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Eggmanone

 
Catalog No.
C4796
PDE4的选择性抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 9,425.00
Ship with 10-15 days

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A

背景

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.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt416.6
Cas No.505068-32-6
FormulaC20H20N2O2S3
Solubility≤0.5mg/ml in ethanol;10mg/ml in DMSO;5mg/ml in dimethyl formamide
Chemical Name5,6,7,8-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
SDFDownload SDF
Canonical SMILESO=C1N(CC(C)=C)C(SCC(C2=CC=CS2)=O)=NC3=C1C4=C(S3)CCCC4
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质量控制

质量控制和MSDS

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化学结构

Eggmanone