Cat. No.: HY-18980

Rottlerin

(Synonyms: Mallotoxin; NSC 56346; NSC 94525)

22 Cited Publications

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Based on 22 publication(s) in Google Scholar

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.

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Pureté: 98.45%
CAS No.: 82-08-6
Formule: C₃₀H₂₈O₈
Masse moléculaire:516.54

Stockage:

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

Rottlerin Chemical Structure

CAS No.: 82-08-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (22)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

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

Voir tous les produits spécifiques à Isoform PKC :

Voir tous les produits spécifiques à Isoform HIV :

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]
Sf9	IC₅₀	1.9 μM Compound: Rottlerin	Inhibition of His-tagged human PRAK expressed in Sf9 cells Inhibition of His-tagged human PRAK expressed in Sf9 cells	[PMID: 10998351]

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.

Chemical Information

CAS No. 82-08-6
Appearance Solid
Masse moléculaire 516.54
Formule C₃₀H₂₈O₈
Color Brown to reddish brown
SMILES

O=C(/C=C/C1=CC=CC=C1)C2=C3C(C=CC(C)(O3)C)=C(C(CC4=C(C(C)=C(C(C(C)=O)=C4O)O)O)=C2O)O
Synonyms

Mallotoxin; NSC 56346; NSC 94525
Structure Classification
- Flavonoids
- Chalcones
- Phenols
- Polyphenols
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (22)

All RT-PCRCell Imaging/StainingWBCell Proliferation/Viability AssayIn Vivo Efficacy Study

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Journal Impact Factor

Adv Healthc Mater

Self-Assembled Nanoparticles with Well-Defined Oligosaccharide Promote Osteogenesis by Regulating Golgi Stress Response. [Abstract]

2024 Dec 1:e2402976. PMID: 39618007
Cell Commun Signal

Mitochondria-mediated ferroptosis induced by CARD9 ablation prevents MDSCs-dependent antifungal immunity. [Abstract]

2024 Apr 2;22(1):210. PMID: 38566195
Phytomedicine

Allicin alleviates traumatic brain injury-induced neuroinflammation by enhancing PKC-δ-mediated mitophagy. [Abstract]

2025 Feb 21:139:156500. PMID: 39986225
EMBO Mol Med

Organotypic culture of human brain explants as a preclinical model for AI-driven antiviral studies. [Abstract]

2024 Apr;16(4):1004-1026. PMID: 38472366

Rottlerin purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2024 Apr;16(4):1004-1026. [Abstract]

Vero E6 cells were infected for 1 or 2 days with TAHV at MOI 0.1 either non-treated (NT) or treated with 100 nM Bafilomycin A1 (Baf A1), 10 µM RG10b or 20 µM Rottlerin. Quantification of TAHV RNA, normalized by GAPDH RNA (control), was measured by RT-qPCR.

Rottlerin purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2024 Apr;16(4):1004-1026. [Abstract]

Cytotoxicity in non-infected (NI) and TAHV-infected OPAB with 10 µM RG10b or 20 µM Rottlerin treatment at 0, 2, 4, and 7 dpi.
Free Radic Biol Med

HIF-1α translation mediated by PKCδ facilitates RSV-induced production of innate inflammatory cytokines in vitro and in vivo. [Abstract]

2026 Mar 16:246:614-626. PMID: 41611036
Food Res Int

2026 Feb 11.
Phytother Res

6-Shogaol Reduces Renal Macrophage Infiltration by Targeting the STING Pathway to Alleviate Cisplatin Induced Renal Injury. [Abstract]

2025 Jul 29. PMID: 40728195
J Med Virol

Hesperetin blocks poxvirus replication with a low tendency to select for drug-resistant viral variants. [Abstract]

2024 Apr;96(4):e29555. PMID: 38546037
J Dairy Sci

Molecular docking and in vitro fermentation reveal plant-derived rottlerin targeting methyl-coenzyme M reductase to reduce enteric methane emissions from dairy cows. [Abstract]

2025 Sep;108(9):9788-9801. PMID: 40639644
Virol Sin

Development of the reverse genetics system for viral hemorrhagic septicemia virus genotype IVa and its application in antiviral compound screening. [Abstract]

2025 Dec 27:S1995-820X(25)00177-4. PMID: 41461367

Rottlerin purchased from MedChemExpress. Usage Cited in: Virol Sin. 2025 Dec 27:S1995-820X(25)00177-4. [Abstract]

Fluorescence microscopy imaging of FHM cells infected with rVHSV-EGFP after treatment with varying concentrations of Rottlerin (2, 4, 6, 8, 10 μM) to assess GFP fluorescence intensity.
Virol Sin

Rottlerin plays an antiviral role at early and late steps of Zika virus infection. [Abstract]

2022 Oct;37(5):685-694. PMID: 35934227

Rottlerin purchased from MedChemExpress. Usage Cited in: Virol Sin. 2022 Oct;37(5):685-694. [Abstract]

Treatment of Rottlerin (2.5 μM) throughout the infection showed a pronounced reduction of protein levels.

Rottlerin purchased from MedChemExpress. Usage Cited in: Virol Sin. 2022 Oct;37(5):685-694. [Abstract]

All the DMSO-treated mice died while 75% of the Rottlerin (6 mg/kg, i.p.)-treated mice survived.
Microbiol Spectr

Protein Kinase C Inhibitors Reduce SARS-CoV-2 Replication in Cultured Cells. [Abstract]

2022 Oct 26;10(5):e0105622. PMID: 36000889
J Virol

The CCCH-Type Zinc Finger Antiviral Protein Relieves Immunosuppression of T Cells Induced by Avian Leukosis Virus Subgroup J via the NLP-PKC-δ-NFAT Pathway. [Abstract]

2022 Jan 26;96(2):e0134421. PMID: 34705559
Mol Pharmacol

Bryostatins 1 and 3 inhibit TRPM8 and modify TRPM8- and TRPV1-mediated lung epithelial cell responses to a proinflammatory stimulus via protein kinase C. [Abstract]

2025 Jun;107(6):100042. PMID: 40378651
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Cartilage

PKC-δ Promotes IL-1β-Induced Apoptosis of Rat Chondrocytes and Via Activating JNK and P38 MAPK Pathways. [Abstract]

2024 Sep;15(3):315-327. PMID: 37491820
PLoS One

Proteomic and phosphoproteomic analysis of rabies pathogenesis in the clinical canine brain and identification of a kinase inhibitor as a potential repurposed antiviral agent. [Abstract]

2025 Jun 27;20(6):e0323931. PMID: 40577348
PLoS One

Screening novel antiviral compounds to treat Clostridioides difficile infections. [Abstract]

2024 Dec 13;19(12):e0309624. PMID: 39671442
bioRxiv

2026 Feb 10.
Res Sq

2026 Jan 16.
Drexel University

2025.
bioRxiv

2024 August 17.

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

Keywords

Rottlerin

22 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Rottlerin

Voir tous les produits spécifiques à Isoform PKC

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

Chemical Information

Publications (22)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Rottlerin Related Classifications

Cat. No.: HY-18980