Ro 31-8220 mesylate

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Cat.No. 2002 - Ro 31-8220 mesylate | C25H23N5O2S.CH3SO3H | CAS No. 138489-18-6
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)
Datasheet
Citations (3)
Literature

Biological Activity

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.

Compound Libraries

Ro 31-8220 mesylate is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 553.65. Batch specific molecular weights may vary from batch to batch due to solvent 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 0.9 mL 1.81 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Davis et al (1989) Potent, selective inhibitors of protein kinase C. FEBS Lett. 259 61 PMID: 2532156

Lingameneni et al (2000) Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor. FEBS Lett. 473 265 PMID: 10812087

Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351

Standaert et al (1999) RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of insulin. Endocrinology 150 2145 PMID:


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3 Citations for Ro 31-8220 mesylate

Citations are publications that use Tocris products. Selected citations for Ro 31-8220 mesylate include:

Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor. PLoS One 8 e80833 PMID: 24265838

Mou et al (2016) Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells Cell: Stem Cell 19 217 PMID: 27320041

Tang et al (2015) Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex. Brain 5 14099 PMID: 26370265


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