Ro 31-8220 mesylate
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
Biological ActivityRo 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.
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.
Potent, selective inhibitors of protein kinase C.
Davis et al.
FEBS Lett., 1989;259:61
Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor.
Lingameneni et al.
FEBS Lett., 2000;473:265
Specificity and mechanism of action of some commonly used protein kinase inhibitors.
Davies et al.
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
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.
Citations for Ro 31-8220 mesylate
The citations listed below are publications that use Tocris products. Selected citations for Ro 31-8220 mesylate include:
6 Citations: Showing 1 - 6
Organic barn dust inhibits surfactant protein D production through protein kinase-c alpha dependent increase of GPR116
Authors: Schneberger Et al.
PLoS One 2018;13:e0208597
Dual SMAD Signaling Inhibition Enables Long-Term Expansion of Diverse Epithelial Basal Cells
Authors: Mou Et al.
Cell: Stem Cell 2016;19:217
Cocaine-seeking is associated with PKC-dependent reduction of excitatory signaling in accumbens shell D2 DA receptor-expressing neurons.
Authors: Ortinski Et al.
Modulation of AMPA receptor mediated current by nicotinic acetylcholine receptor in layer I neurons of rat prefrontal cortex.
Authors: Tang Et al.
A kinase inhibitor screen reveals protein kinase C-dependent endocytic recycling of ErbB2 in breast cancer cells.
Authors: Bailey Et al.
J Biol Chem 2014;289:30443
Characterisation of AmphiAmR11, an amphioxus (Branchiostoma floridae) D2-DA-like G protein-coupled receptor.
Authors: Bayliss and Evans
PLoS One 2013;8:e80833
No product specific FAQs exist for this product, however you mayView all Small Molecule FAQs
Reviews for Ro 31-8220 mesylate
There are currently no reviews for this product. Be the first to review Ro 31-8220 mesylate and earn rewards!
Have you used Ro 31-8220 mesylate?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image