Ro 31-8220 mesylate (Synonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate)

Name: Ro 31-8220 mesylate
Brand: MedChemExpress
SKU: HY-13866
Rating: 5.0 (13 reviews)

Cat. No.: HY-13866 Purity: 99.57%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Ro 31-8220 mesylate Chemical Structure

CAS No. : 138489-18-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 218	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 218	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 127	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 198	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Ro 31-8220 mesylate:

Ro 31-8220 Get quote

11 Publications Citing Use of MCE Ro 31-8220 mesylate

: 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.

: 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.

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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

In Vitro

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.

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

553.65

Formula

C₂₆H₂₇N₅O₅S₂

CAS No.

138489-18-6

Appearance

Solid

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

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)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8062 mL	9.0310 mL	18.0620 mL
5 mM	0.3612 mL	1.8062 mL	3.6124 mL
10 mM	0.1806 mL	0.9031 mL	1.8062 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.57%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (255 KB) LCMS (96 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]

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]

Complete Stock Solution Preparation Table

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

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 31-8220138489-18-6Bisindolylmaleimide IXPKCProtein kinase CInhibitorinhibitorinhibit

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Ro 31-8220 mesylate (Synonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate)

Customer Review

Other Forms of Ro 31-8220 mesylate:

Ro 31-8220 mesylate Related Antibodies

11 Publications Citing Use of MCE Ro 31-8220 mesylate

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ro 31-8220 mesylate Related Antibodies

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Complete Stock Solution Preparation Table

Ro 31-8220 mesylate Related Classifications

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