Rottlerin(Synonyms: Mallotoxin; NSC 56346; NSC 94525)

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Rottlerin (Synonyms: Mallotoxin; NSC 56346; NSC 94525) 纯度: 98.02%

Rottlerin 是可从 Mallotus Philippinensis 中的到的一种天然产物， 是 PKC 的一个特异性抑制剂，其对 PKCδ 的 IC50 值为 3-6 μM， PKCα，β，γ 的为 30-42 μM，PKCε，η，ζ 为 80-100 μM。Rottlerin 可作为线粒体直接解偶联剂，通过编写那个 mTOR1 上游的信号级联刺激自噬。Rottlerin 通过活化 caspase 3 诱导细胞凋亡。Rottlerin 抑制 HIV-1 整合和狂犬病病毒 (RABV) 感染。

Rottlerin(Synonyms: Mallotoxin; NSC 56346; NSC 94525)

Rottlerin Chemical Structure

CAS No. : 82-08-6

规格 价格 是否有货 数量
10 mg ￥1300 In-stock
25 mg ￥2800 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[1][2][3]. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection[4][5].

IC50 & Target[1][4]

PKCδ

3 μM (IC50, Porcine spleen)

PKCα

30 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCγ

40 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCβ

42 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCη

82 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCζ

100 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCε

100 μM (IC50, baculovirus-infected Sf9 insect cells)

CaM kinase III

5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)

CKII

30 μM (IC50, holoenzyme expressed in E.coli)

PKA

78 μM (IC50, catalytic subunit from porcine heart)

HIV-1

 

体外研究
(In Vitro)

Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC[2].
Rottlerin (20 μM) exhibits cell proliferation in HMVEC[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration: 20 μM.
Incubation Time: 2, 6, 24 hours.
Result: Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h.

Cell Proliferation Assay[2]

Cell Line: Primary HMVEC (Human Microvascular Endothelial Cell).
Concentration: 20 μM.
Incubation Time: 24/48 hours.
Result: Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively.

体内研究
(In Vivo)

Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity[3].
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×106 cells mixed with Matrigel, 50:50 ratio) injection[3].
Dosage: 0 or 20 mg/kg.
Administration: Gavage 5 days per week, once daily, for 6 weeks.
Result: Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice.

分子量

516.54

Formula

C30H28O8
CAS 号

82-08-6
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
In Vitro: 

DMSO : 50 mg/mL (96.80 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9360 mL 9.6798 mL 19.3596 mL
5 mM 0.3872 mL 1.9360 mL 3.8719 mL
10 mM 0.1936 mL 0.9680 mL 1.9360 mL

*

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 0.5% CMC-Na/saline water

    Solubility: 22 mg/mL (42.59 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.84 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.84 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.

    [2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.

    [3]. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.

    [4]. María Rosa López-Huertas, et al. Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes. J Biol Chem. 2011 Aug 5;286(31):27363-77.

    [5]. Zoé Lama, et al. Kinase inhibitors tyrphostin 9 and rottlerin block early steps of rabies virus cycle. Antiviral Res. 2019 Aug;168:51-60.

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