CAS Number133053-19-7
Synonyms3-{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
Molecular FormulaC26H26N4O3
Molecular Weight442.510
Purity98%%
Density1.3±0.1 g/cm3
Boiling Point709.0±60.0 °C at 760 mmHg
Appearancered
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 133053-19-7 |
| Catalog No. | 2A-1171174 |
| Chinese Name | Go 6983 |
| 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 |
| Molecular Formula | C26H26N4O3 |
| Molecular Weight | 442.510 |
| Purity | 98% |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 709.0±60.0 °C at 760 mmHg |
| Appearance | red |
| Water Solubility | DMSO: 20 mg/mL, clear, red |
| Storage Condition | −20°C |
| Application | Go 6983 is a potent PKC inhibitor that targets PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 values of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM respectively. |
| PubChem ID | 7351422 |
| SMILES | COc1ccc2c(c1)c(C1=C(c3c[nH]c4ccccc34)C(=O)NC1=O)cn2CCCN(C)C |
| InChI | InChI=1S/C26H26N4O3/c1-29(2)11-6-12-30-15-20(18-13-16(33-3)9-10-22(18)30)24-23(25(31)28-26(24)32)19-14-27-21-8-5-4-7-17(19)21/h4-5,7-10,13-15,27H,6,11-12H2,1-3H3,(H,28,31,32) |
| InChI Key | LLJJDLHGZUOMQP-UHFFFAOYSA-N |
| Hazard Symbols | transportation |
| MSDS | msds/171360_2_133053_19_7.pdf |
| Bioactivity | 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 Signaling Pathways >> Epigenetics >> PKC Signaling Pathways >> TGF-beta/Smad >> PKC Research Areas >> Cancer 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 [1]. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett, 1996, 392(2), 77-80. [2]. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol, 2004, 43(5), 645-656. [3]. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. Cardiovasc Drug Rev, 2005, 23(3), 255-272. Chemical & Physical Properties 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 of Characters red Vapour Pressure 0.0±2.3 mmHg at 25°C Index of Refraction 1.670 InChIKey LLJJDLHGZUOMQP-UHFFFAOYSA-N SMILES COc1ccc2c(c1)c(C1=C(c3c[nH]c4ccccc34)C(=O)NC1=O)cn2CCCN(C)C Storage condition −20°C Water Solubility DMSO: 20 mg/mL, clear, red |
| Use of | 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. Properties Name 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione Synonym More Synonyms Go 6983 Biological Activity 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 Signaling Pathways >> Epigenetics >> PKC Signaling Pathways >> TGF-beta/Smad >> PKC Research Areas >> Cancer PKCγ:6 nM (IC50) PKCα:7 nM (IC50) PKCβ:7 nM (IC50) PKCδ:10 nM (IC50) PKCζ:60 nM (IC50) PKCμ:20000 nM (IC50) References [1]. Gschwendt M, et al. Inhibition of protein kinase C mu by various inhibitors. Differentiation from protein kinase c isoenzymes. FEBS Lett, 1996, 392(2), 77-80. [2]. Peterman EE, et al. G0 6983 exerts cardioprotective effects in myocardial ischemia/reperfusion. J Cardiovasc Pharmacol, 2004, 43(5), 645-656. [3]. Young LH, et al. G0 6983: a fast acting protein kinase C inhibitor that attenuates myocardial ischemia/reperfusion injury. Cardiovasc Drug Rev, 2005, 23(3), 255-272. Chemical & Physical Properties Molecular Formula C26H26N4O3 Exact Mass 442.200500 PSA 79.36000 Appearance of Characters red Index of Refraction 1.670 InChIKey LLJJDLHGZUOMQP-UHFFFAOYSA-N |
| Transport Info | Product name: Purity: 96.0% |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN dangerous goods number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: Non-dangerous goods IMDG Code: Non-dangerous goods International air transport dangerous goods regulations: non-dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special reminder to users No data available |
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