A selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling

Eggmanone – 10 mg

Brand:
Cayman
CAS:
505068-32-6
Storage:
-20
UN-No:
Non-Hazardous - /

Type 4 cyclic nucleotide phosphodiesterase (PDE4) selectively inactivates the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP. PDE4 has been reported to play a key regulatory role in Hedgehog signaling downstream of smoothened and, thus, represents a potential therapeutic target for Hedgehog-dependent cancers.{28683} Eggmanone is a selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway.{28683} It demonstrates 40- to 50-fold lower potency at PDE3, PDE10, and PDE11 (IC50s = 3, 3.05, and 4.08 µM, respectively).{28683} Inhibition of PDE4 activity via eggmanone was shown to activate localized protein kinase A signaling, which, in turn, regulates Gli processing and translocation.{28683}  

 

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Description

A selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation

Formal name: 5,6,7,8-tetrahydro-3-(2-methyl-2-propen-1-yl)-2-[[2-oxo-2-(2-thienyl)ethyl]thio]-[1]benzothieno[2,3-d]pyrimidin-4(3H)-one

Synonyms: 

Molecular weight: 416.6

CAS: 505068-32-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phosphodiesterases||Research Area|Cell Biology|Cell Signaling|cAMP Signaling||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling

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