ALDH3A1-IN-4 is a selective ALDH3A1 inhibitor with an IC50 of 0.2 μM. ALDH3A1-IN-4 binds to the aldehyde-binding pocket of ALDH3A1 via hydrophobic interactions and van der Waals forces. ALDH3A1-IN-4 acts as a chemosensitizer that sensitizes ALDH3A1-expressing cancer cells to the antiproliferative effect of mafosfamide, but does not produce a sensitizing effect on non-cancer cells that do not express ALDH3A1. ALDH3A1-IN-4 is applicable to research related to lung adenocarcinoma and glioblastoma [1].
In Vitro, ALDH3A1-IN-4 (compound CB7) (10 μM; 1 min) potently inhibits ALDH3A1 activity in ALDH3A1-expressing cancer cell lysates[1]. ALDH3A1-IN-4 (10 μM; 19 h) selectively sensitizes ALDH3A1-expressing A549 and SF767 cancer cells to mafosfamide[1].
References:
[1]. Parajuli B, et al. Selective ALDH3A1 inhibition by benzimidazole analogues increase mafosfamide sensitivity in cancer cells. J Med Chem. 2014;57(2):449-461.
In Vitro, ALDH3A1-IN-4 (compound CB7) (10 μM; 1 min) potently inhibits ALDH3A1 activity in ALDH3A1-expressing cancer cell lysates[1]. ALDH3A1-IN-4 (10 μM; 19 h) selectively sensitizes ALDH3A1-expressing A549 and SF767 cancer cells to mafosfamide[1].
References:
[1]. Parajuli B, et al. Selective ALDH3A1 inhibition by benzimidazole analogues increase mafosfamide sensitivity in cancer cells. J Med Chem. 2014;57(2):449-461.