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ζ-Stat trisodium (NSC37044 trisodium) 31894-34-5

ζ-Stat trisodium (NSC37044 trisodium) 31894-34-5

CAS No.: 31894-34-5

ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical inhibitor of PKC-ζ with IC50 of 5 μM. ζ-Stat trisod
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ζ-Stat trisodium (NSC37044 trisodium) is a specific and atypical inhibitor of PKC-ζ with IC50 of 5 μM. ζ-Stat trisodium reduces proliferation and causes apoptosis in melanoma cell lines and has anticancer effect in vitro.

Physicochemical Properties


Molecular Formula C10H5O10S3-3.3[NA+]
Molecular Weight 450.3051
Exact Mass 449.873
CAS # 31894-34-5
PubChem CID 90471481
Appearance Light yellow to light brown solid powder
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 10
Rotatable Bond Count 0
Heavy Atom Count 26
Complexity 711
Defined Atom Stereocenter Count 0
SMILES

[Na+].[Na+].[Na+].O=S(C1=CC(O)=C2C(S([O-])(=O)=O)=CC(=CC2=C1)S([O-])(=O)=O)(=O)[O-]

InChi Key VQXXRDCDIFAODW-UHFFFAOYSA-K
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
Chemical Name

trisodium;8-hydroxynaphthalene-1,3,6-trisulfonate
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets aPKC-ζ 5 μM (IC50)
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].
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.
References

[1]. Oncogenic PKC-ι activates Vimentin during epithelial-mesenchymal transition in melanoma; a study based on PKC-ι and PKC-ζ specific inhibitors. Cell Adh Migr. 2018; 12(5):447-463.

[2]. Atypical Protein Kinase-C inhibitors exhibit a synergistic effect in facilitating DNA damaging effect of 5-fluorouracil in colorectal cancer cells. Biomed Pharmacother. 2020 Jan; 121:109665.


Solubility Data


Solubility (In Vitro) H2O: 12.5 mg/mL (27.76 mM)
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.