Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

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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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Ro 31-8220 mesylate) that retains the same biological activity.

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

Ro 31-8220 Chemical Structure

CAS No. : 125314-64-9

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Other In-stock Forms of Ro 31-8220:

Ro 31-8220 mesylate

Other Forms of Ro 31-8220:

Ro 31-8220 mesylate In-stock

11 Publications Citing Use of MCE Ro 31-8220

: 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.

: 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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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 5 nM (PKCα), 24 nM (PKCβI), 14 nM (PKCβII), 27 nM (PKCγ), 24 nM (PKCε), 23 nM (Rat brain PKC)^[1], 3 nM (MAPKAP-K1b), 8 nM (MSK1), 15 nM (S6K1), 38 nM (GSK3β)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.84 μM Compound: 4, Ro-318220	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	[PMID: 21488662]
MCF7	IC₅₀	1.96 μM Compound: Ro31-8220	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	[PMID: 23434140]
MCF7	IC₅₀	1.96 μM Compound: 4, Ro-318220	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	[PMID: 21488662]
MDA-MB-231	IC₅₀	1.77 μM Compound: 4, Ro-318220	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	[PMID: 21488662]
PC-3	IC₅₀	1.74 μM Compound: Ro31-8220	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	[PMID: 23434140]

In Vitro

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.

In Vivo

Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP^−/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

457.55

Formula

C₂₅H₂₃N₅O₂S

CAS No.

125314-64-9

SMILES

NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[4]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]

Ro 31-8220 Related Classifications

Neurological Disease Cardiovascular Disease

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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.

Keywords:

Ro 31-8220125314-64-9Bisindolylmaleimide IXPKCProtein kinase CInhibitorinhibitorinhibit

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