Eggmanone

Eggmanone is a potent and selective PDE4D3 inhibitor with IC50 value of 72 nM that antagonizes the Hedgehog signaling pathway . 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 . 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 .

Product information

CAS Number: 505068-32-6

Molecular Weight: 416.58

Formula: C20H20N2O2S3

Chemical Name: 4-(2-methylprop-2-en-1-yl)-5-{[2-oxo-2-(thiophen-2-yl)ethyl]sulfanyl}-8-thia-4,6-diazatricyclo[7.4.0.0²,⁷]trideca-1(9),2(7),5-trien-3-one

Smiles: CC(=C)CN1C(=NC2SC3CCCCC=3C=2C1=O)SCC(=O)C1=CC=CS1

InChiKey: XAKJIQPEGSCYIP-UHFFFAOYSA-N

InChi: InChI=1S/C20H20N2O2S3/c1-12(2)10-22-19(24)17-13-6-3-4-7-15(13)27-18(17)21-20(22)26-11-14(23)16-8-5-9-25-16/h5,8-9H,1,3-4,6-7,10-11H2,2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.