Rottlerin - CAS:82-08-6

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

目录号 : KM18863 CAS No. : 82-08-6 纯度 : 96%

Data Sheet 产品使用指南

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。

规格	价格	是否有货	数量
10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock

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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. Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection.

体外研究

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

Western Blot Analysis

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

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

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.
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP).

Animal Model:	Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10 cells mixed with Matrigel, 50:50 ratio) injection.
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.

分子式

C₃₀H₂₈O₈

分子量

516.54

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 : 2 mg/mL (3.87 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	---	---	---
10 mM	---	---	---

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

科研文献

•J Virol. 2021 Oct 27;JVI0134421.

纯度： 96%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

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分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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Other Forms of Rapamycin:

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The molarity calculator equation

The dilution calculator equation