| Size | Price | Stock | Qty |
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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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Purity: ≥98%
Ro 31-8220 is a novel and potent 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. Ro-31-8220 displayed apoptotic effect on HL-60 cells, which was mediated by a well-characterized transduction process of apoptotic signals: i.e., mitochondrial cytochrome c efflux and the activation of caspase-3 in the cytosol. Ro-31-8220 showed the apoptotic effect on HL-60 cells, which was mediated by a well-characterized transduction process of apoptotic signals: i.e., mitochondrial cytochrome c efflux and the activation of caspase-3 in the cytosol.
| ln Vitro |
With IC50s of 5, 24, 14, 27, 24, and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε, and rat brain PKC, respectively, Ro 31-8220 is a strong inhibitor of PKC[1]. Furthermore, Ro 31-8220 strongly inhibits MSK1, S6K1, GSK3β, and MAPKAP-K1b (IC50s: 3, 8, 15, and 38 nM, respectively); MKK3, MKK4, MKK6, and MKK7 are unaffected. Moreover, voltage-dependent Na+ channels are directly suppressed by Ro 31-8220[2]. In cerebellar granule neurons, Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death, inhibits paraoxon-induced caspase-3 activity, and lowers the increase in phospho-PKC pan levels caused by paraoxon [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
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| Molecular Weight |
457.55
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| CAS # |
125314-64-9
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| Related CAS # |
Ro 31-8220 mesylate;138489-18-6
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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
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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 |
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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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1856 mL | 10.9278 mL | 21.8555 mL | |
| 5 mM | 0.4371 mL | 2.1856 mL | 4.3711 mL | |
| 10 mM | 0.2186 mL | 1.0928 mL | 2.1856 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.
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