Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

Cat. No.: HY-13866A: Fiche technique Instruction de manipulation
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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. 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.

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.

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CAS No. : 125314-64-9

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Other In-stock Forms of Ro 31-8220:

Ro 31-8220 mesylate Ro 31-8220 formic

Other Forms of Ro 31-8220:

Ro 31-8220 mesylate In-stock
Ro 31-8220 formic In-stock

13 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.

Recommandations en vedette

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform PKC:

Voir toutes les isoformes

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

Voir tous les produits spécifiques à Isoform JNK:

Voir toutes les isoformes

JNK1 JNK2 JNK3 JNK

Activité biologique
Protocole
Pureté et documentation
Références
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Description

IC₅₀ & Target^[1]^[2]

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)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.84 3 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]
HCT-116	IC₅₀	0.84 3 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 3 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]
Sf9	IC₅₀	8 1 Compound: Ro-318220	Inhibition of His-tagged human MSK1 expressed in Sf9 cells Inhibition of His-tagged human MSK1 expressed in Sf9 cells	[PMID: 10998351]
Sf21	IC₅₀	38 1 Compound: Ro-318220	Inhibition of His-tagged human GSK3b expressed in Sf21 cells Inhibition of His-tagged human GSK3b expressed in Sf21 cells	[PMID: 10998351]
MCF7	IC₅₀	1.96 3 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]
MCF7	IC₅₀	1.96 3 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 3 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 3 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]
MCF7	IC₅₀	1.96 3 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]
MDA-MB-231	IC₅₀	1.77 3 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]
HCT-116	IC₅₀	0.84 3 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]
PC-3	IC₅₀	1.74 3 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]
MCF7	IC₅₀	1.96 3 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]
MCF7	IC₅₀	1.96 3 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]
MDA-MB-231	IC₅₀	1.77 3 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 3 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]
Sf21	IC₅₀	38 1 Compound: Ro-318220	Inhibition of His-tagged human GSK3b expressed in Sf21 cells Inhibition of His-tagged human GSK3b expressed in Sf21 cells	[PMID: 10998351]
Sf9	IC₅₀	8 1 Compound: Ro-318220	Inhibition of His-tagged human MSK1 expressed in Sf9 cells Inhibition of His-tagged human MSK1 expressed in Sf9 cells	[PMID: 10998351]

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.

Masse moléculaire

457.55

Formule

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

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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]

Test cellulaire ^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[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 n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[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]

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 IXPKCJNKProtein kinase Cc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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