1. Autophagy GPCR/G Protein
  2. Autophagy ICMT
  3. Cysmethynil

Cysmethynil 是一种 Icmt 抑制剂(IC50 = 2.4 μM)。Cysmethynil 抑制 RAS 膜结合和EGF的信号转导。Cysmethynil 将细胞周期阻滞在 G1 期,诱导细胞自噬。Cysmethynil 抑制 PC3 细胞增殖,与 Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A) 有协同作用。Cysmethynil 具有抗肿瘤作用,可用于实体瘤 (例如前列腺癌等) 研究。

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Cysmethynil Chemical Structure

Cysmethynil Chemical Structure

CAS No. : 851636-83-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research[1][2][3].

IC50 & Target

IC50 = 2.4 μM for Icmt

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HepG2 IC50
19.3 μM
Compound: 1
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 23514631]
IMR-90 IC50
29.2 μM
Compound: 1
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
Antiproliferative activity against human IMR90 cells after 72 hrs by MTT assay
[PMID: 23514631]
MDA-MB-231 IC50
21.8 μM
Compound: 45292
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by colorimetric tetrazolium assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by colorimetric tetrazolium assay
[PMID: 20809634]
MDA-MB-231 IC50
22.1 μM
Compound: 1
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 23514631]
PC-3 IC50
21.3 μM
Compound: 1
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
[PMID: 23514631]
Sf9 IC50
1.5 μM
Compound: 45292
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H] AdoMet after 20 mins by scintillation counting
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H] AdoMet after 20 mins by scintillation counting
[PMID: 20809634]
Sf9 IC50
1.9 μM
Compound: 1
Inhibition of recombinant Icmt (unknown origin) expressed in Sf9 cells assessed as transfer of methyl group from [3H]-S-adenosylmethionine to [3H]-biotin-S-farnesyl-L-cysteine after 30 mins
Inhibition of recombinant Icmt (unknown origin) expressed in Sf9 cells assessed as transfer of methyl group from [3H]-S-adenosylmethionine to [3H]-biotin-S-farnesyl-L-cysteine after 30 mins
[PMID: 23514631]
Sf9 IC50
2.4 μM
Compound: cysmethynil
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H]-AdoMet after 20 mins by scintillation counter
Inhibition of recombinant ICMT expressed in Sf9 cells using [3H]-AdoMet after 20 mins by scintillation counter
[PMID: 21661760]
Sf9 IC50
2.4 μM
Compound: 31
Inhibition of recombinant ICMT (unknown origin) expressed in sf9 cells using biotin S-farnesyl-L-cysteine as substrate
Inhibition of recombinant ICMT (unknown origin) expressed in sf9 cells using biotin S-farnesyl-L-cysteine as substrate
[PMID: 23566315]
体外研究
(In Vitro)

Cysmethynil (15 μM or 20 μM or 30 μM; 6天) 抑制 Icmt+/+ 细胞和 Icmt-/- /ICMT 细胞增殖,不影响 Icmt-/- 细胞生长[1]
Cysmethynil (20-30 μM; 1-6 天) 抑制 PC3 细胞增殖,导致存活 PC3 细胞数量呈剂量和时间依赖性减少[2]

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

Cell Viability Assay

Cell Line: PC3 cells[2]
Concentration: 20-30 μM cysmethynil
Incubation Time: 1-6 days
Result: Resulted in a dose- and time-dependent reduction in the number of viable PC3 cells.
体内研究
(In Vivo)

Cysmethynil(100 mg/kg, 200 mg/kg; 腹腔注射;每48小时一次;28天)对小鼠体重无不良影响,会显着影响肿瘤生长,导致 G1 期细胞积聚和细胞死亡[2]
Cysmethynil(20 mg/kg; 腹腔注射;每周3次;2周;单独使用或与 Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) 联用)对小鼠无毒性,并且作为单药诱导仅中度抑制肿瘤生长,与 Paclitaxel (HY-B0015)/ Doxorubicin (HY-15142A) 联用可显着提高治疗效果,抑制肿瘤生长。Cysmethynil 在异种移植小鼠模型中使宫颈癌细胞对化疗药物敏感[3]

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

Animal Model: 6 week-old SCID mice with SiHa cells in the mice flank [3]
Dosage: 20 mg/kg (single; combination with Paclitaxel or Doxorubicin)
Administration: intraperitoneal injection; three times a week; 2 weeks
Result: Decreased in tumor size when treated with Cys alone, or Cysmethynil+Paclitaxel(HY-B0015)/Cysmethynil+ Doxorubicin(HY-15142A) .
Animal Model: SCID mice with PC3 cells in a xenograft model[2]
Dosage: 0.1 mg/g or 0.2 mg/g Cysmethynil
Administration: intraperitoneal injection; every 48 h; 28 days
Result: Decreased in tumor size when treated with both doses of cysmethynil.
分子量

376.53

Formula

C25H32N2O

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
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 (265.58 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 2.6558 mL 13.2792 mL 26.5583 mL
5 mM 0.5312 mL 2.6558 mL 5.3117 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.87%

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 2.6558 mL 13.2792 mL 26.5583 mL 66.3958 mL
5 mM 0.5312 mL 2.6558 mL 5.3117 mL 13.2792 mL
10 mM 0.2656 mL 1.3279 mL 2.6558 mL 6.6396 mL
15 mM 0.1771 mL 0.8853 mL 1.7706 mL 4.4264 mL
20 mM 0.1328 mL 0.6640 mL 1.3279 mL 3.3198 mL
25 mM 0.1062 mL 0.5312 mL 1.0623 mL 2.6558 mL
30 mM 0.0885 mL 0.4426 mL 0.8853 mL 2.2132 mL
40 mM 0.0664 mL 0.3320 mL 0.6640 mL 1.6599 mL
50 mM 0.0531 mL 0.2656 mL 0.5312 mL 1.3279 mL
60 mM 0.0443 mL 0.2213 mL 0.4426 mL 1.1066 mL
80 mM 0.0332 mL 0.1660 mL 0.3320 mL 0.8299 mL
100 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6640 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:
Cysmethynil
目录号:
HY-16160
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