1. NF-κB
  2. NF-κB
  3. Helenalin

Helenalin 是一种抗炎的倍半萜内酯。Helenalin 通过直接靶向 p65 选择性抑制转录因子 NF-κB。Helenalin 具有烷基化活性,以 NF-κB 的 p65 亚基中的半胱氨酸巯基为靶点,从而抑制其 DNA 结合。

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Helenalin Chemical Structure

Helenalin Chemical Structure

CAS No. : 6754-13-8

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查看 NF-κB 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

Helenalin is an anti-inflammatory sesquiterpene lactone. Helenalin selectively inhibits transcription factor NF-κB by directly targeting p65. Helenalin has alkylating activity, targets the cysteine sulfhydryl groups in the p65 subunit of NF-κB, thereby inhibits its DNA binding[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
0.8 μM
Compound: helenalin
Cytotoxicity against human A431 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human A431 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
A-431 IC50
0.9 μM
Compound: helenalin
Cytotoxicity against human A431 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human A431 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
A-431 IC50
0.9 μM
Compound: helenalin
Cytotoxicity against human A431 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human A431 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
HCT-15 IC50
0.29 μM
Compound: Helenalin
Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human HCT15 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22574648]
HeLa EC50
0.7 μM
Compound: Helenalin
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 28958621]
HEp-2 ED50
0.08 μg/mL
Compound: 1
Cytotoxicity against human Hep2 cells assessed as growth inhibition by microtiter method
Cytotoxicity against human Hep2 cells assessed as growth inhibition by microtiter method
[PMID: 671468]
HEp-2 ED50
0.08 μg/mL
Compound: 1
Cytotoxicity against human Hep2 cells assessed a growth inhibition by rapid microtiter technique
Cytotoxicity against human Hep2 cells assessed a growth inhibition by rapid microtiter technique
[PMID: 691008]
HEp-2 IC50
0.8 μM
Compound: helenalin
Cytotoxicity against human HEP2 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human HEP2 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
HEp-2 IC50
0.9 μM
Compound: helenalin
Cytotoxicity against human HEP2 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human HEP2 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
HEp-2 IC50
0.9 μM
Compound: helenalin
Cytotoxicity against human HEP2 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human HEP2 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
HL-60 IC50
0.32 μM
Compound: helenalin
Cytotoxicity against human HL-60 cells after 5 hrs by MTT assay
Cytotoxicity against human HL-60 cells after 5 hrs by MTT assay
[PMID: 10425121]
HL-60 IC50
0.7 μM
Compound: helenalin
Cytotoxicity against human HL60 after 20 hrs by WST1 assay
Cytotoxicity against human HL60 after 20 hrs by WST1 assay
[PMID: 16499337]
HL-60 IC50
4 μM
Compound: Helenalin
Inhibition of telomerase in human HL60 cells by TRAP assay
Inhibition of telomerase in human HL60 cells by TRAP assay
10.1039/C0MD00241K
Jurkat IC50
0.46 μM
Compound: helenalin
Cytotoxicity against human Jurkat T cells after 20 hrs by WST1 assay
Cytotoxicity against human Jurkat T cells after 20 hrs by WST1 assay
[PMID: 16499337]
Jurkat IC50
4 μM
Compound: Helenalin
Inhibition of telomerase in human Jurkat cells by TRAP assay
Inhibition of telomerase in human Jurkat cells by TRAP assay
10.1039/C0MD00241K
K562 IC50
0.28 μM
Compound: Helenalin
Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human K562 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22574648]
MCF7 IC50
0.5 μM
Compound: helenalin
Cytotoxicity against human MCF7 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human MCF7 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
MCF7 IC50
0.7 μM
Compound: helenalin
Cytotoxicity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human MCF7 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
MCF7 IC50
0.8 μM
Compound: helenalin
Cytotoxicity against human MCF7 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human MCF7 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
OVCAR-3 IC50
1.4 μM
Compound: helenalin
Cytotoxicity against human OVCAR-3 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human OVCAR-3 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
OVCAR-3 IC50
1.6 μM
Compound: helenalin
Cytotoxicity against human OVCAR-3 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human OVCAR-3 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
OVCAR-3 IC50
1.7 μM
Compound: helenalin
Cytotoxicity against human OVCAR-3 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human OVCAR-3 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SK-LU-1 IC50
0.21 μM
Compound: Helenalin
Cytotoxicity against human SKLU1 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human SKLU1 cells assessed as growth inhibition after 48 hrs by SRB assay
[PMID: 22574648]
SK-MEL-28 IC50
0.5 μM
Compound: helenalin
Cytotoxicity against human SK MEL28 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SK MEL28 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SK-MEL-28 IC50
0.9 μM
Compound: helenalin
Cytotoxicity against human SK MEL28 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SK MEL28 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SK-MEL-28 IC50
1.3 μM
Compound: helenalin
Cytotoxicity against human SK MEL28 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SK MEL28 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SW872 IC50
1.2 μM
Compound: helenalin
Cytotoxicity against human SW872 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SW872 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SW872 IC50
1.2 μM
Compound: helenalin
Cytotoxicity against human SW872 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SW872 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
SW872 IC50
1.4 μM
Compound: helenalin
Cytotoxicity against human SW872 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human SW872 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
ZR-75-1 IC50
0.7 μM
Compound: helenalin
Cytotoxicity against human ZR-75-1 cells after 24 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human ZR-75-1 cells after 24 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
ZR-75-1 IC50
0.8 μM
Compound: helenalin
Cytotoxicity against human ZR-75-1 cells after 48 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human ZR-75-1 cells after 48 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
ZR-75-1 IC50
1.1 μM
Compound: helenalin
Cytotoxicity against human ZR-75-1 cells after 72 hrs by [3H]thymidine incorporation assay
Cytotoxicity against human ZR-75-1 cells after 72 hrs by [3H]thymidine incorporation assay
[PMID: 10425121]
体外研究
(In Vitro)

Helenalin (10 μM;20-120 分钟) 在 80 分钟后完全抑制 NF-κB DNA 结合[1]
Helenalin 是一种抗炎、抗癌的植物化学物质,是一种周期性 Skp2 积累的有效抑制剂,一种 F-box 蛋白,在 S 期进展期间介导 SCF E3 连接酶泛素化和两种 CKI 的降解[3]

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

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 10 μM
Incubation Time: 20-120 minutes
Result: Caused complete inhibition of NF-κB DNA binding after 80 minutes.
体内研究
(In Vivo)

Helenalin (25 mg/kg;腹腔注射;6 至 12 小时) 对未成熟的雄性 ICR 小鼠给药,导致肝脏谷胱甘肽水平迅速下降[2]

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

Animal Model: Immature male ICR mice[2]
Dosage: 25 mg/kg
Administration: i.p.; 6 to 12 hours
Result: Caused a rapid decrease in hepatic glutathione levels.
分子量

262.30

Formula

C15H18O4

CAS 号
性状

固体

颜色

White to yellow

结构分类
初始来源
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 (381.24 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 3.8124 mL 19.0621 mL 38.1243 mL
5 mM 0.7625 mL 3.8124 mL 7.6249 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: 99.75%

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 3.8124 mL 19.0621 mL 38.1243 mL 95.3107 mL
5 mM 0.7625 mL 3.8124 mL 7.6249 mL 19.0621 mL
10 mM 0.3812 mL 1.9062 mL 3.8124 mL 9.5311 mL
15 mM 0.2542 mL 1.2708 mL 2.5416 mL 6.3540 mL
20 mM 0.1906 mL 0.9531 mL 1.9062 mL 4.7655 mL
25 mM 0.1525 mL 0.7625 mL 1.5250 mL 3.8124 mL
30 mM 0.1271 mL 0.6354 mL 1.2708 mL 3.1770 mL
40 mM 0.0953 mL 0.4766 mL 0.9531 mL 2.3828 mL
50 mM 0.0762 mL 0.3812 mL 0.7625 mL 1.9062 mL
60 mM 0.0635 mL 0.3177 mL 0.6354 mL 1.5885 mL
80 mM 0.0477 mL 0.2383 mL 0.4766 mL 1.1914 mL
100 mM 0.0381 mL 0.1906 mL 0.3812 mL 0.9531 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:
Helenalin
目录号:
HY-119970
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