Go6976
Based on 14 publication(s) in Google Scholar
Go6976 is a Protein Kinase C (PKC) inhibitor, with an IC50 of 20 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.57%
- No. CAS: 136194-77-9
- Fòrmula: C24H18N4O
- Peso molecular:378.43
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Go6976
More- Phytomedicine. 2026 Jun:155:158121. [Abstract]
- Brain Behav Immun. 2026 Mar 6:135:106529. [Abstract]
- Biochem Pharmacol. 2025 Jun 3:117015. [Abstract]
- Life Sci. 2023 Sep 1:328:121903. [Abstract]
- J Cell Mol Med. 2019 Apr;23(4):2731-2743. [Abstract]
- Reg Anesth Pain Med. 2025 Feb 27:rapm-2024-106195. [Abstract]
- Mol Med Rep. 2024 Jul;30(1):110. [Abstract]
- Thromb Res. 2024 Nov 7:244:109210. [Abstract]
- Cardiovasc Drugs Ther. 2022 Aug;36(4):633-643. [Abstract]
- FEBS Lett. 2024 Feb;598(4):400-414. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 19:785:152676. [Abstract]
- University of Pittsburgh. 2025.
- bioRxiv. 2025 May 19:2025.05.15.654389. [Abstract]
- Res Sq. 2024 Jun 11.
Actividad biológica
IC50: 20 nM (PKC)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Splenocyte | IC50 |
>10 μM
Compound: 3k
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In vitro for inhibitory activity against tyrosine specific protein kinase from murine spleen cells (T-kinase)
In vitro for inhibitory activity against tyrosine specific protein kinase from murine spleen cells (T-kinase)
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10.1016/S0960-894X(01)80995-1 |
| Vero | CC50 |
6 μM
Compound: 208; Go6976
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Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis
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[PMID: 28689975] |
Go6976 is a potent inhibitor of PKC in vitro IC50 is 20 nM. This compound is structurally related to staurosporine, which is the most potent PKC inhibitor[1]. UCN-01 is originally identified as a PKC inhibitor. Surprisingly, Go6976 is found to abrogate S and G2 arrest. Dose-response studies reveal that 30 nM Go6976 is sufficient to cause abrogation of S-phase arrest in 6 h and abrogation of G2 arrest followed by lethal mitosis in 24 h. Incubation of cells with 100 nM Go6976 is sufficient to cause complete abrogation of S and G2 arrest at 6 and 24 h, respectively, which is only slightly less potent than in bovine serum. Incubation of cells with UCN-01 or Go6976 alone do not decrease viability compared with control at the concentrations used. Incubation of cells with 5 ng/mL SN38 result in cytostasis, and addition of 50 nM UCN-01 or 100 nM Go6976 to arrested MDA-MB-231 cells cause a dramatic decrease in viable cell number by 96 h[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 136194-77-9
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Appearance Solid
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Peso molecular 378.43
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Fòrmula C24H18N4O
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Color White to light yellow
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SMILES
N#CCCN(C1=C2C(CNC3=O)=C3C4=C1N(C)C5=C4C=CC=C5)C6=C2C=CC=C6
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Multi-omics and machine learning reveal a critical mediator of PRKCA in quercetin-mediated protection against Sarcopenia. [Abstract]2026 Jun:155:158121. PMID: 41936173 -
Brain Behav Immun
NR2B-CaMKII signaling in the dentate gyrus driven by astrocytic P2Y1Rs mediates the antidepressant effect of low-dose LPS. [Abstract]2026 Mar 6:135:106529. PMID: 41796645 -
Biochem Pharmacol
Interplay between G protein-biased and arrestin-biased pathways in 5-HT2AR-mediated ERK activation. [Abstract]2025 Jun 3:117015. PMID: 40473228 -
Life Sci
Receptor-specific contributions of caveolae, PKC, and Src tyrosine kinase to serotonergic and adrenergic regulation of Kv channels and vasoconstriction. [Abstract]2023 Sep 1:328:121903. PMID: 37394095 -
J Cell Mol Med
Matrine attenuates high-fat diet-induced in vivo and ox-LDL-induced in vitro vascular injury by regulating the PKCα/eNOS and PI3K/Akt/eNOS pathways. [Abstract]2019 Apr;23(4):2731-2743. PMID: 30770623 -
Reg Anesth Pain Med
Elevated 18:1 lysophosphatidylcholine contributes to neuropathic pain in peripheral nerve injury. [Abstract]2025 Feb 27:rapm-2024-106195. PMID: 40016127 -
Mol Med Rep
Calcitonin gene‑related peptide alleviates hyperoxia‑induced human alveolar cell injury via the CGRPR/TRPV1/Ca2+ axis. [Abstract]2024 Jul;30(1):110. PMID: 38695251 -
Thromb Res
The role of protein kinase C and the glycoprotein Ibα cytoplasmic tail in anti-glycoprotein Ibα antibody-induced platelet apoptosis and thrombocytopenia. [Abstract]2024 Nov 7:244:109210. PMID: 39541612 -
Cardiovasc Drugs Ther
Berberine Reverses Nitroglycerin Tolerance through Suppressing Protein Kinase C Alpha Activity in Vascular Smooth Muscle Cells. [Abstract]2022 Aug;36(4):633-643. PMID: 34319490 -
FEBS Lett
Mdm2-mediated ubiquitination of PKCβII is responsible for insulin-induced heterologous desensitization of dopamine D3 receptor. [Abstract]2024 Feb;598(4):400-414. PMID: 38302840 -
Biochem Biophys Res Commun
Glucose transports in the ileum: mechanism, regulation and physiological role of ileal glucose absorption. [Abstract]2025 Sep 19:785:152676. PMID: 41005286 -
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bioRxiv
Desmoplakin loss leads to PKC-dependent insertion of series sarcomeres and contractile dysfunction in cardiomyocytes. [Abstract]2025 May 19:2025.05.15.654389. PMID: 40475450 -
Solvente y solubilidad
DMSO : 65 mg/mL (171.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 3.25 mg/mL (8.59 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 3.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (32.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Logarithmically growing cells are incubated with or without 5 ng/mL SN38 for 24 h and then incubated with or without 50 nM UCN-01 or 100 nM Go6976 for the following 24 h. MDA-MB-231 (500 cells) or MCF-10A (1000 cells) are plated in 100 μL in each well of a 96-well plate. The following day, drugs are added at the desired concentrations (Go6976: 1, 3, 10, 30, 100 nM) and with the required schedule to replicate wells (a minimum of 4 wells/concentration). Drugs are removed, and plates are rinsed and then incubated for an additional 6 days. Inhibition of growth was then assessed on the basis of DNA content. Briefly, the media are removed, and attached cells are washed in 0.25×PBS, followed by the addition of 100 μL of H2O. Cells are lysed by freeze/thawing the plates. Hoechst 33258 is added in high-salt buffer, cells are incubated for 2 h, and fluorescence is measured[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Qatsha KA, et al. Gö 6976, a selective inhibitor of protein kinase C, is a potent antagonist of human immunodeficiency virus 1 induction from latent/low-level-producing reservoir cells in vitro. Proc Natl Acad Sci U S A. 1993 May 15;90(10):4674-8. [Content Brief]
[2]. Hayamitsu Adachi, et al. Microbial metabolites and derivatives targeted at inflammation and bone diseases therapy: chemistry, biological activity and pharmacology. The Journal of Antibiotics volume 71, pages 60–71 (2018). [Content Brief]
[3]. Mahmoudian S, et al. Influenza A virus proteins PB1 and NS1 are subject to functionally important phosphorylation by protein kinase C. J Gen Virol. 2009;90(Pt 6):1392-1397. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6425 mL | 13.2125 mL | 26.4250 mL | 66.0624 mL |
| 5 mM | 0.5285 mL | 2.6425 mL | 5.2850 mL | 13.2125 mL | |
| 10 mM | 0.2642 mL | 1.3212 mL | 2.6425 mL | 6.6062 mL | |
| 15 mM | 0.1762 mL | 0.8808 mL | 1.7617 mL | 4.4042 mL | |
| 20 mM | 0.1321 mL | 0.6606 mL | 1.3212 mL | 3.3031 mL | |
| 25 mM | 0.1057 mL | 0.5285 mL | 1.0570 mL | 2.6425 mL | |
| 30 mM | 0.0881 mL | 0.4404 mL | 0.8808 mL | 2.2021 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
| 50 mM | 0.0528 mL | 0.2642 mL | 0.5285 mL | 1.3212 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1010 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2642 mL | 0.6606 mL |
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