| 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)
ζ-Stat specifically targets PKC-ζ (protein kinase C-zeta), a member of the atypical protein kinase C family involved in various cellular processes including NF-κB signaling. |
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| ln Vitro |
At the 5 μM level, ζ-Stat (0.1 – 20 μM) demonstrated a considerable 51% inhibition of PKC-ζ, whereas at 20 μM, it only showed 13% [1]. With increasing doses, ζ-Stat (0.1-10 μM; 3 d) dramatically inhibits the cell growth of MeWo and SK-MEL-2 [1]. LoVo CRC cell viability can be decreased by more than 75% when 5-FU and ζ-Stat (7 or 10 μM; 24-72 h) are used together [2]. In SK-MEL-2 and MeWo cells, Ε-Stat (5 μM; 3 d) significantly reduces the levels of phosphorylated and total PKC-ζ, Bcl-2, and PARP and increases the levels of Caspase-3 and cleaved PARP [1]. When applied to MEL-F-NEO, SK-MEL-2, and MeWo cells, ζ-Stat (5 μM; 1–10 hours) does not significantly harm them [1].
ζ-Stat inhibits PKC-ζ with an IC₅₀ of 5 μM. At 20 μM, it shows only 13% inhibition of PKC-ι, demonstrating selectivity for PKC-ζ over other PKC isoforms. |
| ln Vivo |
ζ-Stat reduces proliferation and causes apoptosis in melanoma cell lines. It downregulates TNF-α induced NF-κB translocation to the nucleus, thereby inducing apoptosis. In vivo activity data is limited to its antitumor effects observed in vitro.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for ζ-Stat typically involve cell-free kinase activity assays using purified PKC-ζ enzyme. The compound is incubated with the kinase, ATP, and a suitable substrate, and kinase activity is measured by detecting phosphorylated substrate using radiometric or fluorescence-based methods. IC₅₀ values are determined from dose-response inhibition curves.
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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. For in vitro cellular experiments, ζ-Stat is dissolved in DMSO and diluted in cell culture medium. Melanoma cell lines or other cancer cell lines are treated with the compound at concentrations ranging from 1-50 μM. Cell proliferation is assessed using MTT or CCK-8 assays. Apoptosis is measured by Annexin V/PI staining, caspase activity assays, or TUNEL staining. NF-κB translocation to the nucleus is assessed by immunofluorescence or Western blot analysis of nuclear and cytoplasmic fractions. |
| Animal Protocol |
In vivo animal experiments with ζ-Stat would typically involve formulation in suitable vehicles for administration to mouse xenograft models of melanoma or other cancers. Dosing routes may include intraperitoneal injection or oral gavage. Pharmacodynamic endpoints include tumor growth inhibition, assessment of apoptosis in tumor tissues, and evaluation of PKC-ζ and NF-κB pathway biomarkers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ζ-Stat have not been extensively characterized. The compound has a molecular formula of C₁₀H₈O₁₀S₃. Standard PK studies would assess parameters such as half-life, oral bioavailability, and tissue distribution in rodent models.
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| Toxicity/Toxicokinetics |
Toxicological data for ζ-Stat is limited to research applications. The compound is intended for laboratory use only and has not been evaluated for human therapeutic safety. Standard chemical handling precautions should be followed.
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| References |
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| Additional Infomation |
ζ-Stat (NSC37044) is a specific and atypical inhibitor of PKC-ζ with an IC₅₀ of 5 μM. It reduces proliferation and causes apoptosis in melanoma cell lines and exhibits antitumor activity in vitro. The compound is used as a research tool for studying PKC-ζ signaling and cancer biology. No clinical trials or regulatory approvals have been reported.
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| Molecular Formula |
C10H8O10S3
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|---|---|
| Molecular Weight |
384.36
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| Exact Mass |
383.928
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| CAS # |
3316-02-7
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| PubChem CID |
76828
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| Appearance |
Light brown to brown solid powder
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| Density |
2.019g/cm3
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| Index of Refraction |
1.741
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| LogP |
3.527
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
751
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C2C=C(C=C(C2=C(C=C1S(=O)(=O)O)O)S(=O)(=O)O)S(=O)(=O)O
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| InChi Key |
KMXMLAGYNHELHA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H8O10S3/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)
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| Chemical Name |
8-hydroxynaphthalene-1,3,6-trisulfonic acid
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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 |
| 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: 62.5 mg/mL (162.61 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (260.17 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6017 mL | 13.0086 mL | 26.0173 mL | |
| 5 mM | 0.5203 mL | 2.6017 mL | 5.2035 mL | |
| 10 mM | 0.2602 mL | 1.3009 mL | 2.6017 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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