KAAD-Cyclopamine

Description: Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells. Target: Others. Smiles: C[C@H]1[C@]2(C(C)=C3[C@@](CC2)([C@]4([C@](C3)([C@]5(C)C(=CC4)CC(=O)CC5)[H])[H])[H])O[C@]6([C@]1(N(CCNC(CCCCCNC(CCC7=CC=CC=C7)=O)=O)C[C@@H](C)C6)[H])[H]