The small-molecule Echinomycin is an inhibitor of hypoxia-inducible factor 1 (HIF1), an important transcription factor controlling the expression of genes that facilitate the response to a hypoxic environment. Cellular response to hypoxia involves angiogenesis, erythropoiesis, cell cycle, metabolism, and apoptosis, all of which are important for metastasis and tumor progression. Echinomycin inhibits HIF-1α and HIF-1β binding to a hypoxia-responsive element sequence of promoters of hypoxia-responsive genes (1). Echinomycin eliminated the ability of mouse lymphoma and human acute myeloid leukemia (AML) cancer stem cells to form colonies, and inhibited human AML in a xenogeneic model through preferential elimination of cancer stem cells (2). Inhibition of HIF-1α by Echinomycin can reduce the effects of acute graft-versus-host disease and extend leukemia free survival following allogeneic hematopoietic stem cell transplantation (3). Echinomycin inhibited adipogenesis and suppressed adipocyte differentiation in 3T3-L1 WAT preadipocytes, which may lead to a new therapeutic approach targeting obesity and diabetes (4).

C₅₁H₆₄N₁₂O₁₂S₂

>98%

512-64-1

Soluble in DMSO at 5 mg/mL.

Echinomycin is supplied as a lyophilized powder. For a 1 mM stock, reconstitute 1 mg of powder in 0.91 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.