A potent inhibitor of hedgehog signaling (IC50 = 20 nM in a Shh-LIGHT2 assay); blocks binding of BODIPY-cyclopamine to cells expressing Smo in a dose-dependent manner; cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum; inhibits the invasion and migration (45.9 and 43.3% inhibition

Cyclopamine-KAAD – 1 mg

Brand:
Cayman
CAS:
306387-90-6
Storage:
-20
UN-No:
Non-Hazardous - /

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay.{36120} 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.{36121} 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.{36122}  

 

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Description

A potent inhibitor of hedgehog signaling (IC50 = 20 nM in a Shh-LIGHT2 assay); blocks binding of BODIPY-cyclopamine to cells expressing Smo in a dose-dependent manner; cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum; inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells; decreases the expression of nuclear Gli1 and cytosoloic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner; increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures; upregulates expression of DR4 and DR5 in LN229 and U251 glioma cells,

Formal name: N-[6-[[2-[(3’R,3’aS,6’S,6aS,6bS,7’aR,2’R,11aS,11bR)-1,2,3,3′,3’a,4,5′,6,6′,6a,6b,7,7′,7’a,8,11,11a,11b-octadecahydro-3′,6′,10,11b-tetramethyl-3-oxospiro[9H-benzo[a]fluorene-9,2′(4’H)-furo[3,2-b]pyridin]-4′-yl]ethyl]amino]-6-oxohexyl]-benzenepropanamide

Synonyms: 

Molecular weight: 698

CAS: 306387-90-6

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Cell Signaling|Hedgehog Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking

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