Eggmanone (Synonyms: EGM1) |
| Catalog No.GC10796 |
Eggmanone(EGM1)은 PDE4D3에 대한 IC50이 72nM인 강력하고 선택적인 PDE4(phosphodiesterase 4) 길항제입니다. Eggmanone은 다른 PDE에 비해 PDE4D3에 대해 약 40~50배 선택성을 보입니다. Eggmanone은 PDE4의 선택적 길항 작용을 통해 Hh 억제 효과를 발휘하여 protein kinase A 활성화 및 후속 Hh 차단으로 이어집니다.
Products are for research use only. Not for human use. We do not sell to patients.
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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