ALDH1 Inhibitor

Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC₅₀ of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.

NCT-501 is a reversible, non-competitive, selective, blood-brain barrier-permeable ALDH1A1 inhibitor with an IC₅₀ of 40 nM. NCT-501 inhibits the AKT-β-catenin signaling pathway, induces necroptosis in nasopharyngeal carcinoma cells, suppresses their proliferation and inhibits stem cell spheroid formation. NCT-501 can be used in research related to nasopharyngeal carcinoma, esophageal squamous cell carcinoma and malignant tumors.

IGUANA-1 is a potent and selective ALDH1B1 inhibitor. IGUANA-1 shows no significant mitochondrial toxicity. IGUANA-1 has antitumor activity.

CM037 is a highly selective and competitive ALDH1A1 inhibitor (IC₅₀=4.6 μM). CM037 blocks the catalytic activity of ALDH1A1, thereby inhibiting the activation of the downstream HIF-1α/VEGF pathway. CM037 is mainly used to study the ALDH1A1-mediated regulation of cancer stem cells (CSCs) and angiogenesis, especially in breast cancer, showing the potential to inhibit tumor angiogenesis and stem cell characteristics.

Z3405279217 is an inhibitor of ALDH1A3 and ALDH1A1, with an IC₅₀ value of 12.9 μM against ALDH1A3. Z3405279217 can be used in studies of non-small cell lung cancer and glioblastoma.

BM-51 is a selective inhibitor of CYP4Z1, with a human IC₅₀ value of 91.7 nM. BM-51 binds to amino acid residues of CYP4Z1, thereby inhibiting its enzymatic activity. BM-51 downregulates the protein expression of stem cell markers (ALDH1A1, SOX2, OCT3/4 and KLF4) in cancer cells, inhibits cancer cell migration and invasion, and exhibits low toxicity to normal cells/tissues. BM-51 suppresses tumor initiation capacity and enhances the chemotherapeutic efficacy of Doxorubicin (HY-15142A). BM-51 can be used in breast cancer-related research.

ALDH1A3-IN-1 (Compound 14) is a potent ALDH1A3 inhibitor, with an IC₅₀ of 0.63 μM and a K_i of 0.46 μM. ALDH1A3-IN-1 can be studied in prostate cancer.

ALDH1A3-IN-3 is a potent inhibitor of ALDH1A3, with an IC₅₀ of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate which limits its application as a selective inhibitor. ALDH1A3-IN-3 can be used for the research of prostate cancer.

CM010 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC₅₀s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM010 does not inhibit any of the other ALDH family members. CM010 can regulate metabolism and has anti-cancer activity.

MCI-INI-3 is a selective ALDH1A3 inhibitor, with an IC₅₀ of 0.46 μM and a K_i of 0.55 μM against hALDH1A3. MCI-INI-3 inhibits retinoic acid (HY-14649) biosynthesis. MCI-INI-3 can be used in research related to glioblastoma and glioma.

KOTX1 is an orally active and selective ALDH1A3 inhibitor. KOTX1 improves glucose tolerance, insulin secretion and blood sugar levels in diabetic mouse models.

NCT-506 is an orally bioavailable aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with an IC₅₀ of 7 nM.

ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC₅₀ of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.

KS106 is a potent ALDH inhibitor with IC₅₀s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase.

ALDH1A1-IN-2 (compound 297) is a potent inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1). Aldehyde dehydrogenases (ALDH) constitute a family of enzymes that play a critical role in oxidizing various cytotoxic xenogenic and biogenic aldehydes. ALDH1A1-IN-2 has the potential for the research of cancer, inflammation, or obesity.

Nitrefazole (EMD-15700) is an aldehyde dehydrogenase (ALDH) inhibitor. Nitrefazole specifically inhibits human liver ALDH I and human erythrocyte ALDH isozymes, but does not alter the activity of human liver ALDH II or human placental ALDH. Nitrefazole effectively promotes exosome secretion in prostate cancer cells by increasing the levels of Alix, nSMase2, Rab27a and p-ERK. Nitrefazole can be used in studies related to prostate cancer.

NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC₅₀ of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC₅₀s, >57, 22.8, 20.1, >57 μM).

ALDH1A1-IN-4 (compound A1) is a potent inhibitor of aldehyde dehydrogenase (ALDH) A1, with IC₅₀ value of 0.32 μM. ALDH1A1-IN-4 plays an important role in cancer research.

ALDH1A1-IN-5 (compound 25) is a potent aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitor with EC₅₀ value of 83, 45, 43 µM for ALDH1A1, ALDH1A2, ALDH1A3, respectively. ALDH1A1-IN-5 has the potential for the research of high-grade serous ovarian cancer (HGSOC).

NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC₅₀ of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC₅₀ >57 μM).