A cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner

Echinomycin – 5 mg

Brand:
Cayman
CAS:
512-64-1
Storage:
-20
UN-No:
De Minimis - 3462 / 6.1

Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription.{20741,20742} It acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the hypoxia-responsive element.{20741,20742,20743} Echinomycin reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50 value of 1.2 nM.{20741} It inhibits hypoxia-induced expression of vascular endothelial growth factor, blocking angiogenesis and altering excitatory synaptic transmission in hippocampal neurons.{20742,20740} Echinomycin also impairs expression of survivin, enhancing the sensitivity of multiple myeloma cells to melphalan.{20739}  

 

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SKU: 11049 - 5 mg Category:

Description

A cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the HRE; reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50 value of 1.2 nM

Formal name: N-(2-quinoxalinylcarbonyl)-O-[N-(2-quinoxalinylcarbonyl)-D-seryl-L-alanyl-3-mercapto-N,S-dimethylcysteinyl-N-methyl-L-valyl]-D-seryl-L-alanyl-N-methylcysteinyl-N-methyl-(8→1)-lactone, cyclic (3→7)-thioether-L-valine

Synonyms:  Antibiotic A 654I|NSC 13502|NSC 526417|Quinomycin A|SK 302B

Molecular weight: 1,101.30

CAS: 512-64-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors

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