CAY10585, 10 mg

A novel small molecule inhibitor of hypoxia inducible factor-1α (HIF-1α) from STEMCELL Technologies targets the oxygen-regulated subunit of the heterodimeric HIF-1 transcription factor. Under normoxic conditions HIF-1α is targeted for destruction by the ubiquitin-proteasome system, whereas under hypoxic conditions it accumulates and dimerizes with HIF-1β to promote transcription of genes involved in angiogenesis, glycolysis, growth factor signaling, tumor invasion, and metastasis. The inhibitor blocks HIF-1 accumulation and prevents HIF-1 transcriptional activity, with reported IC₅₀ values of 2.6 and 0.7 µM in Hep3B and AGS cell reporter assays.

Supplied as a crystalline solid, the compound has the chemical formula C₂₆H₂₉NO₅, a molecular weight of 435.5 g/mol, and a purity of ≥ 97%. It has low solubility in aqueous media but is soluble in DMSO at ≤ 20 mM. The product is stable at -20°C as supplied, should be protected from prolonged exposure to light, and remains stable for 12 months from date of receipt. For cell culture use, stock solutions should be diluted into culture medium immediately before use, with final DMSO concentration kept at or below 0.1% to avoid potential cell toxicity.

Differentiation is the primary application listed in the manufacturer's small molecules catalogue. Published applications include inhibition of BMP9- and HIF-1-induced osteogenic differentiation in mesenchymal stem cells (Hu et al.) and rescue of cardiomyocyte differentiation in Fgfr1(-/-) mouse embryonic stem cells (Crescini et al.).