Ro 31-8220 mesylate
Based on 13 publication(s) in Google Scholar
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Ro 31-8220 mesylate can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.
For research use only. We do not sell to patients.
- Purity: 99.57%
- CAS No.: 138489-18-6
- Formula: C26H27N5O5S2
- Molecular Weight:553.65
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Epigenetics Compound Library
HY-L005
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
MAPK Compound Library
HY-L010
-
TGF-beta/Smad Compound Library
HY-L018
-
Anti-Cancer Compound Library
HY-L025
-
Reprogramming Compound Library
HY-L039
-
Oxygen Sensing Compound Library
HY-L045
-
Anti-Cardiovascular Disease Compound Library
HY-L046
-
Cytoskeleton Compound Library
HY-L060
-
Neuroprotective Compound Library
HY-L070
-
Transcription Factor-Targeted Library
HY-L090
-
Human Metabolite Library
HY-L123
-
Osteogenesis Compound Library
HY-L131
-
Cancer Stem Cells Compound Library
HY-L135
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Mitochondrial Toxicity Compound Library
HY-L155
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Multi-Target Compound Library
HY-L176
-
MCE Bioactive Compound Library
HY-L001V
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Ro 31-8220 mesylate
More- Nat Commun. 2018 Sep 11;9(1):3688. [Abstract]
- J Clin Invest. 2022 Feb 15;132(4):e150101. [Abstract]
- Food Res Int. 2026 Feb 11.
- EMBO Mol Med. 2023 Jan 11;15(1):e16373. [Abstract]
- Aging Cell. 2022 Mar;21(3):e13573. [Abstract]
- Aging Cell. 2020 Oct;19(10):e13217. [Abstract]
- Front Immunol. 2021 Feb 2:11:625542. [Abstract]
- Life Metab. 2025 Jan 29;4(2):loaf002. [Abstract]
- Biomolecules. 2022 Mar 10;12(3):426. [Abstract]
- Mol Med Rep. 2017 Nov;16(5):5924-5930. [Abstract]
- FASEB J. 2019 Feb;33(2):2435-2450. [Abstract]
- Neurogastroenterol Motil. 2020 Oct;32(10):1514-1528. [Abstract]
- bioRxiv. 2024 Jul 25.
Customer Validation & Images
-
WB
-
WB
Biological Activity
|
PKC-α 5 nM (IC50) |
PKC-βII 14 nM (IC50) |
PKC-βI 24 nM (IC50) |
PKC-ε 24 nM (IC50) |
PKC-γ 27 nM (IC50) |
Rat Brain PKC 23 nM (IC50) |
MAPKAP-K1b 3 nM (IC50) |
MSK1 8 nM (IC50) |
S6K1 15 nM (IC50) |
GSK3β 38 nM (IC50) |
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively[1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na+ channels[2]. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 138489-18-6
-
Appearance Solid
-
Molecular Weight 553.65
-
Formula C26H27N5O5S2
-
Color Yellow to orange
-
SMILES
NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N.CS(=O)(O)=O
-
Synonyms
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
Publications (13)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Exome-wide analysis identifies three low-frequency missense variants associated with pancreatic cancer risk in Chinese populations. [Abstract]2018 Sep 11;9(1):3688. PMID: 30206226
Ro 31-8220 mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2018 Sep 11;9(1):3688. [Abstract]
Levels of phosphorylated FAK and AKT are reduced by the PKN1 inhibitors. Cells are seeded in six-well plates after transfection with PKN1 inhibitors Lestaurtinib and Ro318220 or DMSO as control.
-
J Clin Invest
2022 Feb 15;132(4):e150101. PMID: 34964720 -
-
EMBO Mol Med
PGF2α facilitates pathological retinal angiogenesis by modulating endothelial FOS-driven ELR+ CXC chemokine expression. [Abstract]2023 Jan 11;15(1):e16373. PMID: 36511116 -
Aging Cell
Gamma frequency light flicker regulates amyloid precursor protein trafficking for reducing β-amyloid load in Alzheimer's disease model. [Abstract]2022 Mar;21(3):e13573. PMID: 35199454 -
Aging Cell
Testicular Lmcd1 regulates phagocytosis by Sertoli cells through modulation of NFAT1/Txlna signaling pathway. [Abstract]2020 Oct;19(10):e13217. PMID: 32840323 -
Front Immunol
CBP Bromodomain Inhibition Rescues Mice From Lethal Sepsis Through Blocking HMGB1-Mediated Inflammatory Responses. [Abstract]2021 Feb 2:11:625542. PMID: 33603756 -
Life Metab
Intermittent fasting inhibits platelet activation and thrombosis through the intestinal metabolite indole-3-propionate. [Abstract]2025 Jan 29;4(2):loaf002. PMID: 40078933 -
Biomolecules
Ketamine Improves Desensitization of µ-Opioid Receptors Induced by Repeated Treatment with Fentanyl but Not with Morphine. [Abstract]2022 Mar 10;12(3):426. PMID: 35327617 -
Mol Med Rep
2017 Nov;16(5):5924-5930. PMID: 28849166
Ro 31-8220 mesylate purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2017 Nov;16(5):5924-5930. [Abstract]
The PKC inhibitor Ro 31 8220 is used to investigate the implication of PKC mediated signaling pathways.
-
FASEB J
Bile acids induce visceral hypersensitivity via mucosal mast cell-to-nociceptor signaling that involves the farnesoid X receptor/nerve growth factor/transient receptor potential vanilloid 1 axis. [Abstract]2019 Feb;33(2):2435-2450. PMID: 30260705 -
Neurogastroenterol Motil
Acute stress induces visceral hypersensitivity via glucocorticoid receptor-mediated membrane insertion of TRPM8: Involvement of a non-receptor tyrosine kinase Pyk2. [Abstract]2020 Oct;32(10):1514-1528. PMID: 32391653 -
Solvent & Solubility
DMSO : 35.71 mg/mL (64.50 mM; Need ultrasonic; 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 2.08 mg/mL (3.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.76 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)
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.
Protocol
A neurotoxic concentration of paraoxon (200 μM) is added to the granule cell cultures for the indicated time on day in vitro (DIV) 8. The following drugs are added to the granule cell cultures prior to or after paraoxon exposure on DIV 8: Ro-81-3220 (1 μM) is added 15 min prior to or 3 h after the addition of paraoxon. TPA (0.1 μM) is added 15 min prior to the addition of paraoxon[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[4]
The affects of long-term Ro 31-8220 administration over 4 to 6 weeks in MLP−/− heart failure mice are investigated. All mice are assessed for ventricular performance by echocardiography at the beginning of the study and 6 weeks later. Ro 31-8220 (or vehicle) is injected subcutaneously once per day at a dosage of 6 mg/kg/d[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (280 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7. [Content Brief]
[2]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief]
[3]. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. [Content Brief]
[4]. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82. [Content Brief]
[5]. Beltman J, et al. The selective protein kinase C inhibitor, Ro-31-8220, inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) expression, induces c-Jun expression, and activates Jun N-terminal kinase. J Biol Chem. 1996 Oct 25;271(43):27018-24. [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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8062 mL | 9.0310 mL | 18.0620 mL | 45.1549 mL |
| 5 mM | 0.3612 mL | 1.8062 mL | 3.6124 mL | 9.0310 mL | |
| 10 mM | 0.1806 mL | 0.9031 mL | 1.8062 mL | 4.5155 mL | |
| 15 mM | 0.1204 mL | 0.6021 mL | 1.2041 mL | 3.0103 mL | |
| 20 mM | 0.0903 mL | 0.4515 mL | 0.9031 mL | 2.2577 mL | |
| 25 mM | 0.0722 mL | 0.3612 mL | 0.7225 mL | 1.8062 mL | |
| 30 mM | 0.0602 mL | 0.3010 mL | 0.6021 mL | 1.5052 mL | |
| 40 mM | 0.0452 mL | 0.2258 mL | 0.4515 mL | 1.1289 mL | |
| 50 mM | 0.0361 mL | 0.1806 mL | 0.3612 mL | 0.9031 mL | |
| 60 mM | 0.0301 mL | 0.1505 mL | 0.3010 mL | 0.7526 mL |
Ro 31-8220 mesylate Related Classifications
HY-13866 Related Classifications
Powered by Bioz