Eggmanone (Synonyms: EGM1) |
| Catalog No.GC10796 |
Eggmanone (EGM1) es un potente y selectivo antagonista de la fosfodiesterasa 4 (PDE4) con una IC50 de 72 nM para PDE4D3. Eggmanone muestra aproximadamente 40 a 50 veces mÁs selectivo para PDE4D3 que para otras PDE. Eggmanone ejerce sus efectos inhibidores de Hh a través del antagonismo selectivo de PDE4, lo que lleva a la activaciÓn de la proteÍna quinasa A y al posterior bloqueo de Hh.
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Cas No.: 505068-32-6
Sample solution is provided at 25 µL, 10mM.
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Eggmanone is a potent and selective PDE4D3 inhibitor with IC50 value of 72 nM that antagonizes the Hedgehog signaling pathway [1].
Hedgehog (Hh) signaling plays an important role in vertebrate development, and its dysregulation is a driver of numerous malignancies. Phosphodiesterase 4 (PDE4) is a target for Hh inhibition. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade [1].
Eggmanone is a potent and selective PDE4 inhibitor that antagonizes the Hedgehog signaling pathway. In Sufu-/- mouse embryonic fibroblasts (MEFs), Eggmanone significantly reduced transcription levels of Gli1 and Ptc1. Eggmanone functioned upstream of Gli processing and nuclear translocation to exert its Hh-inhibitory effects. Eggmanone exhibited potent antagonism of PDE4D3 with IC50 value of 0.072 μM, approximately 40- to 50-fold selective over PDE3A, PDE10A2, and PDE11A4 (IC50s = 3, 3.05, and 4.08 μM, respectively). In Shh-Light2 cells transfected with PDE4D3, Eggmanone restored the increased Hh signaling [1].
Reference:
[1]. Williams CH, Hempel JE, Hao J, et al. An in vivo chemical genetic screen identifies phosphodiesterase 4 as a pharmacological target for hedgehog signaling inhibition. Cell Rep. 2015 Apr 7;11(1):43-50.
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