Ro 31-8220 mesylate

Name: Ro 31-8220 mesylate
Brand: Tocris Bioscience
SKU: 2002

Tocris Bioscience, part of Bio-Techne | Catalog # 2002

Citations (310)

COA / SDS

Protein kinase inhibitor

Key Product Details

Description:	Protein kinase inhibitor
Alternative Names:	Bisindolylmaleimide IX
Chemical Name:	3-[3-[2,5-Dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl]-1H-indol-1-yl]propyl carbamimidothioic acid ester mesylate
Purity:	≥97% (HPLC)
Molecular Weight:	553.65

View Full Technical Details for Ro 31-8220 mesylate

Technical Data
Citations

Biological Activity for Ro 31-8220 mesylate

Ro 31-8220 mesylate is a protein kinase C inhibitor, with activity at other protein kinases (IC₅₀ values are 33, 3, 8, 15 and 38 nM for PKCα, MAPKAP-K1b, MSK1, GSK3β and S6K1 respectively). Activates JNK and glycogen synthase, and inhibits MAPK and ERK2, in rat adipocytes and L6 myotubes. Also inhibits voltage-dependent Na⁺ channels in the micromolar range. Induces protein-protein interaction between mutant SMAD4^R361H and SMAD3, leading to reactivation of dormant SMAD4^R361H-mediated transcriptional activity and restoration of TGF-β-induced tumor suppression activity in SMAD4 mutant cancer cells.

Compound Libraries for Ro 31-8220 mesylate

Ro 31-8220 mesylate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Ro 31-8220 mesylate

M. Wt	553.65
Formula	C₂₅H₂₃N₅O₂S.CH₃SO₃H
Storage	Desiccate at -20°C
Purity	≥97% (HPLC)
CAS Number	138489-18-6
PubChem ID	11628205
InChi Key	SAWVGDJBSPLRRB-UHFFFAOYSA-N
Smiles	CS(O)(=O)=O.CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CN(CCCSC(N)=N)C2=CC=CC=C12

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Ro 31-8220 mesylate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	55.37	100
	ethanol	2.77	5

Preparing Stock Solutions for Ro 31-8220 mesylate

The following data is based on the product molecular weight 553.65.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.81 mL	9.03 mL	18.06 mL
5 mM	0.36 mL	1.81 mL	3.61 mL
10 mM	0.18 mL	0.90 mL	1.81 mL
50 mM	0.04 mL	0.18 mL	0.36 mL

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References for Ro 31-8220 mesylate

References are publications that support the biological activity of the product.

Tang Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-β signaling. Cell Chem.Biol. 2020 PMID: 33326750
Standaert RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of Ins. Endocrinology 1999 PMID: 10218965
Lingameneni Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS Lett. 2000 PMID: 10812087
Davies Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 2000 PMID: 10998351
Davis Potent, selective inhibitors of protein kinase C. FEBS Lett. 1989 PMID: 2532156