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C188

Cat. No. M30649
C188 Structure
Synonym:

CPD188

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Biological Activity

C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).

Chemical Information
Molecular Weight 433.45
Formula C19H15NO7S2
CAS Number 823828-18-8
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yuko Ono, et al. Front Pharmacol. C188-9, a specific inhibitor of STAT3 signaling, prevents thermal burn-induced skeletal muscle wasting in mice

[2] Junnv Xu, et al. Front Oncol. IL-6/STAT3 Is a Promising Therapeutic Target for Hepatocellular Carcinoma

[3] Jiao Liu, et al. FEBS Open Bio. C188-9 reduces TGF-β1-induced fibroblast activation and alleviates ISO-induced cardiac fibrosis in mice

[4] Rui Kong, et al. Front Oncol. Small Molecule Inhibitor C188-9 Synergistically Enhances the Demethylated Activity of Low-Dose 5-Aza-2'-Deoxycytidine Against Pancreatic Cancer

[5] Jian-Xin Di, et al. Anticancer Drugs. C188-9, a small-molecule STAT3 inhibitor, exerts an antitumor effect on head and neck squamous cell carcinoma

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  Catalog
Abmole Inhibitor Catalog




Keywords: C188, CPD188 supplier, STAT, inhibitors, activators


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