| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
aPKC-ζ 5 μM (IC50)
The compound specifically targets Protein Kinase C-zeta (PKC-zeta), an atypical PKC isoenzyme involved in key signaling pathways that regulate cell polarity, proliferation, and survival. It is a selective inhibitor with an IC50 of 5 microM, making it a valuable tool for dissecting PKC-zeta-mediated cellular functions. |
|---|---|
| ln Vitro |
At 20 μM, ζ-Stat (0.1–20 µM) only exhibits 13% inhibition on PKC–ζ; but, at 5 μM, it exhibits a strong 51% inhibition on PKC–ζ[1]. As the concentrations of ζ-Stat (0.1-10 µM; 3 d) increase, so does the cell proliferation of SK-MEL-2 and MeWo. The combination of 5-FU and ζ-Stat (7 or 10 µM; 24-72 h) can reduce the viability of LoVo CRC cells by about 75%[2]. ζ-Stat (5 µM; 3 d) significantly reduces the levels of Bcl-2, PARP, and phosphorylated total PKC-ζ in SK-MEL-2 and MeWo cells while increasing the levels of caspase-3 and cleaved PARP[1]. On MEL-F-NEO, SK-MEL-2, and MeWo cells, ζ-Stat (5 µM; 1–10 h) does not exhibit appreciable cytotoxicity[1].
In vitro, zeta-Stat trisodium effectively reduces the proliferation of melanoma cell lines and induces apoptosis. By selectively inhibiting PKC-zeta, it disrupts downstream pro-survival signaling cascades, leading to growth arrest and cell death in cancer cells. It has demonstrated consistent antitumor activity across multiple melanoma cell lines. |
| ln Vivo |
In vivo data for zeta-Stat trisodium is currently limited, as it is primarily a research tool for in vitro studies. Its demonstrated ability to reduce proliferation and induce apoptosis in vitro positions it as a potential candidate for future in vivo studies in animal models of melanoma and other cancers.
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| Enzyme Assay |
Cell-free PKC-zeta activity assays are performed using immunoprecipitated PKC-zeta from cell lysates or a purified recombinant enzyme. The kinase is incubated with a specific substrate (e.g., myelin basic protein or a synthetic peptide), [gamma-32P]ATP, and varying concentrations of zeta-Stat trisodium. The IC50 is determined by measuring the incorporation of radiolabeled phosphate into the substrate.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: MEL-F-NEO, SK-MEL-2 and MeWo cells Tested Concentrations: 0.1, 0.5, 1, 2.5, 5, 7.5, 10 µM Incubation Duration: 3 days Experimental Results: diminished proliferation by 47.7% for 5 µM in SK-MEL-2 cells and by 50.6% for 5 µM in MeWo cells. demonstrated significant inhibitions on MEL-F-NEO cells 19.3% (P ≤ 0.05) at 10 μM. Western Blot Analysis[1] Cell Types: SK-MEL-2 and MeWo cells Tested Concentrations: 5 µM Incubation Duration: 3 days Experimental Results: diminished phosphorylated and total PKC-ζ levels. Cellular assays are performed in cancer cell lines (e.g., melanoma). Cells are seeded in multi-well plates and treated with zeta-Stat trisodium for 24-72 hours. Cell proliferation is measured using a standard MTT or CCK-8 assay. Apoptosis is assessed by flow cytometry using Annexin V/PI staining or by measuring caspase-3/7 activity. |
| Animal Protocol |
In vivo studies for PKC-zeta inhibitors are typically conducted in xenograft mouse models of cancer (e.g., melanoma). Animals are implanted subcutaneously with cancer cells and once tumors are established, they are treated with zeta-Stat trisodium via intraperitoneal or intratumoral injection. Tumor growth is monitored over time to evaluate antitumor efficacy.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of zeta-Stat trisodium is currently being characterized. As an anionic molecule (trisodium salt), its absorption and cellular permeability are key areas of focus. Early data suggests it is suitable for in vitro use, with ongoing work to optimize its properties for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological profiles have not been formally established. The compound is intended for research use only and is not for human consumption. Standard safety precautions for handling cytotoxic agents and fine chemicals should be followed. It has shown activity in cancer cell lines, indicating potential for target-based toxicity.
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| References |
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| Additional Infomation |
zeta-Stat trisodium, with the molecular formula C10H5Na3O10S3 and a molecular weight of 450.31, is a specific chemical probe for PKC-zeta. Unlike general PKC inhibitors, its selectivity for the atypical zeta isoform makes it a critical tool for deconvoluting the specific role of aPKC in physiological and pathological conditions, particularly in cancer research.
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| Molecular Formula |
C10H5O10S3-3.3[NA+]
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|---|---|
| Molecular Weight |
450.3051
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| Exact Mass |
449.873
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| CAS # |
31894-34-5
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| PubChem CID |
90471481
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| Appearance |
Light yellow to light brown solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
26
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| Complexity |
711
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Na+].[Na+].[Na+].O=S(C1=CC(O)=C2C(S([O-])(=O)=O)=CC(=CC2=C1)S([O-])(=O)=O)(=O)[O-]
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| InChi Key |
VQXXRDCDIFAODW-UHFFFAOYSA-K
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| InChi Code |
InChI=1S/C10H8O10S3.3Na/c11-8-3-6(21(12,13)14)1-5-2-7(22(15,16)17)4-9(10(5)8)23(18,19)20;;;/h1-4,11H,(H,12,13,14)(H,15,16,17)(H,18,19,20);;;/q;3*+1/p-3
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| Chemical Name |
trisodium;8-hydroxynaphthalene-1,3,6-trisulfonate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 12.5 mg/mL (27.76 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.63 mg/mL (5.84 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2207 mL | 11.1035 mL | 22.2069 mL | |
| 5 mM | 0.4441 mL | 2.2207 mL | 4.4414 mL | |
| 10 mM | 0.2221 mL | 1.1103 mL | 2.2207 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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