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

Name: Rottlerin
Brand: MedChemExpress
SKU: HY-18980
Rating: 5.0 (9 reviews)

Cat. No.: HY-18980 Purity: 98.09%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Rottlerin Chemical Structure

CAS No. : 82-08-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 48	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 48	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 42	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 143	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 9 publication(s) in Google Scholar

9 Publications Citing Use of MCE Rottlerin

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

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

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	IC₅₀	> 20 μM Compound: 1	Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay	[PMID: 24041234]
Hep 3B2	IC₅₀	0.25 μM Compound: 13	Anticancer activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay Anticancer activity against human Hep3B cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay	[PMID: 33873056]
HepG2	IC₅₀	> 20 μM Compound: 1	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 24041234]
HL-60	IC₅₀	9 μM Compound: 1	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 24041234]
Huh-7	IC₅₀	0.57 μM Compound: 13	Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation incubated for 4 days by MTS assay	[PMID: 33873056]
MIA PaCa-2	IC₅₀	8 μM Compound: 1	Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay	[PMID: 24041234]
PC-3	IC₅₀	> 20 μM Compound: 1	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 24041234]

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].

MedChemExpress (MCE) 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.

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].

MedChemExpress (MCE) 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.

Molecular Weight

516.54

Formula

C₃₀H₂₈O₈

CAS No.

82-08-6

Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C(C1=C2C(C=CC(C)(C)O2)=C(O)C(CC3=C(O)C(C)=C(O)C(C(C)=O)=C3O)=C1O)/C=C/C4=CC=CC=C4

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (24.20 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.42 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.42 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 22 mg/mL (42.59 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.09%

Select Batch:

Data Sheet (286 KB) SDS (393 KB)

COA (256 KB) HNMR (279 KB) RP-HPLC (244 KB) MS (184 KB)

Handling Instructions (2659 KB)

References

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

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

[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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9360 mL	9.6798 mL	19.3596 mL	48.3990 mL
	5 mM	0.3872 mL	1.9360 mL	3.8719 mL	9.6798 mL
	10 mM	0.1936 mL	0.9680 mL	1.9360 mL	4.8399 mL
	15 mM	0.1291 mL	0.6453 mL	1.2906 mL	3.2266 mL
	20 mM	0.0968 mL	0.4840 mL	0.9680 mL	2.4199 mL

Rottlerin Related Classifications

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

Customer Review

9 Publications Citing Use of MCE Rottlerin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All HIV Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

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Complete Stock Solution Preparation Table

Rottlerin Related Classifications

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

Customer Review

Rottlerin Related Antibodies

9 Publications Citing Use of MCE Rottlerin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PKC Isoform Specific Products:

View All HIV Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Rottlerin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rottlerin Related Classifications

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Your Recently Viewed Products:

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