Ro 31-8220 mesylate

Biological Activity

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.

Technical Data

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.

Background References

1. Intestinal epithelial potassium channels and CFTR chloride channels activated in ErbB tyrosine kinase inhibitor diarrhea
   T Duan, O Cil, JR Thiagaraja, AS Verkman
   JCI Insight, 2019;0(0):.
2. Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-dopamine-like G protein-coupled receptor.
   Bayliss A, Evans P
   PLoS ONE, 2013;8(11):e80833.
3. Potent, selective inhibitors of protein kinase C.
   Davis et al.
   FEBS Lett., 1989;259:61
4. Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor.
   Lingameneni et al.
   FEBS Lett., 2000;473:265
5. Specificity and mechanism of action of some commonly used protein kinase inhibitors.
   Davies et al.
   Biochem.J., 2000;351:95
6. Hypomorph mutation-directed small-molecule protein-protein interaction inducers to restore mutant SMAD4-suppressed TGF-β signaling.
   Tang et al.
   Cell Chem.Biol., 2020;S2451-9456:30473
7. RO 31-8220 activates c-Jun N-terminal kinase and glycogen synthase in rat adipocytes and L6 myotubes. Comparison to actions of Ins.
   Standaert et al.
   Endocrinology, 1999;150:2145

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