Go 6983 (Synonyms: Goe 6983;Go6983;Go-6983) |
Catalog No.GC16907
One-Click Copy Product Info
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Go 6983 is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ, PKCδ, andPKCμ with IC50 values of 7nM, 7nM, 6nM, 10nM, and 20µM, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133053-19-7
Sample solution is provided at 25 µL, 10mM.
Go 6983 is a pan-PKC inhibitor that acts on PKCα, PKCβ, PKCγ, PKCδ, and PKCμ with IC50 values of 7nM, 7nM, 6nM, 10nM, and 20µM, respectively[1]. Go 6983 inhibits titanium particle-induced osteolysis and RANKL-mediated osteoclastogenesis by suppressing the NFκB/JNK/p38 pathway[2]. Go 6983 has been widely used for regulating calcium sensitivity and inhibiting the contraction of prostate smooth muscle[3].
In vitro, Go 6983 significantly inhibits the replication of SARS-CoV-2 virus in Huh7 cells within 24 hours, with an IC50 value of 0.3614µM[4]. 6nM of Go 6983 pretreatment for 30 minutes markedly suppressed the increase in lactate dehydrogenase (LDH) leakage and the decrease in cell survival rate in neuronal cells of BALB/c mice induced by oxygen-glucose deprivation (OGD)[5]. Treatment with 10µM Go 6983 for 24 hours inhibited the migration and invasion of MDA-MB-231 cells[6].
In vivo, a single intraventricular injection of 5µl of Go 6983 (6µM) was administered for 6 hours eliminated the neuroprotective effect of hypoxic preconditioning (HPC) on mice under the condition of middle cerebral artery occlusion (MCAO), and aggravated the neurological damage[7]. Tail vein injection of Go 6983 (10nmol/kg/day) for 28 days inhibited the tumor burden in the DAN cell-xenograft tumor mouse model and prevented lung metastasis[8].
References:
[1] Gschwendt M, Dieterich S, Rennecke J, et al. Inhibition of protein kinase C μ by various inhibitors. Inhibition from protein kinase c isoenzymes[J]. FEBS letters, 1996, 392(2): 77-80.
[2] Feng W, Li J, Liao S, et al. Gö6983 attenuates titanium particle-induced osteolysis and RANKL mediated osteoclastogenesis through the suppression of NFκB/JNK/p38 pathways[J]. Biochemical and biophysical research communications, 2018, 503(1): 62-70.
[3] Huang R, Liu Y, Li B, et al. Inhibition of human prostate smooth muscle contraction by the inhibitors of protein kinase C, GF109203X, and Go6983[J]. The Prostate, 2022, 82(1): 59-77.
[4] Huang C, Feng F, Shi Y, et al. Protein kinase C inhibitors reduce SARS-CoV-2 replication in cultured cells[J]. Microbiology spectrum, 2022, 10(5): e01056-22.
[5] Liu Y, Li J, Yang J, et al. Inhibition of PKCgamma membrane translocation mediated morphine preconditioning-induced neuroprotection against oxygen–glucose deprivation in the hippocampus slices of mice[J]. Neuroscience letters, 2008, 444(1): 87-91.
[6] Luan Z, Li J, Huang X, et al. Gö6983 attenuates breast cancer‐induced osteolysis by the apoptotic pathway[J]. Cell Biology International, 2020, 44(3): 838-847.
[7] Zhang N, Yin Y, Han S, et al. Hypoxic preconditioning induced neuroprotection against cerebral ischemic injuries and its cPKCγ-mediated molecular mechanism[J]. Neurochemistry international, 2011, 58(6): 684-692.
[8] Hu H J, Deng X W, Li R X, et al. Inhibition of protein kinase C activity inhibits osteosarcoma metastasis[J]. Archives of Medical Science, 2019, 15(4): 1028-1034.
| Cell experiment [1]: | |
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Cell lines |
BHK-21 cells |
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Preparation Method |
BHK-21 cells were cultured in DMEM medium, supplemented with 10% fetal bovine serum (FBS), and 1% penicillin/streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in a 96-well plate at a density of 1×104 cells/well overnight. The pBAC-SARS-CoV-2-replicon-luciferase plasmid was transfected into the cells and then incubated for 24 hours in the presence of different concentrations of Go 6983 (0, 1, 5, 10, 20, and 100µM). Subsequently, the cell viability was detected. |
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Reaction Conditions |
0, 1, 5, 10, 20, and 100µM; 24h |
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Applications |
Go 6983 treatment reduced cell viability of BHK-21 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female p53–/– mice |
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Preparation Method |
Female p53–/– mice (6 weeks old) were raised in a standard environment, with free access to food and water. 106 firefly luciferase expressing DAN cells were injected via the tail vein of mice. One day after the initial injection, mice were injected with either DMSO or 10nmol/kg of Go 6983 (once every day). Mice were assessed weekly for tumor formation up to 28 days using in vivo bioluminescence imaging. |
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Dosage form |
10nmol/kg/day; 28 days; tail vein injection |
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Applications |
Go 6983 treatment inhibited the tumor burden in the DAN cell-xenograft tumor mouse model. |
References: [1] Huang C, Feng F, Shi Y, et al. Protein kinase C inhibitors reduce SARS-CoV-2 replication in cultured cells[J]. Microbiology spectrum, 2022, 10(5): e01056-22. [2] Hu H J, Deng X W, Li R X, et al. Inhibition of protein kinase C activity inhibits osteosarcoma metastasis[J]. Archives of Medical Science, 2019, 15(4): 1028-1034. | |
| Cas No. | 133053-19-7 | SDF | |
| Synonyms | Goe 6983;Go6983;Go-6983 | ||
| Chemical Name | 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione | ||
| Canonical SMILES | CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 | ||
| Formula | C26H26N4O3 | M.Wt | 442.51 |
| Solubility | ≥ 22.15mg/mL in DMSO | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2598 mL | 11.2992 mL | 22.5984 mL |
| 5 mM | 452 μL | 2.2598 mL | 4.5197 mL |
| 10 mM | 226 μL | 1.1299 mL | 2.2598 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)