BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220]
Ro 31-8220 Mesylate
CAS: 138489-18-6
Molecular Formula: C25H23N5O2S
BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220] - Names and Identifiers
BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220] - Physico-chemical Properties
| Molecular Formula | C25H23N5O2S |
| Molar Mass | 457.55 |
| Appearance | Red solid |
| Storage Condition | 2-8°C |
| In vitro study | Ro 31-8220 mesylate is a potent PKC inhibitor, with IC 50 s 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 (IC 50 s, 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. |
| In vivo study | 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. |
BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220] - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.806 ml | 9.031 ml | 18.062 ml |
| 5 mM | 0.361 ml | 1.806 ml | 3.612 ml |
| 10 mM | 0.181 ml | 0.903 ml | 1.806 ml |
| 5 mM | 0.036 ml | 0.181 ml | 0.361 ml |
Last Update：2024-01-02 23:10:35
BisindolylMaleiMide IX . Methansulfonate [Ro 31-8220] - Reference Information
| biological activity | Ro 31-8220 mesylate is an effective PKC inhibitor, inhibiting PKCα,PKCβ I,PKCβ II,PKCγ,PKCε and rat brain PKC with IC50 values of 5,24,14,27,24 and 23 nM, it can also inhibit MAPKAP-K1b,MSK1,S6K1 and GSK3β,IC50 is 3,8,15,38 nM. |
| target | PKC-α 5 nM (IC 50 ) PKC-β I 24 nM (IC 50 ) PKC-β II 14 nM (IC 50 ) PKC-γ 27 nM (IC 50 ) PKC-ε 24 nM (IC 50 ) Rat Brain PKC 23 nM (IC 50 ) MAPKAP-K1b 3 nM (IC 50 ) MSK1 8 nM (IC 50 ) S6K1 15 nM (IC 50 ) GSK3 β 38 nM (IC 50 ) |
| in vitro study | Ro 31-8220 mesylate is a potent PKC inhibitor, with IC 50 s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβ I, PKCβ II, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC 50 s, 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. |
| in vivo study | 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. |
Last Update：2024-04-09 20:52:54
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Product Name: Ro 31-8220 Mesylate Visit Supplier Webpage Request for quotationCAS: 138489-18-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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