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  1. MAPK/ERK Pathway NF-κB Metabolic Enzyme/Protease
  2. Ribosomal S6 Kinase (RSK) Keap1-Nrf2 Endogenous Metabolite
  3. Carnosol

Carnosol 是一種有效的核糖體S6激酶 (RSK2) 抑制劑,可用于胃癌相關(guān)研究,其 IC50 值約為 5.5 μM。Carnosol 是一種 Nrf2 激活劑,增加 Nrf2 的水平以及能促進(jìn)血紅素氧合酶 1 (HMOX1) 的表達(dá)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Carnosol Chemical Structure

Carnosol Chemical Structure

CAS No. : 5957-80-2

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Other Forms of Carnosol:

查看 Ribosomal S6 Kinase (RSK) 亞型特異性產(chǎn)品:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM[1]. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1)[2][3].

IC50 & Target[1][2]

RSK2

~5.5 μM (IC50)

Nrf2

 

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A2780 GI50
3.6 μM
Compound: 2
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
Cytotoxicity against human A2780 cells after 48 hrs by SRB assay
[PMID: 17190465]
A549 IC50
> 60 μM
Compound: 1
Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay
Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
A549 IC50
47 μM
Compound: 1
Cytotoxicity against human A549 cells at exponential phase of growth after 48 hrs by MTT assay
Cytotoxicity against human A549 cells at exponential phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
A549 IC50
5 μM
Compound: 7
Inhibition of microsomal PGES1 in ILbeta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
Inhibition of microsomal PGES1 in ILbeta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis
10.1039/C5MD00278H
HBL-100 GI50
3.9 μM
Compound: 2
Cytotoxicity against human HBL100 cells after 48 hrs by SRB assay
Cytotoxicity against human HBL100 cells after 48 hrs by SRB assay
[PMID: 17190465]
HeLa IC50
> 60 μM
Compound: 1
Cytotoxicity against human HeLa cells at exponential phase of growth after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells at exponential phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
HeLa IC50
43.9 μM
Compound: 1
Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
MCF7 IC50
40.9 μM
Compound: 1
Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
MCF7 IC50
44.5 μM
Compound: 1
Cytotoxicity against human sMCF7 cells at exponential phase of growth after 48 hrs by MTT assay
Cytotoxicity against human sMCF7 cells at exponential phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
SW1573 GI50
10 μM
Compound: 2
Cytotoxicity against human SW1573 cells after 48 hrs by SRB assay
Cytotoxicity against human SW1573 cells after 48 hrs by SRB assay
[PMID: 17190465]
T47D GI50
24 μM
Compound: 2
Cytotoxicity against human T47D cells after 48 hrs by SRB assay
Cytotoxicity against human T47D cells after 48 hrs by SRB assay
[PMID: 17190465]
Vero IC50
> 60 μM
Compound: 1
Cytotoxicity against african green monkey Vero cells at lag phase of growth after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells at lag phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
Vero IC50
51.5 μM
Compound: 1
Cytotoxicity against african green monkey Vero cells at exponential phase of growth after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells at exponential phase of growth after 48 hrs by MTT assay
[PMID: 19711987]
WiDr GI50
26 μM
Compound: 2
Cytotoxicity against human WiDr cells after 48 hrs by SRB assay
Cytotoxicity against human WiDr cells after 48 hrs by SRB assay
[PMID: 17190465]
體外研究
(In Vitro)

It is showed that carnosol has no cytotoxic effects on GES1 cells and 10 μM carnosol strongly suppresses RSK2 activity, but has little effect on any other kinase. Carnosol exerts strong dose-dependent inhibitory effects against RSK2 autophosphorylation and phosphorylation of its substrate ATF1[1].

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

體內(nèi)研究
(In Vivo)

Results indicate that Carnosol significantly decreaseS the volume and weight of gastric tumors relative to the vehicle-treated group. Additionally, mice tolerate treatment with carnosol without significant loss of body weight similar to the vehicle-treated group. The phosphorylation of CREB, a direct downstream protein of RSK2, Is strongly inhibited in the carnosol-treated group but the expression of total CREB is relatively unchanged[1].

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

分子量

330.42

Formula

C20H26O4

CAS 號(hào)
性狀

固體

顏色

White to off-white

中文名稱

鼠尾草酚

結(jié)構(gòu)分類
初始來(lái)源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式
Powder -20°C 3 years

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 50 mg/mL (151.32 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 3.0265 mL 15.1323 mL 30.2645 mL
5 mM 0.6053 mL 3.0265 mL 6.0529 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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

  • 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)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.30 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.30 mM); 澄清溶液

    此方案可獲得 ≥ 2.08 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
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(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.90%

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;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0265 mL 15.1323 mL 30.2645 mL 75.6613 mL
5 mM 0.6053 mL 3.0265 mL 6.0529 mL 15.1323 mL
10 mM 0.3026 mL 1.5132 mL 3.0265 mL 7.5661 mL
15 mM 0.2018 mL 1.0088 mL 2.0176 mL 5.0441 mL
20 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7831 mL
25 mM 0.1211 mL 0.6053 mL 1.2106 mL 3.0265 mL
30 mM 0.1009 mL 0.5044 mL 1.0088 mL 2.5220 mL
40 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8915 mL
50 mM 0.0605 mL 0.3026 mL 0.6053 mL 1.5132 mL
60 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2610 mL
80 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
100 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7566 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:
Carnosol
目錄號(hào):
HY-N0643
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