| CAS NO: | 505068-32-6 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 416.6 |
| Cas No. | 505068-32-6 |
| Formula | C20H20N2O2S3 |
| Solubility | ≤0.5mg/ml in ethanol;10mg/ml in DMSO;5mg/ml in dimethyl formamide |
| Chemical 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 |
| Canonical SMILES | O=C1N(CC(C)=C)C(SCC(C2=CC=CS2)=O)=NC3=C1C4=C(S3)CCCC4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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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