A potent, cell-permeable analog of Cyclopamine that specifically inhibits the Hedgehog (Hh) signaling with similar or lower toxicity (IC50 = 20nM in Shh-LIGHT2 assay; 50nM in p2Ptch-/-cells; 500nM in SmoA1-LIGHT cells). Binds to SmoA1 and promotes its exit from the endoplasmic reticulum. Suppresses both the ShhNp-induced pathway activity and SmoA1-induced reporter activity. Shown to sensitize human glioma cells to TRAIL-induced apoptosis.
Synonyms:3-Keto-N-(aminoethyl-aminocaproyl-dihydrocinnamoyl)cyclopamine, KAAD-Cyclopamine, Shh Signaling Antagonist II
Molecular Formula:C₄₄H₆₃N₃O₄
Primary Target:Hh signaling in Shh-light2 assay
Primary Target IC50:20nM
Secondary Target:in P2Ptch-/-cells (IC50 = 50nM)
Solubility:DMSO, EtOH, or MeOH
Molecular Weight:698
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
