Home TGF-beta/Smad PKC inhibitor Bisindolylmaleimide IX (Ro 31-8220) Mesylate

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Bisindolylmaleimide IX (Ro 31-8220) Mesylate PKC inhibitor

Cat.No.S7207

Bisindolylmaleimide IX (Ro 31-8220 Mesylate) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1.
Bisindolylmaleimide IX (Ro 31-8220) Mesylate PKC inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 553.65

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 Function assay Inhibition of His-tagged human MSK1 expressed in Sf9 cells, IC50=0.008μM 10998351
Sf21 Function assay Inhibition of His-tagged human GSK3b expressed in Sf21 cells, IC50=0.038μM 10998351
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells over expressing RSK2 after 48 hrs by MTT assay, IC50=0.84μM 21488662
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=1.74μM 23434140
MDA-MB-231 Antiproliferative assay 48 hrs Antiproliferative activity against human MDA-MB-231 cells over expressing RSK2 after 48 hrs by MTT assay, IC50=1.77μM 21488662
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells over expressing RSK2 after 48 hrs by MTT assay, IC50=1.96μM 21488662
MCF7 Cytotoxicity assay 48 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=1.96μM 23434140
DE3 Function assay Inhibition of human full length SIRT1 expressed in DE3 cells by fluorimetric assay, IC50=25μM 19734050
A549 Function assay Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin by Western blot analysis 17149860
A549 Function assay 10 uM Inhibition of SIRT2 in A549 cells assessed as ability to induce hyperacetylation of tubulin at 10 uM by Western blot analysis 17149860
MCF7 Function assay 10 uM 16 hrs Inhibition of SIRT2 in human MCF7 cells assessed as tubulin hyperacetylation at 10 uM after 16 hrs by Western blot 20030343
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 553.65 Formula

C25H23N5O2S.CH4O3S

 Storage (From the date of receipt)
CAS No. 138489-18-6 Download SDF Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 100 mg/mL ( (180.61 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
PKCα [1]
(Cell-free assay)
5 nM
PKCβ2 [1]
(Cell-free assay)
14 nM
PKCβ1 [1]
(Cell-free assay)
24 nM
PKCε [1]
(Cell-free assay)
24 nM
PKCγ [1]
(Cell-free assay)
27 nM
In vitro
Ro 31-8220 inhibits rat brain PKC activity with IC50 of 23 nM, and does not show any high degree of selectivity between PKC-α, PKC-β, PKC-γ, and PKC-ε. [1] Ro 31-8220 also inhibits MSK1, MAPKAPK1, RSK, GSK3β and S6K1 with a potency similar to that for PKC. In addition, Ro 31-8220 inhibits voltage-dependent Na+ channels. [2] Ro 31-8220 alters cellular protein kinase C localization and potently inhibits growth of A549 and MCF-7 cells with IC50 of 0.78 μM and 0.897 μM, respectively. [3] RO 31-8220 enhances epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. [4] Ro 31-8220 significantly decreases apoE secretion from primary human macrophages by inhibiting vesicular transport of apoE to the plasma membrane without significantly affecting apoE mRNA or apoE protein levels. [5]
Kinase Assay
Assay of PKC Activity
Assay mixtures contain 0.2 mg/mL peptide-gamma, 10 μM MgCl2, 0.6 mM CaCl2, 10 μM [γ-32P]ATP, 1.25 mg/mL phosphatidylserine and 1.25 ng/mL phorbol 12-myristate 13-acetate in 20 mM Hepes (pH 7.5), 2 mM EDTA, 1 mM dithiothreitol and 0.02% (w/v) Triton X-100. Peptide-γ is a synthetic peptide, GPRPLFCRKGSLRQKW, resembling the PKC-γ pseudosubstrate site, except that a serine residue replaces the pseudosubstrate alanine, converting the peptide from an inhibitor into a substrat. The assays are started by the addition of 2.5 m-units of enzyme, incubated at 30 °C for 10 min and terminated by spotting on to P81 paper, followed by extensive washing in 75 mM orthophosphoric acid. The papers are then washed in ethanol, dried, and incorporated radioactivity is determined by liquidscintillation spectroscopy.
In vivo
In MLP−/− Mice, Ro 31-8220 (6 mg/kg/d, s.c.) results in a significant increase in cardiac contractility. [6]
References
  • https://pubmed.ncbi.nlm.nih.gov/21345315/
  • https://pubmed.ncbi.nlm.nih.gov/23288845/
  • https://pubmed.ncbi.nlm.nih.gov/16880328/

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