Rottlerin
Based on 23 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.45%
- No. CAS: 82-08-6
- Fòrmula: C30H28O8
- Peso molecular:516.54
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Rottlerin
More- Bioact Mater. 2026 Jun 17:65:644-662. [Abstract]
- Cell Commun Signal. 2024 Apr 2;22(1):210. [Abstract]
- Phytomedicine. 2025 Feb 21:139:156500. [Abstract]
- Adv Healthc Mater. 2025 Jan;14(3):e2402976. [Abstract]
- Food Res Int. 2026 Feb 11.
- Phytother Res. 2025 Jul 29. [Abstract]
- Free Radic Biol Med. 2026 Mar 16:246:614-626. [Abstract]
- EMBO Mol Med. 2024 Apr;16(4):1004-1026. [Abstract]
- Virol Sin. 2025 Dec 27:S1995-820X(25)00177-4. [Abstract]
- J Dairy Sci. 2025 Sep;108(9):9788-9801. [Abstract]
- Virol Sin. 2022 Oct;37(5):685-694. [Abstract]
- Microbiol Spectr. 2022 Oct 26;10(5):e0105622. [Abstract]
- J Virol. 2022 Jan 26;96(2):e0134421. [Abstract]
- J Med Virol. 2024 Apr;96(4):e29555. [Abstract]
- Mol Pharmacol. 2025 Jun;107(6):100042. [Abstract]
- Vet Microbiol. 2026 May:316:110992. [Abstract]
- PLoS One. 2025 Jun 27;20(6):e0323931. [Abstract]
- PLoS One. 2024 Dec 13;19(12):e0309624. [Abstract]
- Cartilage. 2024 Sep;15(3):315-327. [Abstract]
- bioRxiv. 2026 Feb 10.
- Res Sq. 2026 Jan 16.
- Drexel University. 2025.
- bioRxiv. 2024 August 17.
Customer Validation & Images
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Cell Imaging/Staining
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RT-PCR
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Cell Proliferation/Viability Assay
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WB
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In Vivo Efficacy Study
Actividad biológica
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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 |
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Cell Line
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Type | Value | Description | References |
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| COLO 205 | IC50 |
>20 μM
Compound: 1
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Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay
Cytotoxicity against human COLO205 cells after 48 hrs by MTT assay
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[PMID: 24041234] |
| Hep 3B2 | IC50 |
0.25 μM
Compound: 13
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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
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[PMID: 33873056] |
| HepG2 | IC50 |
>20 μM
Compound: 1
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Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
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[PMID: 24041234] |
| HL-60 | IC50 |
9 μM
Compound: 1
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Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
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[PMID: 24041234] |
| Huh-7 | IC50 |
0.57 μM
Compound: 13
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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
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[PMID: 33873056] |
| MIA PaCa-2 | IC50 |
8 μM
Compound: 1
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Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
Cytotoxicity against human MIAPaCa2 cells after 48 hrs by MTT assay
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[PMID: 24041234] |
| PC-3 | IC50 |
>20 μM
Compound: 1
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Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
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[PMID: 24041234] |
| Sf9 | IC50 |
1.9 μM
Compound: Rottlerin
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Inhibition of His-tagged human PRAK expressed in Sf9 cells
Inhibition of His-tagged human PRAK expressed in Sf9 cells
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[PMID: 10998351] |
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.
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Cell Line:Primary HMVEC (Human Microvascular Endothelial Cell).
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Concentration:20 μM.
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Incubation Time:2, 6, 24 hours.
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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.
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Cell Line:Primary HMVEC (Human Microvascular Endothelial Cell).
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Concentration:20 μM.
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Incubation Time:24/48 hours.
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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.
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.
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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].
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Dosage:0 or 20 mg/kg.
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Administration:Gavage 5 days per week, once daily, for 6 weeks.
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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
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No. CAS 82-08-6
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Appearance Solid
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Peso molecular 516.54
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Fòrmula C30H28O8
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Color Brown to reddish brown
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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
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Synonyms
Mallotoxin; NSC 56346; NSC 94525
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Structure Classification
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Initial Source
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (23)
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Journal Impact Factor
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Most Recent
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Bioact Mater
Growth plate cartilage-targeting nanoparticles for pharmacological treatment of hypochondroplasia. [Abstract]2026 Jun 17:65:644-662. PMID: 42338508 -
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 -
Adv Healthc Mater
Self-Assembled Nanoparticles with Well-Defined Oligosaccharide Promote Osteogenesis by Regulating Golgi Stress Response. [Abstract]2025 Jan;14(3):e2402976. PMID: 39618007 -
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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 -
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 -
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.
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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.
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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
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.
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Microbiol Spectr
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 -
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 -
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 -
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
2024 Dec 13;19(12):e0309624. PMID: 39671442 -
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 -
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Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 22 mg/mL (42.59 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (284 KB)
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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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
[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
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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
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