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Dichloro-all-trans-retinone (DAR) is an irreversible inhibitor of retinaldehyde dehydrogenase (RALDH/ALDH1A) with IC50 of 434/55/161 nM for RALDH1/RALDH2/RALDH3.Dichloro-all-trans-retinone has no activity on human mitochondrial ALDH2.Dichloro-all-trans-retinone inhibits ATRA synthesis in a RALDH2 expressing cell line with IC50 of 3 uM.The retinaldehyde dehydrogenase (RALDH, also ALDH1A) subfamily consists of three members, RALDH1 (ALDH1A1), RALDH2 (ALDH1A2), and RALDH3 (ALDH1A3), which synthesize all-trans-retinoic acid (ATRA) from retinaldehyde.
AD-9308 is a water-soluble, orally bioavailable, potent, and highly selective ALDH2 activator, AD-9308 is a valine ester prodrug of a potent and selective small molecule ALDH2 activator AD-5591.
AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1.
AD-5591 (100 μM) significantly increases the enzymatic activity of recombinant WT and mutant human ALDH2 proteins.
AD-5591 is the active form of AD-9308.
MCI-INI-3 is a potent, selective, competitive inhibitor of ALDH1A3 (Ki=0.55 uM), shows poor inhibitory effect on the structurally related isoform ALDH1A1 (>140-fold selectivity).MCI-INI-3 also displays on inhibition against six isoforms of ALDH (ALDH16A1, ALDH7A1, ALDH9A1, ALDH2, ALDH1B1, ALDH18A1).MCI-INI-3 demonstrates selective binding to ALDH1A3 in glioma stem cell lysates, inhibits ALDH activity and affects RA synthesis in cells.
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
Mirivadelgat is an activator of aldehyde dehydrogenase 2 activator. Mirivadelgat is promising for research of interstitial lung disease-pulmonary hypertension and cancers.
STA-55 is a broad-spectrum activity-based probe of aldehyde dehydrogenase family, can be used to identify therapy resistance biomarkers in cancer and to validate target engagement of ALDH drug candidates.
NCT-507 (NCT507) is a potent, selective, orally available ALDH1A1 inhibitor with IC50 of 7 nM (hALDH1A1), exhibits high specificity over other ALDH isozymes and unrelated dehydrogenases.