Biochem/physiol Actions

Primary TargetALDH1A1

Cell permeable: yes

General description

A cell permeable benzothieno[3,2-d]pyrimidone derivative that acts as a selective, substrate competitive inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1; K_i = 300 nM; IC₅₀ = 4.6 µM) in ovarian cancer spheroids. Does not affect the activity of other related orthologs, including ALDH1A2, ALDH1A3, ALDH2 and ALDH3A1 even at higher concentrations (>100 µM). Enhances sensitization of IGROV1 ovarian carcinoma cells to cisplatin. Disrupts spheroid formation and reduces viability of ovarian cancer cells.

A cell permeable benzothieno[3,2-d]pyrimidone derivative that acts as a selective, substrate competitive inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1; K_i = 300 nM; IC₅₀ = 4.6 µM) in ovarian cancer spheroids. Does not affect the activity of other related orthologs, including ALDH1A2, ALDH1A3, ALDH2 and ALDH3A1 even at higher concentrations (>100 µM). Enhances sensitization of IGROV1 ovarian carcinoma cells to cisplatin. Disrupts spheroid formation and reduces viability of ovarian cancer cells.Please note that the molecular weight for this compound is batch-specific due to variable water content.

A cell permeable, selective, substrate competitive inhibitor of aldehyde dehydrogenae 1A1 (ALDH1A1; K_i = 300 nM; IC₅₀ = 4.6 µM). Does not affect the activity of other related orthologs.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Condello, S., et al. 2014. Oncogene.33, in press.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)