Compounds and methods are provided for inhibiting an aldehyde dehydrogenase (ALDH). Methods of treating cancer are also provided. The ALDH-inhibitor can be a compound that is based on a cyclic guanidine, or an imidazolium core. In certain embodiments, the ALDH-inhibitor compound is a substituted cyclic guanidine, or a substituted imidazolium compound. Aspects of the methods include methods of selectively inhibiting a particular ALDH family member. In some cases, the subject compounds are ALDH1 B1-selective inhibitors. In some cases, the subject compounds are ALDH1A3-selective inhibitors.
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