aldh3a1

CB29 is a specific inhibitor of aldehyde dehydrogenase 3A1 (ALDH3A1).

Metapramine (19560 RP) is a novel psychostimulant, an N-methyl-D-aspartate receptor (NMDA) antagonist with antidepressant and anti-injury perception activity that promotes increased levels of acetylcholine in the striatum.

NCT-505 is a potent and selective inhibitor of aldehyde dehydrogenase (ALDH1A1, IC50 = 7 nM) and a weak inhibitor of hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 with IC50 values of >57 μM, 22.8 μM, 20.1 μM, and >57 μM, respectively.

EN40, as a covalent ligand, is a selective inhibitor of aldehyde dehydrogenase 3A1 (IC50: 2 uM).

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 models, where ALDH3A1-IN-4 is used to investigate aldehyde dehydrogenase-dependent detoxification pathways, enzyme–ligand binding interactions, and differential cellular response mechanisms in tumor versus non-tumor cellular systems.

ALDH3A1-IN-1 (Compound 18) is a potent ALDH3A1 inhibitor with an IC 50 of 1.61 μM. It is more effective than DEAB against patient-derived primary prostate tumor epithelial cells, both as a single agent and in combination with docetaxel [1].

ALDH3A1-IN-2 (Compound 19), a potent inhibitor of aldehyde dehydrogenases (ALDHs), demonstrates high efficacy against ALDH3A1 with an IC50 of 1.29 μM. Given the overexpression of ALDHs in multiple tumor types, including prostate cancer, ALDH3A1-IN-2 holds significant potential for cancer research [1].

ALDH1A3-IN-1 (Compound 14) is a potent inhibitor of ALDH1A3, with IC50 = 0.63 μM and Ki = 0.46 μM, and is utilized in prostate cancer research [1].

KS106 is a selective and potent ALDH inhibitor with antiproliferative and anticancer activity, inhibits ALDH1A1, ALDH2, and ALDH3A1 with IC50 of 334, 2137, and 360 nM, respectively.KS106 contributes to apoptosis, induces an increase in G2/M cell cycle arrest, and can be used to study melanoma and colon cancer.

4-Isopropoxybenzaldehyde (compound 16), a powerful ALDH1A3 inhibitor with an IC50 of 0.26 μM (cell free assay), serves as an effective ALDH3A1 substrate. But shows weak antiproliferative effect against PC3, LNCaP, and DU145 PCa cell lines with IC50>200 μM[1].

Aldi-2 is a potent and specific covalent inhibitor of aldehyde dehydrogenases (ALDHs), with IC50 values of 2.5 μM for ALDH1A1, 6.4 μM for ALDH2, and 1.9 μM for ALDH3A1. This compound is applicable in cancer research.

KS124 (compound 3) is a potent ALDH inhibitor, effectively targeting ALDH1A1, ALDH1A3, and ALDH3A1. It exhibits antiproliferative activity and induces apoptosis and reactive oxygen species (ROS) production.

NCT 501 hydrochloride is a potent and selective ALDH1A1 inhibitor (IC50 = 40 nM). Exhibits >1000-fold selectivity for ALDH1A1 over ALDH3A1, ALDH1B1, ALDH2, HPGD and HSD17β4. Also selective over a panel of 168 GPCRs. Blood-brain barrier permeable.

KS100 is a selective and potent ALDH inhibitor with antiproliferative and anticancer activities.KS100 inhibits ALDH1A1, ALDH2 and ALDH3A1 with IC50 of 334, 2137 and 360 nM, respectively.KS100 promotes apoptosis and induces cell-cycle arrest, which can be used to study colon cancer.