Ro 31-8220 Mesylate

SKU: orb1300591

Description

Ro 31-8220 Mesylate is a potent, cell-permeable pan-PKC inhibitor targeting isoforms α, βI, βII, γ, and ε. It also effectively inhibits kinases MSK1, MAPKAP-K1b, S6K1, and GSK3β. This compound is widely used in vitro and in vivo to investigate PKC-mediated signaling pathways in cancer, neuroscience, and inflammation research.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 138489-18-6
• MW: 553.65
• Purity: 99.18%
• Formula: C₂₅H₂₃N₅O₂S·CH₄O₃S
• SMILES: CS(O)(=O)=O.Cn1cc(C2=C(C(=O)NC2=O)c2cn(CCCSC(N)=N)c3ccccc23)c2ccccc12
• Target: JNK,PKC
• Solubility: DMSO:55.4 mg/mL (100.06 mM);Ethanol:2.8 mg/mL (5.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.61 mM)

Bioactivity

• Target IC50:
  PKCβ2:14 nM|MAPKAP-K1b:3 nM|S6K1:15 nM|MSK1:8 nM|PKC (rat brain):23 nM|PKCα:5 nM|PKCγ:27 nM|PKCβ1:24 nM|PKCε:24 nM|GSK-3β:38 nM
• In Vivo:
  RO31-8220 effectively inhibits the growth of A549 cells (IC50: 0.78 μM) and MCF-7 cells (IC50: 0.897 μM). In platelets with low adrenergic response, RO31-8220 amplifies the phosphorylation of Akt, thereby enhancing adrenalin-induced platelet aggregation. It significantly reduces the secretion of apolipoprotein E from primary human macrophages by inhibiting the vesicular transport of the apoE gene to the plasma membrane, without significantly affecting the mRNA or protein levels of ApoE. RO31-8220 inhibits the activity of rat brain protein kinase C (IC50: 23 nM) without selectivity towards PKC-α/β/γ/ε isoforms. Additionally, RO31-8220 exerts an inhibitory effect on voltage-dependent sodium channels.
• In Vitro:
  Within MLP/mice, Ro 31-8220 (6 mg/kg/d, s.c.) significantly enhances myocardial contractility.
• Cell Research:
  Human A549 lung and MCF-7 breast carcinoma cells are obtained from the European Collection of Animal Cell Cultures. Cells (passage number 10-30) are cultured in an atmosphere of 5% carbon dioxide, the former in Ham's F-12 medium with penicillin/streptomycin, the latter in minimum essential medium (Eagle's modification) with additional pyruvate (1 mM) and non-essential amino acids. Both media are supplemented with 10% FCS and glutamine (2 mM). Cells are subcultured routinely twice weekly to maintain logarithmic growth. For cell proliferation studies cells are seeded and incubated with 3 ml of medium including agents, which is replenished at intervals of 48 h (A549) or 72 h (MCF-7). Following incubation for 4 days (A549) or 6 days (MCF-7) with drugs, cell number is assessed using a Coulter Counter Model ZM. In order to achieve PKC depletion, cells are incubated for 24 h with bryostatin 1 (1 μM). Under these conditions growth inhibition caused by bryostatin 1 is negligible. Bryostatin is removed by extensive washing of the cells followed by a 2 h recovery period. In previous work using the A549 cell line this washing procedure has been shown to eliminate bryostatin-mediated effects. The cells are then incubated for a further 24 h with staurosporine, RO 31-8220, UCN-01 or H-7. In some experiments cells are incubated with inhibitor for 48 rather than 24 h, in this case bryostation was not removed and left in the incubate. After removal of agents inhibition of DNA synthesis is evaluated by measurement of [3H]Tdr incorporation into cell. Radioactivity is counted using a Packard 1500 Tricarb scintillation counter. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Bisindolylmaleimide IX mesylate, Ro 31-8220, Ro 318220 Mesylate, Ro 31-8220 Mesylate, Ro 31-8220 methanesulfonate, Ro 31 8220 Mesylate, Protein kinase C, PKCα, PKCβ1, PKCβ2, PKCγ, PKCε, PKC

Compound Identifiers

PubChem CID

11628205