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Rottlerin
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Rottlerin图片
CAS NO:82-08-6
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Mallotoxin
NSC 56346
NSC 94525
产品介绍
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，通过靶向mTORC1 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。
生物活性

Rottlerin, a natural product purified fromMallotus Philippinensis, is a specificPKCinhibitor, withIC50values forPKCδof 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 stimulatesautophagyby targeting a signaling cascade upstream ofmTORC1. Rottlerin inducesapoptosisviacaspase 3activation[1][2][3]. Rottlerin inhibitsHIV-1integration andRabies 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].

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].

Animal Model:Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×106cells 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

性状

Solid

Formula

C30H28O8

CAS 号

82-08-6

结构分类
  • Flavonoids
  • Chalcones
  • Phenols
  • Polyphenols
来源
  • Plants
  • Euphorbiaceae
  • Mallotus philippensis
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL(24.20 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9360 mL9.6798 mL19.3596 mL
5 mM0.3872 mL1.9360 mL3.8719 mL
10 mM0.1936 mL0.9680 mL1.9360 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 1.25 mg/mL (2.42 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.42 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 12.5 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
  • 3.

    请依序添加每种溶剂： 10% DMSO    90%corn oil

    Solubility: ≥ 1.25 mg/mL (2.42 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。