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PDE12 inhibitor Compound 1

Chemical Structure : PDE12 inhibitor Compound 1

CAS No.: 2259620-80-7

PDE12 inhibitor Compound 1

Catalog No.: PC-20981Not For Human Use, Lab Use Only.

PDE12 inhibitor Compound 1 is a potent, selective inhibitor of phosphodiesterase 12 (PDE12) with pIC50 of 9.1 and Ki of 17.5 nM, >1000-fold selectivity over EEP nuclease family member CNOT6.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PDE12 inhibitor Compound 1 is a potent, selective inhibitor of phosphodiesterase 12 (PDE12) with pIC50 of 9.1 and Ki of 17.5 nM, >1000-fold selectivity over EEP nuclease family member CNOT6.
PDE12 inhibitor Compound 1 produced increase in 2',5'-oligoadenylate (2-5A) levels in HeLa cells with pEC50 of 7.7.
PDE12 inhibitor Compound 1 inhibited the EMCV-induced cytopathic effect in HeLa Ohio cells with a pIC50 of 6.7.
PDE12 inhibitor Compound 1 inhibited HeLa Ohio cell proliferation in the absence of EMCV infection with a pIC50 of 5.7.
PDE12 inhibitor Compound 1 inhibited HRV infection with a pIC50 of 6.9.

Physicochemical Properties

M.Wt 616.49
Formula C31H27BrFN5O3
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

10 mM in DMSO

Chemical Name/SMILES

N#CC1=CC2=C(C=C1)C(C3=NC4=CC(Br)=C(C(N5[C@@H](CO)[C@H](C6=CC=C(F)C=C6)OCC5)=O)C=C4N3C)=CN2CC

References

1. Wood ER, et al. J Biol Chem. 2015 Aug 7;290(32):19681-96.

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