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Closantel

Chemical Structure : Closantel

CAS No.: 57808-65-8

Closantel (FICD inhibitor C22)

Catalog No.: PC-45380Not For Human Use, Lab Use Only.

Closantel (FICD inhibitor C22) is a veterinary anthelmintic with known proton ionophore activities, also is a small molecule inhibitor of the AMP transferase FICD with IC50 of 7.27 uM.

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Biological Activity

Closantel (FICD inhibitor C22) is a veterinary anthelmintic with known proton ionophore activities, also is a small molecule inhibitor of the AMP transferase FICD with IC50 of 7.27 uM.
Closantel (FICD inhibitor C22) is identified as a potent and specific inhibitor of filarial chitinases; also shows to be an allosteric inhibitor of SPAK and OSR1.
FICD inhibitor C22 is a small molecule inhibitor of the AMP transferase FICD with IC50 of 7.27 uM, significantly inhibits FICD-mediated BiP/GRP78 AMPylation in intact cells, while only weakly inhibiting BiP/GRP78 deAMPylation.
FICD inhibitor C22 also efficiently inhibit pathogenic FICD variants and improve proinsulin processing in β cells.
FICD is a bi-functional enzyme, catalyzing both AMP addition (AMPylation) and removal (deAMPylation) from the ER resident chaperone BiP/GRP78.

Physicochemical Properties

M.Wt 663.0737
Formula C22H14Cl2I2N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 49 mg/mL

Chemical Name/SMILES

Benzamide, N-[5-chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodo-

References

1. AlAmri MA, et al. ChemMedChem. 2017 May 9;12(9):639-645.

2. Gloeckner C, et al. Proc Natl Acad Sci U S A. 2010 Feb 23;107(8):3424-9.

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