Rottlerin

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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。

CAS NO:

82-08-6

Mallotoxin
NSC 56346
NSC 94525

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°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 : 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 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℃, 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。