤组织的重量和体积[1]

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

Animal Model: BALB/c-nu nude mice[1]
Dosage: 25 mg/kg
Administration: 25 mg/kg/day; i.p.; 21 days
Result: Significantly inhibited the growth of gastric cancer and greatly reduced the weight and volume of the tumor tissues.
分子量

612.76

Formula

C30H36N4O6S2

性状

固体

颜色

Light yellow to yellow

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
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (163.20 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 1.6320 mL 8.1598 mL 16.3196 mL
5 mM 0.3264 mL 1.6320 mL 3.2639 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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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 (4.08 mM); 澄清溶液; 超声助溶

    此方案可获得 2.5 mg/mL的澄清溶液。

    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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.08 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

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, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6320 mL 8.1598 mL 16.3196 mL 40.7990 mL
5 mM 0.3264 mL 1.6320 mL 3.2639 mL 8.1598 mL
10 mM 0.1632 mL 0.8160 mL 1.6320 mL 4.0799 mL
15 mM 0.1088 mL 0.5440 mL 1.0880 mL 2.7199 mL
20 mM 0.0816 mL 0.4080 mL 0.8160 mL 2.0400 mL
25 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6320 mL
30 mM 0.0544 mL 0.2720 mL 0.5440 mL 1.3600 mL
40 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0200 mL
50 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
60 mM 0.0272 mL 0.1360 mL 0.2720 mL 0.6800 mL
80 mM 0.0204 mL 0.1020 mL 0.2040 mL 0.5100 mL
100 mM 0.0163 mL 0.0816 mL 0.1632 mL 0.4080 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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MY-943
目录号:
HY-149249
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