Ro 31-8220
Based on 13 publication(s) in Google Scholar
Ro 31-8220 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 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.
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- CAS No.: 125314-64-9
- 화학식: C25H23N5O2S
- 분자량:457.55
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ro 31-8220
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
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WB
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WB
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.84 μM
Compound: 4, Ro-318220
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Antiproliferative activity against human HCT116 cells over expressing RSK2 after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells over expressing RSK2 after 48 hrs by MTT assay
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[PMID: 21488662] |
| MCF7 | IC50 |
1.96 μM
Compound: 4, Ro-318220
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Antiproliferative activity against human MCF7 cells over expressing RSK2 after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells over expressing RSK2 after 48 hrs by MTT assay
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[PMID: 21488662] |
| MCF7 | IC50 |
1.96 μM
Compound: Ro31-8220
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Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 23434140] |
| MDA-MB-231 | IC50 |
1.77 μM
Compound: 4, Ro-318220
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Antiproliferative activity against human MDA-MB-231 cells over expressing RSK2 after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells over expressing RSK2 after 48 hrs by MTT assay
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[PMID: 21488662] |
| PC-3 | IC50 |
1.74 μM
Compound: Ro31-8220
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Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 23434140] |
| Sf21 | IC50 |
38 nM
Compound: Ro-318220
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Inhibition of His-tagged human GSK3b expressed in Sf21 cells
Inhibition of His-tagged human GSK3b expressed in Sf21 cells
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[PMID: 10998351] |
| Sf9 | IC50 |
8 nM
Compound: Ro-318220
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Inhibition of His-tagged human MSK1 expressed in Sf9 cells
Inhibition of His-tagged human MSK1 expressed in Sf9 cells
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[PMID: 10998351] |
Ro 31-8220 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
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CAS No. 125314-64-9
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분자량 457.55
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화학식 C25H23N5O2S
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SMILES
NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N
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Synonyms
Bisindolylmaleimide IX
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (13)
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Journal Impact Factor
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Most Recent
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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 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.
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J Clin Invest
2022 Feb 15;132(4):e150101. PMID: 34964720 -
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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 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.
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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 -
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.
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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