Eggmanone

立即咨询

Eggmanone

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

505068-32-6

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议

产品介绍

Eggmanone (EGM1) 是一种有效的选择性磷酸二酯酶 4 (PDE4) 拮抗剂，对 PDE4D3 的 IC50 为 72 nM。 Eggmanone 对 PDE4D3 的选择性比其他 PDE 高约 40 到 50 倍。 Eggmanone 通过选择性拮抗 PDE4 发挥其 Hh 抑制作用，导致蛋白激酶 A 激活和随后的 Hh 阻断。

Cas No.	505068-32-6
别名	EGM1
化学名	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
Canonical SMILES	O=C1N(CC(C)=C)C(SCC(C2=CC=CS2)=O)=NC3=C1C4=C(S3)CCCC4
分子式	C₂₀H₂₀N₂O₂S₃
分子量	416.6
溶解度	≤0.5mg/ml in ethanol;10mg/ml in DMSO;5mg/ml in dimethyl formamide
储存条件	Store at -20℃
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	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.