Go 6983
Go 6983 (CAS 133053-19-7) is a selective inhibitor of protein kinase C isoforms PKCα, PKCβ, PKCγ, PKCδ, and PKCμ, with reported IC50 values of approximately 7 nM, 7 nM, 6 nM, 10 nM, and 20 mM, respectively. Protein kinase C (PKC) isoforms act as receptors for tumor-promoting phorbol ester, mediating various downstream cellular functions. In cancer cell models, Go 6983 suppresses PKCα and PKCδ activation induced by phorbol esters and reduces PKCη expression, inhibiting cell survival pathways. It is frequently employed in biomedical studies examining PKC-dependent signaling in cancer progression and epithelial-to-mesenchymal transition (EMT).
- 1. Shiyu An, Shuyue Hou, et al. "WDR36 Regulates Trophectoderm Differentiation During Human Preimplantation Embryonic Development Through Glycolytic Metabolism." ADVANCED SCIENCE. Volume12, Issue5 February 3, 2025 2412222
- 2. An Liu, Qiaoyun Ren, et al. "Neuroligin 1 regulates autistic-like repetitive behavior through modulating the excitability of striatal D2 expressing medium spiny neurons" Research Square. 10 Jul, 2024
- 3. Li Yuan, Lingming Zhang, et al. "Upregulation of UGT1A1 expression by ursolic acid and oleanolic acid via the inhibition of the PKC/NF-κB signaling pathway." Phytomedicine. 2021 Nov;92:153726. PMID:34536821
- 4. Lee E, Wang J, et al. "DNMT1 Regulates Epithelial-Mesenchymal Transition and Cancer Stem Cells, Which Promotes Prostate Cancer Metastasis."Neoplasia. 2016 Sep;18(9):553-66. PMID:27659015
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 442.51 |
| Cas No. | 133053-19-7 |
| Formula | C26H26N4O3 |
| Synonyms | Goe 6983;Go6983;Go-6983 |
| Solubility | ≥22.15 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione |
| SDF | Download SDF |
| Canonical SMILES | CN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Kinase experiment [1]: | |
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Binding assay |
Phosphorylation reactions were carried out in a total volume of 100 μL, containing buffer C (50 mM Tris-HC1, 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 were omitted or various inhibitors at concentrations indicated in the text were added. After incubation for 10 mins at 30 °C, the reaction was terminated by transferring 50 μL of the assay mixture onto a 20-mm square piece of phosphocellulose paper, which was washed 3 times in deionized water and twice in acetone. The radioactivity on each paper was determined by liquid scintillation counting. |
| Cell experiment [2]: | |
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Cell lines |
ARCcPE cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20 °C for several months. |
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Reaction Conditions |
200 and 1000 nM; 48 hrs |
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Applications |
In ARCaPE cells, Go 6983 at the dose of 200 nM significantly inhibited the up-regulation of PKCs(PKCα, PKCβ and PKCγ) stimulated by the PMA treatment. In addition, Go 6983 showed complete inhibition at the dose of 1000 nM. |
| Animal experiment [3]: | |
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Animal models |
Mice bearing B16BL6 tumors |
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Dosage form |
22 μg/mouse, i.v. |
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Applications |
In a mouse pulmonary B16BL6 tumor model, Go6983 at the dose of 22.0 μg/mouse significantly inhibited tumor metastasis by 51.2 %. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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): p. 77-80. [2]. He, H., et al., Phorbol ester phorbol-12-myristate-13-acetate induces epithelial to mesenchymal transition in human prostate cancer ARCaPE cells. Prostate, 2010. 70(10): p. 1119-26. [3]. Kim HR, Lee KH, Park SJ, Kim SY, Yang YK, Tae J, Kim J. Anti-cancer activity and mechanistic features of a NK cell activating molecule. Cancer Immunol Immunother. 2009 Oct;58(10):1691-700. |
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| Description | Go 6983 is an inhibitor of pan-PKC with IC50 values of 7 nM, 7 nM, 6 nM and 10 nM for PKCα, PKCβ, PKCγ and PKCδ, respectively. | |||||
| Targets | PKCγ | PKCα | PKCβ | PKCδ | PKCζ | PKCμ |
| IC50 | 6 nM | 7 nM | 7 nM | 10 nM | 60 nM | 20 μM |
Quality Control & MSDS
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