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  1. NF-κB
  2. NF-κB
  3. Helenalin

Helenalin 是一種抗炎的倍半萜內(nèi)酯。Helenalin 通過直接靶向 p65 選擇性抑制轉(zhuǎn)錄因子 NF-κB。Helenalin 具有烷基化活性,以 NF-κB 的 p65 亞基中的半胱氨酸巰基為靶點(diǎn),從而抑制其 DNA 結(jié)合。

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Helenalin Chemical Structure

Helenalin Chemical Structure

CAS No. : 6754-13-8

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查看 NF-κB 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(In Vitro)

Helenalin (10 μM;20-120 分鐘) 在 80 分鐘后完全抑制 NF-κB DNA 結(jié)合[1]
Helenalin 是一種抗炎、抗癌的植物化學(xué)物質(zhì),是一種周期性 Skp2 積累的有效抑制劑,一種 F-box 蛋白,在 S 期進(jìn)展期間介導(dǎo) SCF E3 連接酶泛素化和兩種 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.
體內(nèi)研究
(In Vivo)

Helenalin (25 mg/kg;腹腔注射;6 至 12 小時(shí)) 對(duì)未成熟的雄性 ICR 小鼠給藥,導(dǎo)致肝臟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 號(hào)
性狀

固體

顏色

White to yellow

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 100 mg/mL (381.24 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.75%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
Helenalin
目錄號(hào):
HY-119970
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