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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 SMAD4R361H and SMAD3, leading to reactivation of dormant SMAD4R361H-mediated transcriptional activity and restoration of TGF-β-induced tumor suppression activity in SMAD4 mutant cancer cells.
Ro 31-8220 mesylate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Desiccate at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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||0.9 mL||1.81 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
References are publications that support the biological activity of the product.
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 Ins. Endocrinology 150 2145 PMID: 10218965
Tang et al (2020) Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-β signaling. Cell Chem.Biol. S2451-9456 30473 PMID: 33326750
If you know of a relevant reference for Ro 31-8220 mesylate, please let us know.
Keywords: Ro 31-8220 mesylate, Ro 31-8220 mesylate supplier, Protein, kinases, inhibitors, inhibits, Broad, Spectrum, Ro31-8220, mesylate, protein-protein, interaction, inducers, induces, SMAD4, SMAD3, TGF-beta, TGF-B, TGF-β, Bisindolylmaleimide, IX, Kinase, Inhibitors, Receptors, 2002, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Ro 31-8220 mesylate include:
Ortinski et al (2015) Cocaine-seeking is associated with PKC-dependent reduction of excitatory signaling in accumbens shell D2 DA receptor-expressing neurons. Neuropharmacology 92 80 PMID: 25596492
Bayliss and Evans (2013) Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-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
Schneberger et al (2018) Organic barn dust inhibits surfactant protein D production through protein kinase-c alpha dependent increase of GPR116 PLoS One 13 e0208597 PMID: 30543664
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
Bailey et al (2014) A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells. J Biol Chem 289 30443 PMID: 25225290
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