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Go 6983

Catalog No.
A8343
pan-PKC inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$99.00
In stock
5mg
$94.00
In stock
10mg
$149.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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).

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt442.51
Cas No.133053-19-7
FormulaC26H26N4O3
SynonymsGoe 6983;Go6983;Go-6983
Solubility≥22.15 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name3-[1-[3-(dimethylamino)propyl]-5-methoxyindol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
SDFDownload SDF
Canonical SMILESCN(C)CCCN1C=C(C2=C1C=CC(=C2)OC)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
Shipping ConditionSmall 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.

Protocol

Kinase experiment [1]:

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]:

Cell lines

ARCcPE cells

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.

Reaction Conditions

200 and 1000 nM; 48 hrs

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]:

Animal models

Mice bearing B16BL6 tumors

Dosage form

22 μg/mouse, i.v.

Applications

In a mouse pulmonary B16BL6 tumor model, Go6983 at the dose of 22.0 μg/mouse significantly inhibited tumor metastasis by 51.2 %.

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.

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.

Biological Activity

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

Chemical structure

Go 6983

Related Biological Data

Go 6983

Related Biological Data

Go 6983