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  1. Epigenetics TGF-beta/Smad Anti-infection
  2. PKC HIV
  3. Prostratin

Prostratin 是一種天然的二萜類物質(zhì),為 PKC 的激活劑,Ki 值為 12.5 nM,同時可抑制 HIV-1 的活性。

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Prostratin Chemical Structure

Prostratin Chemical Structure

CAS No. : 60857-08-1

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查看 PKC 亞型特異性產(chǎn)品:

查看 HIV 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Prostratin, a natural terpenoid compound, is a PKC activator, with a Ki of 12.5 nM and shows inhibitory effect on HIV-1.

IC50 & TargetPKC PKC [1]

PKC

12.5 nM (Ki)

HIV-1

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
C8166 CC50
> 0.51 μM
Compound: 4, Prostratin
Cytotoxicity against human C8166 cells by MTT assay
Cytotoxicity against human C8166 cells by MTT assay
[PMID: 21534540]
KB IC50
1000 μg/mL
Compound: 11
Cytotoxicity against human KB cells by MTT assay
Cytotoxicity against human KB cells by MTT assay
[PMID: 17512094]
MT2 CC50
> 50 μM
Compound: Prostratin
Cytotoxicity against human MT2 cells by Celltiter-Glo assay
Cytotoxicity against human MT2 cells by Celltiter-Glo assay
[PMID: 28925702]
MT4 EC50
0.9 μM
Compound: 23, prostratin
Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
Antiviral activity against HIV2 ROD infected in MT4 cells assessed as cell viability after 5 days by MTT assay
[PMID: 25970561]
MT4 EC50
1.9 μM
Compound: 23, prostratin
Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
Antiviral activity against HIV1 3B infected in MT4 cells assessed as cell viability after 5 days by MTT assay
[PMID: 25970561]
Ramos IC50
0.056 μg/mL
Compound: 9
Cytotoxicity against human Ramos B cells after 72 hrs by MTT assay
Cytotoxicity against human Ramos B cells after 72 hrs by MTT assay
[PMID: 16792421]
Vero EC50
> 256 μM
Compound: 2
Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
Antiviral activity against Semliki forest virus infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
[PMID: 23215460]
Vero EC50
> 256 μM
Compound: 2
Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
Antiviral activity against Sindbis virus HRsp infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
[PMID: 23215460]
Vero EC50
2.6 μM
Compound: 2
Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
Antiviral activity against Chikungunya virus 899 infected in african green monkey Vero cells assessed as inhibition of virus-induced cytopathic effect incubated for 6 to 7 days by MTS assay
[PMID: 23215460]
Vero EC50
2.7 μM
Compound: 23, prostratin
Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
Antiviral activity against chikungunya virus Indian ocean strain 899 infected in Vero cells assessed as virus-induced cytopathic effect after 6 to 7 days
[PMID: 25970561]
Vero CC50
79 μM
Compound: 2
Cytotoxicity against african green monkey Vero cells by MTS assay
Cytotoxicity against african green monkey Vero cells by MTS assay
[PMID: 23215460]
Vero CC50
79 μM
Compound: Prostratin
Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method
Cytotoxicity against African green monkey Vero cells assessed as morphological changes by microscopic method
[PMID: 28925702]
體外研究
(In Vitro)

Prostratin 抑制 [3H]PDBu 與 CEM 細胞的結(jié)合,Ki 為 210 nM[1]。
Prostratin (125-1000 nM) 劑量依賴性地抑制急性髓性白血病 (AML) 細胞系 (HL-60、NB4 和 U937 細胞) 的生長。Prostratin (125-100 nM) 誘導 AML 細胞的 G1 期阻滯并影響 HL-60 細胞中的細胞周期相關(guān)分子 (pRb 磷酸化、CDK 和 p21)。Prostratin 還通過激活 PKC 導致 AML 細胞系分化。此外,MEK/ERK/MAP 信號通路的 PKC 依賴性激活需要 Prostratin 誘導的分化[2]。
Prostratin 誘導需要 PKD3 活性形式的 HIV-1 轉(zhuǎn)錄激活。Prostratin 還通過新型 PKC 亞家族的 PKCε 激活 PKD3[3]。

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

Cell Viability Assay[2]

Cell Line: HL-60, NB4 and U937 cells
Concentration: 125 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Dose-dependently inhibited the growth of acute myeloid leukemia (AML) cell lines.

Cell Cycle Analysis[2]

Cell Line: HL-60, NB4 and U937 cells
Concentration: 125 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 24 hours
Result: Induced a G0/G1 phase accumulation in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: HL-60 cells
Concentration: 125 nM, 250 nM, 500 nM, 1000 nM
Incubation Time: 24 hours
Result: Affected the cell-cycle-related molecules (pRb phosphorylation, CDKs, and p21) in HL-60 cells.
分子量

390.47

Formula

C22H30O6

CAS 號
性狀

固體

顏色

White to off-white

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 50 mg/mL (128.05 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5610 mL 12.8051 mL 25.6102 mL
5 mM 0.5122 mL 2.5610 mL 5.1220 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
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;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (3.20 mM); 澄清溶液

    此方案可獲得 ≥ 1.25 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 12.5 mg/mL 的澄清 DMSO 儲備液加到 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

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

    Solubility: ≥ 1.25 mg/mL (3.20 mM); 澄清溶液

    此方案可獲得 ≥ 1.25 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 12.5 mg/mL 的澄清 DMSO 儲備液加到 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。
動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動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 2%。
方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,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)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲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: 99.80%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(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 2.5610 mL 12.8051 mL 25.6102 mL 64.0254 mL
5 mM 0.5122 mL 2.5610 mL 5.1220 mL 12.8051 mL
10 mM 0.2561 mL 1.2805 mL 2.5610 mL 6.4025 mL
15 mM 0.1707 mL 0.8537 mL 1.7073 mL 4.2684 mL
20 mM 0.1281 mL 0.6403 mL 1.2805 mL 3.2013 mL
25 mM 0.1024 mL 0.5122 mL 1.0244 mL 2.5610 mL
30 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
40 mM 0.0640 mL 0.3201 mL 0.6403 mL 1.6006 mL
50 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2805 mL
60 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
80 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL
100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6403 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:
Prostratin
目錄號:
HY-107421
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