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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Ro 31-8220 mesylate (RO31-8220; BIM IX; RO-31-8220; Bisindolylmaleimide IX; RO-318220), the mesylate salt of Ro 31-8220, is a novel and potent pan-PKC inhibitor with potential anticancer activity. It inhibits PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε with IC50s of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM, respectively.
ln Vitro |
Effective against PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, Ro 31-8220 mesylate has IC50 values of 5, 24, 14, 27, 24, and 23 nM, respectively[1]. Furthermore, Ro 31-8220 demonstrates no effect on MKK3, MKK4, MKK6, and MKK7 but significantly inhibits MAPKAP-K1b, MSK1, S6K1, and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively). Furthermore, voltage-dependent Na+ channel suppression is a direct effect of Ro 31-8220[2]. Ro 31-8220 (1 μM) inhibits the increase in phospho-PKC pan levels brought on by paraoxons, decreases the neuroprotective effects of paraoxons on cerebellar granule neurons, and suppresses the activity of caspase-3 that is triggered by paraoxons[3].
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ln Vivo |
In mice, Ro 31-8220 (6 mg/kg/d, sc) has a half-life of 5.7 hours and is well tolerated. After six weeks of therapy, MLP−/− mice treated with Ro 31-8220 exhibit a substantial rescue in fractional shortening, but WT mice show no change[4].
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Animal Protocol |
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References |
[1]. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7.
[2]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [3]. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. [4]. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82 |
Molecular Formula |
C25H23N5O2S.CH4O3S
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Molecular Weight |
553.65
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CAS # |
138489-18-6
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Related CAS # |
Ro 31-8220;125314-64-9
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SMILES |
S(/C(=N/[H])/N([H])[H])C([H])([H])C([H])([H])C([H])([H])N1C([H])=C(C2C(N([H])C(C=2C2=C([H])N(C([H])([H])[H])C3=C([H])C([H])=C([H])C([H])=C23)=O)=O)C2=C([H])C([H])=C([H])C([H])=C12.S(C([H])([H])[H])(=O)(=O)O[H]
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8062 mL | 9.0310 mL | 18.0620 mL | |
5 mM | 0.3612 mL | 1.8062 mL | 3.6124 mL | |
10 mM | 0.1806 mL | 0.9031 mL | 1.8062 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.