133053-19-7
133053-19-7 structure
- Name: Go 6983
- Chemical Name: 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
- CAS Number: 133053-19-7
- Molecular Formula: C26H26N4O3
- Molecular Weight: 442.510
- Catalog: Biochemical Inhibitor TGF-beta/Smad signaling pathway inhibitor (TGF-beta/Smad) PKC inhibitor
- Create Date: 2018-12-12 16:14:37
- Modify Date: 2024-01-03 16:06:51
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Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
| Name | 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione |
|---|---|
| Synonyms |
3-{1-[3-(Dimethylamino)propyl]-5-methoxy-1H-indol-3-yl}-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-[1-[3-(Dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione 2-(1-(3-dimethylaminopropyl)-5-methoxyindol-3-yl)-3-(1H-indol-3-yl)maleimide go 6983 1H-Pyrrole-2,5-dione, 3-[1-[3-(dimethylamino)propyl]-5-methoxy-1H-indol-3-yl]-4-(1H-indol-3-yl)- |
| Description | Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively. |
|---|---|
| Related Catalog | |
| Target |
PKCγ:6 nM (IC50) PKCα:7 nM (IC50) PKCβ:7 nM (IC50) PKCδ:10 nM (IC50) PKCζ:60 nM (IC50) PKCμ:20000 nM (IC50) |
| In Vitro | Go 6983 inhibits PKCμ with IC50 of 20 μM, and the pther PKC isoenzymes can be suppressed by Go 6983 with IC50 values from 7 to 60 nM[1]. Go 6983 (100 nM) significantly reduces PMN adherence to the endothelium and infiltration into the myocardium compared with I/R + PMN hearts, and significantly inhibits superoxide release from PMNs by 90 +/- 2% in rat hearts[2]. Go 6983 (200 nM) has a reduced cardioprotective effect compared with the cardioprotective Go 6983 concentrations (50 and 100 nM) despite inhibiting PMN superoxide release by 99%[3]. |
| Kinase Assay | Phosphorylation reactions are carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HCl, pH 7.5, 10 mM β-mercaptoethanol), 4 mM MgCl2, 10 μg PS, 100 nM TPA, 5 μL of a Sf158 cell extract as a source of recombinant PKCμ or of Sf9 cell extracts as a source of other recombinant PKC isoenzymes, 10 μg of syntide 2 as substrate, and 35 μM ATP containing 1 μCi [γ-32P]ATP. In some experiments, PS and TPA are omitted or various inhibitors at concentrations indicated in the text are added. After incubation for 10 min at 30°C, the reaction is terminated by transferring 50 μL of the assay mixture onto a 20 mm square piece of phosphocellulose paper, which is washed 3 times in deionized water and twice in acetone. The radioactivity on each paper is determined by liquid scintillation counting. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 709.0±60.0 °C at 760 mmHg |
| Molecular Formula | C26H26N4O3 |
| Molecular Weight | 442.510 |
| Flash Point | 382.6±32.9 °C |
| Exact Mass | 442.200500 |
| PSA | 79.36000 |
| LogP | 3.80 |
| Appearance | red |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.670 |
| Storage condition | −20°C |
| Water Solubility | DMSO: 20 mg/mL, clear, red |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xi |
| Risk Phrases | 36/37/38 |
| Safety Phrases | 26-36 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |