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Ro 31-8220 Mesylate
CAS No. 138489-18-6
Ro 31-8220 Mesylate( RO31-8220 | RO318220 | RO-318220 )
Catalog No. M17271 CAS No. 138489-18-6
Ro 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 136 | In Stock |
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| 2MG | 59 | In Stock |
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| 5MG | 93 | In Stock |
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| 10MG | 154 | In Stock |
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| 25MG | 243 | In Stock |
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| 50MG | 330 | In Stock |
|
| 100MG | 490 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameRo 31-8220 Mesylate
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NoteResearch use only, not for human use.
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Brief DescriptionRo 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.
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DescriptionRo 31-8220 is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%. 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. Moreover, the ability of Ro-31-8220 to induce apoptotic activation was completely inhibited by the over-expression of the apoptotic suppressor gene, Bcl-2, in the cells.
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In VitroRo 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. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na+ channels. 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.
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In VivoRo 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.
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SynonymsRO31-8220 | RO318220 | RO-318220
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PathwayOthers
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TargetOther Targets
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RecptorPKCα| PKCβ1| PKCβ2| PKCγ| PKCε
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number138489-18-6
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Formula Weight553.65
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Molecular FormulaC25H23N5O2S·CH4O3S
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 50 mg/mL. 90.31 mM; H2O : < 0.1 mg/mL
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SMILESCn1cc(c2ccccc12)C1=C(C(=O)NC1=O)c1cn(c2ccccc12)CCCSC(=N)N.CS(=O)(=O)O
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Chemical Name3-(3-(4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-1H-indol-1-yl)propyl carbamimidothioate methanesulfonate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Wilkinson SE, et al. Biochem J. 1993, 294 ( Pt 2), 335-337.
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