Ro 31-8220 methanesulfonate (Synonyms: BIM IX, Ro 318220) |
| رقم الكتالوجGC10029 |
Ro 31-8220 methanesulfonate هو مثبط قوي لـ PKC ، مع IC50s من 5 و 24 و 14 و 27 و 24 و 23 نانومتر لـ PKCα ؛، PKCβ ؛ I ، PKCβ ؛ II ، PKC7777#88947 ؛، PKC& ؛ و PKC دماغ الفئران ، على التوالي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 138489-18-6
Sample solution is provided at 25 µL, 10mM.
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Ro 31-8220 mesylate is a potent PKC inhibitor, 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 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively[1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na+ channels[2]. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels[3].
Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP−/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change[4].
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.
Cell experiment: | A neurotoxic concentration of paraoxon (200 μM) is added to the granule cell cultures for the indicated time on day in vitro (DIV) 8. The following drugs are added to the granule cell cultures prior to or after paraoxon exposure on DIV 8: Ro-81-3220 (1 μM) is added 15 min prior to or 3 h after the addition of paraoxon. TPA (0.1 μM) is added 15 min prior to the addition of paraoxon[1]. |
Animal experiment: | Mice[4]The affects of long-term Ro 31-8220 administration over 4 to 6 weeks in MLP−/− heart failure mice are investigated. All mice are assessed for ventricular performance by echocardiography at the beginning of the study and 6 weeks later. Ro 31-8220 (or vehicle) is injected subcutaneously once per day at a dosage of 6 mg/kg/d[4]. |
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. | |
| Cas No. | 138489-18-6 | SDF | |
| المرادفات | BIM IX, Ro 318220 | ||
| Chemical Name | 3-(3-(5-hydroxy-4-(1-methyl-1H-indol-3-yl)-2-oxo-2H-pyrrol-3-yl)-1H-indol-1-yl)propyl carbamimidothioate methanesulfonate | ||
| Canonical SMILES | CN1C=C(C(C(O)=NC2=O)=C2C(C3=CC=CC=C34)=CN4CCCSC(N)=N)C5=CC=CC=C51.CS(O)(=O)=O | ||
| Formula | C26H27N5O5S2 | M.Wt | 553.65 |
| الذوبان | DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 20 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8062 mL | 9.031 mL | 18.062 mL |
| 5 mM | 0.3612 mL | 1.8062 mL | 3.6124 mL |
| 10 mM | 0.1806 mL | 0.9031 mL | 1.8062 mL |
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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